82
1
1
38
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T22019 |
ABT 724 trihydrochloride
|
Dopamine Receptor | GPCR/G Protein; Neuroscience |
ABT 724 trihydrochloride 是一种有效的选择性 D4 受体激动剂(EC50 = 12.4 nM,14.3 nM 和 23.2 nM,分别对人、大鼠和雪貂)。 ABT-724 trihydrochloride 可用于勃起功能障碍研究。 | |||
T7834 |
ABT-724
2 - [(4-吡啶-2-基哌嗪-1-基)甲基]-1H-苯并咪唑 |
Dopamine Receptor | GPCR/G Protein; Neuroscience |
ABT-724 是高度选择性的多巴胺D4受体激动剂,对人多巴胺D4受体的EC50=12.4 nM。它是大鼠D4(EC50为 14.3 nM) 和雪貂D4受体 (EC50为 23.2 nM) 的有效部分激动剂,对多巴胺 D1,D2,D3或 D5受体没有影响。它可用于勃起功能障碍的研究,并具有较少的副作用。 | |||
T22904 |
L-745870 trihydrochloride
L-745870三盐酸盐,L-745,870 trihydrochloride |
Dopamine Receptor; Sigma receptor; 5-HT Receptor; Adrenergic Receptor | GPCR/G Protein; Neuroscience |
L-745870 trihydrochloride 是可透过血脑屏障的、选择性的、具有口服活性的多巴胺D4受体拮抗剂,Ki=0.43 nM,而对 D2(Ki 为 960 nM) 和 D3(Ki 为 2300 nM) 受体的亲和力相对较弱,对 5-HT2受体,sigma 位点和 α-肾上腺素受体表现出中等亲和力。 | |||
T60917 |
Dopamine D4 receptor antagonist-1
|
Others | Others |
Dopamine D4 receptor antagonist-1 可用于研究精神分裂症。Dopamine D4 receptor antagonist-1 是多巴胺D4受体 (DRD4) 的选择性拮抗剂。Dopamine D4 receptor antagonist-1 对Hd4.2的Ki 值为 9.0 nM。 | |||
T12761 |
Ro 10-5824 dihydrochloride
|
Dopamine Receptor | GPCR/G Protein; Neuroscience |
Ro 10-5824 dihydrochloride 是选择性的多巴胺D4 受体部分激动剂,Ki=5.2 nM。 | |||
T12383 |
PD 168568 dihydrochloride
PD 168568 (dihydrochloride),二盐酸PD168568 |
Dopamine Receptor | GPCR/G Protein; Neuroscience |
PD 168568 dihydrochloride (PD 168568 (dihydrochloride)) 是一种口服有效的,选择性的 D4 受体拮抗剂,其 Ki 值为 8.8 nM。 | |||
T15270 |
Fananserin
RP 62203,法南色林 |
Dopamine Receptor; 5-HT Receptor | GPCR/G Protein; Neuroscience |
Fananserin 是一种有效的、特异性的、口服活性的 5-HT2 拮抗剂(大鼠 5-HT2A 的 Ki = 0.37 nM)。 Fananserin 是人 D4 受体的拮抗剂 (Ki = 2.93 nM)。 | |||
T10213 |
A-437203
ABT-925,A37203,Lu201640 |
Dopamine Receptor | GPCR/G Protein; Neuroscience |
A-437203 (Lu201640) 是一种基于1H-pyrimidin-2-one scaffold 的、具有选择性的、新型强效的d3受体拮抗剂,对 D2, D3, 和 D4 受体,的Ki 值分别为 71, 1.6 和 6220 nM。 | |||
T11799 |
L-745870 hydrochloride
|
Dopamine Receptor | GPCR/G Protein; Neuroscience |
L-745870 hydrochloride 是可透过血脑屏障的、选择性的、具有口服活性的多巴胺 D4受体拮抗剂,Ki=0.43 nM。它对 D2(Ki 为 960 nM) 和 D3(Ki 为 2300 nM) 受体的亲和力相对较弱,对 5-HT2受体,sigma 位点和 α-肾上腺素受体表现出中等亲和力。 | |||
T23066 |
NGD 94-1
|
Dopamine Receptor | GPCR/G Protein; Neuroscience |
NGD 94-1 是一种选择性的 D4 受体拮抗剂,对D4受体的亲和力为3 nM,而对D1、D2、D3和D5受体的亲和力大于2 pM。NGD 94-1 可用研究认知障碍等精神性疾病。 | |||
T5047 |
PD-168077 maleate
|
Dopamine Receptor | GPCR/G Protein; Neuroscience |
PD-168077 maleate 是多巴胺 D4受体选择性激动剂,其 Ki=9 nM。 | |||
T27979 |
Masilukast
ICI-D-3523,ZD-3523,ICI D-3523,MCC-847,SA-09012,D-3523 |
Leukotriene Receptor | GPCR/G Protein |
Masilukast(MCC-847) 是一种口服的白三烯D4 (LTD4) 受体拮抗剂,可用于研究与炎症相关的疾病。 | |||
T12480 |
Pipamperone
Floropipamide,McN-JR 3345,酰胺哌啶酮,R 3345 |
Others; Dopamine Receptor; 5-HT Receptor | GPCR/G Protein; Neuroscience; Others |
Pipamperone (McN-JR 3345) 是5-HT2A 受体和D4受体的高亲和力拮抗剂,也是D2受体的低亲和力拮抗剂,pKi 分别为 8.2、8.0 和 6.7。 | |||
T27060 |
CP-226269
CP 226269,CP226269 |
Dopamine Receptor | GPCR/G Protein; Neuroscience |
CP-226269 是一种高效的多巴胺 D4 受体 (dopamine D4 receptor) 激动剂,可以调节钙通量,其 EC50 值为32.0 nM。CP 226269 可用于研究精神分裂症等神经系统疾病。 | |||
T5397 |
A-381393
|
Dopamine Receptor | GPCR/G Protein; Neuroscience |
A-381393 是选择性、可透过血脑屏障的多巴胺 D4受体拮抗剂,对人多巴胺 D4.4,D4.2和 D4.7受体的 Ki 分别为 1.5,1.9 和 1.6 nM,选择性是对 D1,D2,D3,D5多巴胺受体的 2700 多倍,对 5-HT2A 的选择性适中,Ki=370 nM。 | |||
T24055 |
FAUC 213
FAUC213,FAUC-213 |
Dopamine Receptor | GPCR/G Protein; Neuroscience |
FAUC 213 是一种具有口服活性的‘、高度选择性的、可透过血脑屏障的多巴胺 D4受体完全拮抗剂,对 hD4.4的 Ki=2.2 nM。它对 D2和 D3受体的活性较低,对于 hD2、hD3的 Ki 分别为 3.4 μM、5.3 μM。它表现出非典型的抗精神病活性。 | |||
T2631 |
WAY-100635 Monomaleate
|
Dopamine Receptor; 5-HT Receptor | GPCR/G Protein; Neuroscience |
WAY-100635 maleate 是一种选择性的5-hydroxytryptamine 1A 受体拮抗剂,IC50值为 0.91 nM,Ki 值为 0.39 nM。它也是多巴胺 D4受体激动剂,对于5-HT1A 和 α1-肾上腺素的 pIC50值分别为 8.9 和 6.6。 | |||
T5158 |
N-Desmethylclozapine
N-去甲基氯氮平,Desmethylclozapine,Normethylclozapine,Norclozapine |
Virus Protease; Dopamine Receptor; 5-HT Receptor; Opioid Receptor; AChR; Drug Metabolite | Endocrinology/Hormones; GPCR/G Protein; Metabolism; Microbiology/Virology; Neuroscience |
N-Desmethylclozapine (Desmethylclozapine) 是非典型抗精神病药 Clozapine 的主要活性代谢产物。它是血清素受体亚型 5-HT2C 的拮抗剂,IC50值为7.1 nM。 它也是多巴胺 D4 受体的拮抗剂和δ-阿片受体的激动剂。 | |||
T30098 |
Aplindore Fumarate
Aplindore,DAB-452 Fumarate,DAB-452 |
Dopamine Receptor; 5-HT Receptor; Adrenergic Receptor | GPCR/G Protein; Neuroscience |
Aplindore Fumarate (DAB-452)是一种小分子多巴胺 D2 受体部分激动剂,Aplindore Fumarate 对多巴胺D2 和D3 受体表现出高亲和力,对多巴胺D4、5-羟色胺(5-HT2)和α1-肾上腺素受体表现出低亲和力。Aplindore Fumarate 可用于研究帕金森和精神分裂症。 | |||
T28167 |
NGB 2904
NGB2904 HCl,NGB-2904,NGB2904 |
Others; Dopamine Receptor; 5-HT Receptor | GPCR/G Protein; Neuroscience; Others |
NGB 2904 是一种具有口服活性的、选择性的多巴胺(DA) D3受体拮抗剂,可用于具可卡因成瘾。 | |||
T31602 |
Ecopipam
Sch-39166,UNII-0X748O646K,Sch 39166 |
Dopamine Receptor | GPCR/G Protein; Neuroscience |
Ecopipam (UNII-0X748O646K) 是一种有效的、选择性、具有口服活性的多巴胺 D1/D5 受体拮抗剂,Ki 值分别为 1.2 nM 和 2.0 nM。Ecopipam 对 D2、D4、5-HT 和 α2a 受体 (Ki=0.98,5.52,0.08 和 0.73 μM) 显示出超过 40 倍的选择性。Ecopipam 可用于精神分裂症、可卡因成瘾和肥胖症的研究。 | |||
T6736 |
Zafirlukast
Vanticon,ICI 204219,Accolate,扎鲁司特 |
Leukotriene Receptor | GPCR/G Protein |
Zafirlukast (ICI 204219) 是一种可口服的白三烯 D4受体拮抗剂,具有平喘、抗炎和抗菌作用。 | |||
T1476 |
Pramipexole
SND 919,普拉克索 |
Dopamine Receptor | GPCR/G Protein; Neuroscience |
Pramipexole (SND 919) 是能够透过血脑屏障的 D2 型多巴胺受体的选择性激动剂,对 D2 型受体、D2、D3、D4亚型受体的Ki 分别为 2.2 nM、3.9 nM、0.5 nM、1.3 nM。它可用于研究帕金森综合症和腿多动综合征。 | |||
T14767 |
BP 897 hydrochloride
|
Dopamine Receptor | GPCR/G Protein; Neuroscience |
BP 897 hydrochloride 是有效的部分多巴胺 D3受体激动剂和弱 D2受体拮抗剂,在多巴胺 D3 受体 (Ki=0.92 nM) 上显示出高亲和力,而在 D2 受体上显示出 70 倍的低亲和力 (Ki=61 nM)。它表现出对可卡因寻求行为的选择性抑制。 | |||
T9100 |
BP 897
2-Naphthalenecarboxamide, N-[4-[4-(2-methoxyphenyl)-1-piperazinyl]butyl]- |
Dopamine Receptor | GPCR/G Protein; Neuroscience |
BP 897 (2-Naphthalenecarboxamide, N-[4-[4-(2-methoxyphenyl)-1-piperazinyl]butyl]-) 是一种有效的部分多巴胺D3受体激动剂和弱D2受体拮抗剂,在多巴胺 D3 受体(Ki=0.92 nM) 上显示出高亲和力,而在 D2 受体上显示出 70 倍的低亲和力 (Ki=61 nM)。它表现出对可卡因寻求行为的选择性抑制。 | |||
T11463 |
GR 103691
|
Dopamine Receptor | GPCR/G Protein; Neuroscience |
GR 103691 是选择性的多巴胺 D3受体拮抗剂,Ki=0.4 nM。它对人多巴胺 D3的选择性超过 D4和 D1的 100 倍以上。 | |||
T23380 |
Sonepiprazole
|
Dopamine Receptor | GPCR/G Protein; Neuroscience |
Sonepiprazole 是D4多巴胺受体选择性拮抗剂,与rD4多巴胺受体,hD4.2多巴胺受体,rD2多巴胺受体和组胺H1受体结合的Ki 分别为 3.6、10.1、5147 和 7430 nM。 | |||
T1539 |
Iloperidone
伊潘立酮,HP 873 |
Dopamine Receptor; 5-HT Receptor; Adrenergic Receptor | GPCR/G Protein; Neuroscience |
Iloperidone (HP 873) 是一种D2/5-HT2受体拮抗剂,是非典型抗精神病药,可治疗精神分裂症。 | |||
T3148 |
MK-571 sodium
L-660711 (sodium salt),L-660711 sodium salt,Verlukast sodium,L-660711,MK571,MK-571 sodium salt,Propanoic acid |
Leukotriene Receptor; LTR | GPCR/G Protein; Immunology/Inflammation |
MK-571 sodium (L-660711 sodium salt) 是一种可口服的选择性白三烯 D4受体拮抗剂,在豚鼠和人肺膜的 Ki 分别为0.22 和 2.1 nM。 | |||
T12252 |
NRA-0160
|
Dopamine Receptor | GPCR/G Protein; Neuroscience |
NRA-0160 is a selective antagonist of dopamine D4 receptor(Ki of 0.48 nM) | |||
T7635L |
Raclopride tartrate
FLA 870,FLA-870,FLA870 |
Others | Others |
Raclopride is a selective antagonist on D2 dopamine receptor ( D2 Ki: 1.8 nm, D3 Ki: 3.5 nm, D4 Ki: 2400, D1 Ki: 18000 nM). | |||
T6951 |
Pramipexole dihydrochloride hydrate
Pramipexole 2HCl Monohydrate,普拉克索盐酸盐水合物,Mirapex,普拉克索 |
Dopamine Receptor | GPCR/G Protein; Neuroscience |
Pramipexole dihydrochloride hydrate (Mirapex) 是选择性的,具有血脑屏障 (BBB) 渗透性的 D2 型多巴胺受体激动剂,对 D2 型受体、D2、D3、D4亚型受体的 Ki 分别为 2.2 nM、3.9 nM、0.5 nM、1.3 nM,可用于研究帕金森综合症和腿多动综合征。 | |||
T11799L |
L-745870
|
Dopamine Receptor | GPCR/G Protein; Neuroscience |
L-745870 is a high-affinity and selective human dopamine D4 receptor antagonist (Ki: 0.43 nM). L-745870 has excellent brain penetration. It considerably weaker D2 (Ki: 960 nM) and D3 (Ki: 2300 nM) receptors affinity. | |||
T25407 |
FAUC-113
FAUC113 |
Others | Others |
FAUC-113 is an antagonist of Dopamine D4 receptor. | |||
T14088 |
ABT-670
|
Dopamine Receptor | GPCR/G Protein; Neuroscience |
ABT-670 is a selective agonist of dopamine D4 receptor. For human D4, ferret D4, and rat D4, the EC50 values are 89 nM, 160 nM, and 93 nM , respectively. | |||
T27893 |
LY 203647
LY203647,LY-203647 |
Others | Others |
LY 203647 is a antagonist of leukotriene D4 and E4 receptor. | |||
T28505 |
RBI-257 Maleate
RBI257 Maleate,p-Iodo-U-101958 Maleate,RBI 257 Maleate,p-Iodo U-101958 Maleate |
Others | Others |
RBI-257 Maleate is a highly potent selective ligand of dopamine D4 receptor. | |||
T11764 |
KP496
|
Others | Others |
KP496 is a selective, dual antagonist for Thromboxane A2 receptor and Leukotriene D4 receptor. | |||
T69095 |
FAUC-179
|
Others | Others |
FAUC-179 is a selective dopamine D4 receptor partial agonist. | |||
T23170 |
PNU-96415E
PNU 96415E |
Others | Others |
dopamine D4 and serotonergic 5-HT2A receptor antagonist | |||
T24304 |
L 648051
4-Apsob,L48051,L-648051 |
Others | Others |
L 648051 is a leukotriene D4 receptor antagonist. | |||
T24358 |
L 741742 (free base)
L-741,742,L-741742,L 741742,L 741,742,L741742 |
Others | Others |
L 741742 is an effective and highly selective antagonist of the D4 dopamine receptor (Ki: 1700, 770, and 3.5 nM at cloned human D2, D3, and D4 receptors). | |||
T19691 |
A412997
|
Others | Others |
A412997 is a selective agonist of dopamine D4 receptor. | |||
T19666 |
PD168,077
PD-168,077,PD 168,077 |
Others | Others |
PD168,077 is an agonist of dopamine D4 receptor. It has a facilitatory effect on memory consolidation. | |||
T27777 |
L-750,667 TriHydrochloride
L 750,667,L750,667,L-750,667 |
Others | Others |
L-750,667 TriHydrochloride is a selective antagonist of D4 dopamine receptor. | |||
T27063 |
CP-293019
CP293019 |
Others | Others |
CP-293019 is a potent, selective antagonist of dopamine D4 receptor. | |||
T22903 |
L-741,742 hydrochloride
|
Others | Others |
highly potent and selective D4 dopamine receptor antagonist | |||
T69466 |
FAUC-299
|
Others | Others |
FAUC-299 is a dopamine D4 receptor agonist. | |||
T70662 |
UCSF924NC
|
Others | Others |
UCSF924NC is the recommended negative control compound for the high-affinity dopamine D4 receptor (DRD4) partial agonist UCSF924. UCSF924NC exhibits a 1/2500-fold reduced D4 affinity when compared with that of UCSF924. | |||
T24056 |
FAUC-312
FAUC 312 |
Others | Others |
FAUC-312 is a potent and selective agonist of the dopamine D4 receptor. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T15686 |
L-741626
3-(4-(4-Chlorophenyl-4-hydroxypiperidino)methyl)indole |
Dopamine Receptor | GPCR/G Protein; Neuroscience |
L-741626 (3-(4-(4-Chlorophenyl-4-hydroxypiperidino)methyl)indole) 是D2多巴胺受体选择性拮抗剂,对人 D2、D3 和 D4 受体的Ki 分别为 2.4、100 和 220 nM。 |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPH-03749 |
CYSLTR1 Protein, Human, Recombinant (His)
Cysteinyl leukotriene receptor 1,G-protein coupled ... |
Human | E. coli |
Receptor for cysteinyl leukotrienes mediating bronchoconstriction of individuals with and without asthma. Stimulation by LTD4 results in the contraction and proliferation of smooth muscle, edema, eosinophil migration and damage to the mucus layer in the lung. This response is mediated via a G-protein that activates a phosphatidylinositol-calcium second messenger system. The rank order of affinities for the leukotrienes is LTD4 >> LTE4 = LTC4 >> LTB4. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T11197 |
Enclomiphene D4 hydrochloride
(E)-Clomiphene D4 hydrochloride,Enclomifene D4 hydrochloride,trans-Clomiphene D4 hydrochloride |
Others | Others |
Enclomiphene D4 hydrochloride ((E)-Clomiphene D4 hydrochloride; trans-Clomiphene D4 hydrochloride; Enclomifene D4 hydrochloride) is a potent and orally active oestrogen receptor antagonist, with antioestrogenic property.Enclomiphene D4 hydrochloride ((E)-Clomiphene D4 hydrochloride; trans-Clomiphene D4 hydrochloride; Enclomifene D4 hydrochloride) is a deuterium labeled Enclomiphene. | |||
T11675 |
Irbesartan-d4
厄贝沙坦 D4,SR-47436 D4,BMS-186295 D4 |
Others | Others |
Irbesartan D4, a deuterium-labeled variant of Irbesartan, is a highly potent and specific antagonist of the angiotensin II type 1 (AT1) receptor. | |||
T12329 |
Ospemifene D4
FC-1271a D4 |
Estrogen/progestogen Receptor | Endocrinology/Hormones |
Ospemifene D4 is a deuterium labeled Ospemifene. Ospemifene is a selective and orally active modulator of estrogen receptor. | |||
T11934 |
Macitentan-d4
Macitentan D4,ACT-064992 D4 |
Endothelin Receptor | GPCR/G Protein |
Macitentan-d4 (ACT-064992 D4) 是一种 Macitentan 氘代物,可被当作非多肽 ETA 和 ETB (内皮素受体)双拮抗剂。Macitentan-d4 比 Macitentan 毒性更低,半衰期更长,可用于研究由内皮素受体介导介导的疾病。 | |||
T11869 |
Losartan (D4 Carboxylic Acid)
E-3174 D4,氯沙坦羧酸 D4,EXP-3174 D4 |
Others | Others |
Losartan D4 Carboxylic Acid is the deuterium labeled Losartan, which is an angiotensin II receptor antagonist. | |||
T11591 |
Hydroxyzine D4
羟嗪 D4 |
Others | Others |
Hydroxyzine D4 is a deuterium-labeled variation of Hydroxyzine, a chemical compound known for its anticholinergic, anxiolytic, and analgesic properties. It is classified as a heterocyclic histamine H1-receptor antagonist. | |||
T73713 |
Flupirtine-d4 hydrochloride
|
||
Flupirtine-d4 (D 9998-d4) hydrochloride,Flupirtine (D 9998) hydrochloride的氘代物,为神经元钾通道开放剂,具有拮抗NMDA受体的作用。 | |||
T11536 |
Haloperidol (D4')
Haloperidol D4',氟哌啶醇 (D4') |
Others | Others |
Haloperidol D4' is deuterium-labeled haloperidol. Haloperidol is a dopamine D2 receptor antagonist. | |||
T19233 |
Cetirizine D4 dihydrochloride
Cetirizine D4 dihydrochloride (1219803-84-5 free base) |
Others | Others |
Cetirizine D4 dihydrochloride is a deuterium-labeled Cetirizine. Cetirizine is a second-generation antihistamine and a long-acting histamine H1-receptor antagonist. | |||
T12300 |
Olmesartan-d4
RNH-6270 D4,奥美沙坦 D4 |
Others | Others |
Olmesartan D4 is the deuterium labeled Olmesartan. Olmesartan is an antagonist of angiotensin II receptor (AT1R) used to treat high blood pressure. | |||
T10670 |
Candesartan-d4
坎地沙坦 D4,CV-11974 D4 |
Others | Others |
Candesartan D4 is the deuterium labeled Candesartan. Candesartan is an antagonist of angiotensin II receptor. | |||
T11870 |
Losartan D4
氯沙坦 D4,DuP-753 D4 |
Others | Others |
Losartan D4, the deuterium-labeled version of Losartan, functions as an angiotensin II receptor antagonist. It inhibits the interaction between angiotensin II and AT1 receptors by competing for binding, achieving an IC50 value of 20 nM. | |||
T10769 |
Cetirizine D4
|
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Cetirizine D4 is a deuterium-labeled Cetirizine. Cetirizine is a second-generation antihistamine and a long-acting histamine H1-receptor antagonist. | |||
T12618 |
Quetiapine-d4 fumarate
Quetiapine D4 fumarate,富马酸奎硫平 D4 |
Others | Others |
Quetiapine D4 fumarate is the deuterium labeled Quetiapine fumarate. Quetiapine fumarate is a agonist of 5-HT receptors and a antagonist of dopamine receptor,with antidepressant and anxiolytic. | |||
T12618L |
Quetiapine-d4 hemifumarate
半富马酸奎硫平 D4 |
Others | Others |
Quetiapine D4 hemifumarate is the deuterium labeled Quetiapine hemifumarate. Quetiapine hemifumarate is a agonist of 5-HT receptors and a antagonist of dopamine receptor,with ntidepressant and anxiolytic. | |||
TMIJ-0248 |
Stanolone-d4
|
||
Stanolone-d4 是 Stanolone 的氘代化合物。Stanolone 的 CAS 号为 521-18-6。Dihydrotestosterone(DHT) 是睾酮的强效雄激素代谢物。它是雄激素受体的激动剂。 | |||
TMID-0064 |
Androsterone-d4
|
||
Androsterone-d4 是 Androsterone 的氘代化合物。Androsterone 的 CAS 号为 53-41-8。Androsterone 是睾酮的代谢产物,可以激活法尼醇 X 受体。 | |||
T11295 |
Flibanserin-d4
BIMT-17BS D4,BIMT-17 D4,Flibanserin D4 |
Others | Others |
Flibanserin, a compound identified as BIMT-17, acts as a complete agonist at the serotonin 5-HT1A receptor, with a binding affinity (Ki) of 1 nM, while functioning as an antagonist at the 5-HT2A receptor with a 49 nM affinity. Flibanserin D4 represents a deuterium-labeled version of Flibanserin. | |||
TMIJ-0057 |
5α-Dihydrotestosterone-d4
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5α-Dihydrotestosterone-d4 是 5α-Dihydrotestosterone 的氘代化合物。5α-Dihydrotestosterone 的 CAS 号为 521-18-6。Dihydrotestosterone(DHT) 是睾酮的强效雄激素代谢物。它是雄激素受体的激动剂。 | |||
TMIJ-0162 |
Dexamethasone-d4
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Dexamethasone-d4 是 Dexamethasone 的氘代化合物。Dexamethasone 的 CAS 号为 50-02-2。Dexamethasone是一种糖皮质激素受体激动剂和一种 IL 受体调节剂。在脂多糖诱导的巨噬细胞炎症反应中,它抑制含有炎性 microRNA-155 的外泌体的产生。 | |||
TMIJ-0173 |
Calcipotriol-d4
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Calcipotriol-d4 是 Calcipotriol 的氘代化合物。Calcipotriol 的 CAS 号为 112965-21-6。Calcipotriol 是一种合成的 VitD3类似物,对维他命D受体具有高亲和力。 | |||
TMIJ-0260 |
Bilastine-d4
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Bilastine-d4 是 Bilastine 的氘代化合物。Bilastine 的 CAS 号为 202189-78-4。Bilastine是新型抗组胺药,对H1组胺受体具有高度选择性,起效快,作用时间长的特性,可用于变应性鼻结膜炎和荨麻疹。 | |||
TMIJ-0193 |
Hydrocortisone-d4
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Hydrocortisone-d4 是 Hydrocortisone 的氘代化合物。Hydrocortisone 的 CAS 号为 50-23-7。Hydrocortisone 是肾上腺皮质分泌的糖皮质激素。 | |||
TMID-0055 |
17β-estradiol-d4
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17β-estradiol-d4 是 17β-estradiol 的氘代化合物。17β-estradiol 的 CAS 号为 50-28-2。Estradiol 是一种类固醇性激素,对于女性生育能力和第二性征的维持至关重要。它通过雌激素受体 β 途径上调 IL-6 表达。 | |||
TMID-0200 |
rac-Clopidogrel-d4 Carboxylic Acid
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rac-Clopidogrel-d4 Carboxylic Acid 是 rac-Clopidogrel Carboxylic Acid 的氘代化合物。rac-Clopidogrel Carboxylic Acid 的 CAS 号为 113665-84-2。Clopidogrel 是一种 P2Y12 受体拮抗剂,可降低血小板聚集,用于抑制冠状动脉疾病、周围血管疾病和脑血管疾病中的血凝块。 | |||
TMIH-0124 |
Brivanib Alaninate-d4
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Brivanib Alaninate-d4 是 Brivanib Alaninate 的氘代化合物。Brivanib Alaninate 的 CAS 号为 649735-63-7。Brivanib alaninate 是一种血管内皮生长因子受体 2 (VEGFR2) 抑制剂的丙氨酸盐,IC50值为 25 nM,具有潜在的抗肿瘤活性。它对 VEGFR1 和 FGFR1 适度抑制,对 VEGFR2 的选择性是对 PDGFRβ 的 240 倍。 | |||
TMIH-0372 |
N-desmethyl Apalutamide-d4
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N-desmethyl Apalutamide-d4 是 N-desmethyl Apalutamide 的氘代化合物。N-desmethyl Apalutamide 的 CAS 号为 1332391-11-3。N-Desmethyl Apalutamide 是一种 Apalutamide 的活性代谢产物,主要由 CYP2C8 和 CYP3A4 介导形成。它是一种低活性的雄激素受体拮抗剂,其作用力是 Apalutamide 活性的三分之一。它是中等至强的CYP3A4和CYP2B6诱导剂,并具有优异的血浆蛋白结合浓度。 | |||
TMIJ-0154 |
Lenvatinib-d4
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Lenvatinib-d4 是 Lenvatinib 的氘代化合物。Lenvatinib 的 CAS 号为 417716-92-8。Lenvatinib 是一种口服具有活性的,多靶点酪氨酸激酶抑制剂,能够抑制血管内皮生长因子受体(VEGFR1-3),成纤维细胞生长因子受体(FGFR1-4),干细胞因子受体(KIT),血小板衍生生长因子受体(PDGFR),转染期间重排(RET),具有效抗癌的作用。 | |||
TMIJ-0119 |
Pitavastatin-d4 Sodium Salt
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Pitavastatin-d4 Sodium Salt 是 Pitavastatin Sodium Salt 的氘代化合物。Pitavastatin Sodium Salt 的 CAS 号为 574705-92-3。 | |||
TMID-0013 |
Tiapride-d3
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Tiapride-d3 是 Tiapride 的氘代化合物。Tiapride 的 CAS 号为 51012-32-9。Tiapride 是一种非典型的抗精神病剂,不会引起强直性昏厥和镇静。Tiapride 是多巴胺 D2受体的选择性拮抗剂,其对 D1;D2;D3;D4 受体的 IC50值分别为 1440、45.8、<100 和 11.7 μM。 | |||
TMIH-0271 |
Hydroxyzine dihydrochloride-d4
(R)-2-(2-(4-((4-chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy-1,1,2,2-d4)ethan-1-ol dihydrochloride |
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Hydroxyzine dihydrochloride-d4 是 Hydroxyzine dihydrochloride 的氘代化合物。Hydroxyzine dihydrochloride 的 CAS 号为 2192-20-3。Hydroxyzine dihydrochloride是一种苯二氮卓抗组胺剂,是可口服的组胺 H1 受体和血清素拮抗剂,可有效治疗慢性荨麻疹、皮炎和组胺介导的瘙痒。它还可以作为止吐剂和镇静剂,有缓解焦虑和紧张的作用。 | |||
TMIJ-0099 |
Minodronic acid-d4
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Minodronic acid-d4 是 Minodronic acid 的氘代化合物。Minodronic acid 的 CAS 号为 180064-38-4。Minodronic acid(YM-529) 是一种 P2X2/3 受体拮抗剂, 具有抗癌活性,可直接或间接的抑制癌细胞增殖,诱导细胞凋亡。Minodronic-acid 对各种类型的癌细胞的转移具有抑制作用。Minodronic-acid 可用于研究骨质疏松。 | |||
TMIJ-0519 |
Fosaprepitant-d4 Dimeglumine
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Fosaprepitant-d4 Dimeglumine 是 Fosaprepitant Dimeglumine 的氘代化合物。Fosaprepitant Dimeglumine 的 CAS 号为 265121-04-8。Fosaprepitant dimeglumine 是 Aprepitant 的前药。它是一种神经激肽 1 受体拮抗剂,可用于预防化疗引起的恶心呕吐。 | |||
TMIH-0609 |
Zafirlukast-d7
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Zafirlukast-d7 是 Zafirlukast 的氘代化合物。Zafirlukast 的 CAS 号为 107753-78-6。Zafirlukast 是一种可口服的白三烯 D4受体拮抗剂,具有平喘、抗炎和抗菌作用。 | |||
T71305 |
Clofibric Acid-d4
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Clofibric acid-d4 is intended for use as an internal standard for the quantification of clofibric acid by GC- or LC-MS. Clofibric acid is a peroxisome proliferator-activated receptor α (PPARα) agonist (EC50 = 50 µM in a transactivation assay) and the active metabolite of clofibrate. It is formed from clofibrate by tissue and serum esterases. Dietary administration of clofibric acid (0.067-0.22%) reduces serum cholesterol, phospholipid, and triglyceride levels in rats. It decreases glutamate oxal... | |||
TMIH-0065 |
Acalabrutinib-d4
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Acalabrutinib-d4 是 Acalabrutinib 的氘代化合物。Acalabrutinib 的 CAS 号为 1420477-60-6。Acalabrutinib 是一种不可逆的、高效的、具有口服活性、选择性的第二代BTK抑制剂。它与 BTK 的 ATP 结合口袋中的 Cys481 共价结合。它在慢性淋巴细胞性白血病 (CLL) 小鼠模型中显示出强大的靶向作用和功效。 | |||
T71402 |
Nicorandil-d4
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Nicorandil-d4 is intended for use as an internal standard for the quantification of nicorandil by GC- or LC-MS. Nicorandil is an activator of sulfonylurea receptor 2B (SUR2B) linked to ATP-sensitive potassium channel Kir6.2 (EC50 = ~10 µM) and a nitric oxide (NO) donor. It is selective for SUR2B/Kir6.2 over the SUR2A/Kir6.2 channel (EC50 = >500 µM). Nicorandil activates soluble guanylate cyclase in a cell-free assay and relaxes partially depolarized isolated bovine coronary artery strips (EC50 =... | |||
T71303 |
Flufenamic Acid-d4
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Flufenamic acid-d4 is intended for use as an internal standard for the quantification of flufenamic acid by GC- or LC-MS. Flufenamic acid is a non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor (IC50s = 3 and 9.3 µM for human COX-1 and COX-2, respectively). Flufenamic acid inhibits TNF-α-induced increases in COX-2 levels and NF-κB activation in HT-29 colon cancer cells in a concentration-dependent manner. It inhibits calcium influx induced by fMLP or A23187 in human polymorphonuclear... |