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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T9623 |
RORγt inverse agonist 13
|
ROR | Metabolism |
RORγt inverse agonist 13 是一种口服有效的RORγt 选择性反向激动剂,IC50为 63.8 nM。 | |||
T12753 |
RORγt Inverse agonist 6
|
ROR | Metabolism |
RORγt Inverse agonist 6 是 RORγt inverse 的激动剂。 RORγt Inverse agonist 6 可用于研究 Th17 驱动的自身免疫性疾病。 | |||
T10694 |
CB1 inverse agonist 1
MRL-650 |
Cannabinoid Receptor | GPCR/G Protein |
CB1 inverse agonist 1 (MRL-650) 是一种具有口服活性和选择性的 CB1 激动剂。 CB1 和 CB2 的 IC50 分别为 7.5 nM 和 4100 nM。 CB1 inverse agonist 1 显示出厌食作用。 | |||
T67943 |
RORγ inverse agonist 1
|
Others | Others |
RORγ inverse agonist 1具有抗炎活性,可用来治疗风湿和银屑病。 | |||
T39720 |
RORγt inverse agonist 23
|
Others | Others |
RORγt inverse agonist 23, an orally available novel retinoic acid receptor-related orphan receptor γt inverse agonist, is a potent and selective RORγt inverse agonist. | |||
T40043 |
RORγt Inverse agonist 10
|
Others | Others |
RORγt Inverse agonist 10 is a highly potent and orally bioavailable compound that acts as an antagonist for the retinoic acid receptor-related orphan nuclear receptor gamma t (RORγt). With an IC50 of 51 nM, it effectively inhibits the activity of RORγt, a prominent transcription factor involved in the regulation of genes associated with the pathogenesis of psoriasis, including IL-17A, IL-22, and IL-23R. | |||
T12754 |
RORγt Inverse agonist 8
|
ROR | Metabolism |
RORγt Inverse agonist 8 is a potent, selective, orally bioavailable RORγt inverse agonist(human RORγt-LBD with an IC50 of 19 nM). | |||
T12752 |
RORγt Inverse agonist 3
|
Others | Others |
RORγt Inverse agonist 3 is a potent, selective and orally active inverse agonist of RORγ(EC50s of 0.22 μM and 0.15 μM for hRORγ and RORγt (human IL-17 cells), respectively). | |||
T12755 |
RORγt Inverse agonist 2
|
Others | Others |
RORγt Inverse agonist 2 is a selective, orally active inverse agonist of RORγt(EC50 of 119 nM). | |||
T11231 |
ERRγ Inverse Agonist 1
|
Estrogen/progestogen Receptor | Endocrinology/Hormones |
ERRγ Inverse Agonist 1 (Compound 12) 是有效的、选择性的、口服生物可利用的雌激素相关受体 γ (ERRγ)的反向激动剂,IC50值为 40 nM。 | |||
T72254 |
RORγt inverse agonist 26
|
Others | Others |
RORγt inverse agonist 26 是一种有效的 RORγt 反向激动剂。RORγt inverse agonist 26 调节 Th17 细胞的分化并抑制 IL-17的产生。RORγt inverse agonist 26 具有研究炎症和自身免疫性疾病的潜力。 | |||
T72252 | RORγt inverse agonist 14 | ROR | Metabolism |
RORγt inverse agonist 14 (8e) 是一种高效、口服活性及选择性 RORγt 反向激动剂(EC50 为 2.5 nM),具有抗炎作用,主要应用于风湿性关节炎和牛皮癣的研究。 | |||
T62564 |
RORγt inverse agonist 30
|
Others | Others |
RORγt inverse agonist 30 (Compound 1) 是一种有效的 RORγt 反向激动剂 (IC50: 46 nM)。靶向核受体 RORγt 能够有效治疗自身免疫性疾病。 | |||
T79470 |
RORγt inverse agonist 31
|
ROR | Metabolism |
RORγt inverse agonist 31 (14g) 为一有效RORγt反向激动剂,具备0.428 μM的IC50值。该化合物能够缓解Imiquimod诱发的小鼠牛皮癣症状。 | |||
T63874 |
RORγt inverse agonist 28
|
Others | Others |
RORγt inverse agonist 28 是有效的 RORγt 反向激动剂。RORγt inverse agonist 28 能够调节 Th17 细胞的分化,并抑制 IL-17 的产生。RORγt inverse agonist 28 对炎症和自身免疫性疾病表现出研究潜力。 | |||
T82263 |
GPR61 Inverse agonist 1
|
Others | Others |
GPR61 Inverse agonist 1 (Compound 1) 作为一种GPR61反向激动剂,显示出11 nM的IC50值。该化合物主要用于代谢和体重疾病的研究,包含肥胖和恶病质。 | |||
T78049 |
Nurr1 inverse agonist-1
|
Others | Others |
Nurr1 inverse agonist-1为Nurr1, 一种具有神经保护功能的转录因子, 的反向激动剂。 | |||
T72395 |
CB1 inverse agonist 2
|
Others | Others |
CB1inverse agonist 2 是一种口服有效的大麻素受体 CB1反向激动剂。CB1inverse agonist 2 在小鼠模型中,能有效抑制 CP55940 导致的体温失温和厌食情况。 | |||
T62956 |
RORγt inverse agonist 29
|
Others | Others |
RORγt inverse agonist 29 是一种有效的、选择性的、口服具有活力的 RORγt 反向激动剂,其 IC50 值为 21 nM。RORγt inverse agonist 29 能够用于皮肤炎症和银屑病等自身免疫性疾病的研究。 | |||
T8439 |
Clobenpropit dihydrobromide
|
Apoptosis; Histamine Receptor | Apoptosis; GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Clobenpropit dihydrobromide 是一种组胺H3R 拮抗剂/反向激动剂。它与 5-HT3 受体和 α2A/α2C 肾上腺素受体结合,对组胺H4受体起部分激动剂的作用,还能促进凋亡。 | |||
T8954 |
ML179
ML-179 |
Others | Others |
ML179 是一种有效的选择性肝受体同源物 1 (LRH1, NR5A2) 反向激动剂,IC50 为 320 nM。 | |||
T12855 |
SB 258719
|
5-HT Receptor | GPCR/G Protein; Neuroscience |
SB 258719 是高亲和力的、选择性的5-HT7受体拮抗剂,pKi 为7.5。SB 258719在癌症和神经系统疾病领域有研究价值。 | |||
T9635 |
Cedirogant
ABBV-157 |
ROR | Metabolism |
Cedirogant (ABBV-157) 是一种口服有活性的 RORγt 反向激动剂,可用于研究银屑病。 | |||
T4050 |
GSK2981278
ROR gama modulator 1 |
ROR | Metabolism |
GSK2981278 (ROR gama modulator 1) 是 RORγ的选择性反向激动剂。它能够抑制 il17启动子的激活,并且干扰 RORγ-DNA 结合。 | |||
T0797 |
Cimetidine
西米替汀,SKF-92334,西咪替丁 |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Cimetidine (SKF-92334) 是一种可口服的可逆组胺H2受体拮抗剂,Ki 为 0.6 μM。它抑制胃酸分泌,以及胃蛋白酶和胃泌素的输出,具有抗癌和抗炎活性。 | |||
T11277 |
FG 7142
ZK 39106,LSU-65 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
FG 7142 (LSU-65) 是一种非选择性苯二氮卓类反向激动剂,对含 α1 亚基的 GABAA 受体具有高亲和力,Ki 为 91 nM。它还调节 GABA 诱导的 GABAA 受体上的氯离子通量,表达 α1 亚基,EC50为 137 nM。它可增加酪氨酸羟基化并导致小鼠大脑皮层中 β-肾上腺素受体的上调。 | |||
T7350 |
Nelotanserin
1-[3-(4-溴-1-甲基-1H-吡唑-5-基)-4-甲氧基苯基]-3-(2,4-二氟苯基)脲,APD125 |
5-HT Receptor | GPCR/G Protein; Neuroscience |
Nelotanserin (APD125) 是5-HT2A 强完全逆向激动剂,5-HT2C 中等强度的部分反向激动剂和5-HT2B 的弱反向激动剂,IC50s 值分别为 1.7、79 和 791 nM。 | |||
T24421 |
LY-2624803
DB-7,LY2624803,HY-10275,LY 2624803 |
5-HT Receptor; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
LY-2624803 是一种 5-HT2A 受体拮抗剂和组胺受体反向激动剂,可用于改善慢波睡眠。 | |||
T4087 |
S 38093 HCl
|
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
S 38093 HCl 是一种新型的脑渗透性 H3 受体拮抗剂/反向激动剂。 | |||
T9226 |
CCG-143140
|
Glucagon Receptor | GPCR/G Protein |
CCG-143140 是一种 GLP-1 受体反向激动剂。 | |||
T8407 |
AF64394
|
GPR | Endocrinology/Hormones; GPCR/G Protein |
AF64394 是一种选择性的 GPR3逆向激动剂(pIC50:7.3)。 | |||
T2674 |
GSK0660
|
PPAR | DNA Damage/DNA Repair; Metabolism |
GSK0660 是 PPARβ/δ 的拮抗剂和反向激动剂,IC50均为155 nM。 | |||
T13172L1 |
TMP-778
|
ROR | Metabolism |
TMP-778是一种RORγt 的选择性逆向激动剂。 | |||
T24524 |
NDT 9513727
NDT9513727,NDT-9513727 |
Complement System | Immunology/Inflammation |
NDT 9513727 是一种强效、选择性和竞争性的 C5aR1反向激动剂,可用于研究炎症和免疫功能异常引发的疾病。 | |||
T1801 |
SR9243
|
Liver X Receptor | Metabolism |
SR9243 是一种 liver-X-receptor 的反向激动剂,可诱导 LXR-辅阻遏物相互作用。 | |||
T5163 |
SR1001
|
ROR | Metabolism |
SR1001 是选择性RORα及RORγt 的反向激动剂,其Ki 分别为 172 和 111 nM。 | |||
T6417 |
BML-190
2-[1-(4-氯苯甲酰基)-5-甲氧基-2-甲基-1H-吲哚-3-基]-1-(4-吗啉基)乙酮,Indomethacin morpholinylamide,吲哚美辛吗啉代酰胺,IMMA,BML 190 |
Cannabinoid Receptor | GPCR/G Protein |
BML-190 (Indomethacin morpholinylamide) 是一种 CB2 受体的配体,其对 CB2 受体 (Ki:435 nM) 和 CB1受体 (Ki> 2 μM)。 | |||
T24381 |
L-822179
L822179,L 822,179,L 822179,L822,179,L-822,179 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
L-822179 (α5IA) 是 GABAA 受体 Α5 亚型的选择性反向激动剂,在 A5 亚型中具有比其他药物更高的内在活性。 | |||
T16929 |
SR2211
|
ROR | Metabolism |
SR2211 是一种特异性调节剂和 RORγ 的反向激动剂(IC50 = 320 nM,Ki = 105 nM)。 | |||
T16508 |
PF-5190457
PF-05190457 |
GHSR | GPCR/G Protein |
PF-5190457 是具有选择性的、有效的生长素释放肽受体选择性的反向激动剂(pKi:8.36)。 | |||
T14369 |
AZD-0284
|
ROR | Metabolism |
AZD-0284 是核受体 (RORγ) 的选择性反向激动剂。它对呼吸道疾病及斑块型寻常型银屑病具有潜在的应用价值。 | |||
T67933 |
BAY-4931
|
PPAR | DNA Damage/DNA Repair; Metabolism |
BAY-4931 是一种有效的、共价的、选择性的 PPARγ反向激动剂,IC50为 0.17 nM。 | |||
T7176 |
Pitolisant hydrochloride
1-[3-[3-(4-氯丙基)丙氧基]丙基]-哌啶盐酸盐,BF 2649,Ciproxidine |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Pitolisant hydrochloride (Ciproxidine) 是一种有效的、选择性的组胺 H3 受体反向激动剂,Ki 为0.16 nM。 | |||
T16844 |
Sarmazenil
R-154513,Ro 15-3505 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Sarmazenil (Ro 15-3505) 是苯二氮卓受体部分反向激动剂,具有促惊厥作用,可用于研究慢性肝性脑病 (HE) 。 | |||
T12192 |
NCGC00229600
|
Others; TSH Receptor | GPCR/G Protein; Others |
NCGC00229600 是促甲状腺激素受体 (TSHR) 的变构反向激动剂。 NCGC00229600 抑制 TSH 和刺激 TSHR 的内源性激活抗体,可用于格雷夫斯病的研究。 | |||
T16930 |
SR9238
|
Liver X Receptor | Metabolism |
SR9238 是有效的肝 X 受体(LXR)反向激动剂,对LXRα和LXRβ的IC50分别为 214 nM 和 43 nM。 | |||
T0593 |
XCT790
|
Estrogen Receptor/ERR; Estrogen/progestogen Receptor; Autophagy | Autophagy; Endocrinology/Hormones |
XCT790 是 ERRα的一种选择性反向激动剂,IC50值为 0.37 μM。它在化疗过程中诱导癌细胞死亡。 | |||
T5829 |
H4 Receptor antagonist 1
|
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
H4 Receptor antagonist 1 是选择性组胺 H4受体反向激动剂,其IC50值为19 nM。 | |||
T6946 |
Pimavanserin tartrate
ACP-103,ACP-103 tartrate,Nuplazid,Pimavanserin,匹莫范色林 |
5-HT Receptor | GPCR/G Protein; Neuroscience |
Pimavanserin tartrate (Nuplazid) 是一种有效的5-HT 2A 受体反向激动剂,pIC50和 pKi 值分别为8.73和9.3,用于治疗与帕金森病相关的精神病。 | |||
T5160 |
SR3335
ML 176 |
ROR | Metabolism |
SR3335 (ML 176) 是特异性RORα反向激动剂,能够与 RORα直接结合,其Ki=220 nM。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2177 |
Kaempferol
Kempferol,山柰酚,山奈酚,Robigenin |
Apoptosis; Estrogen Receptor/ERR; Mitophagy; Estrogen/progestogen Receptor; HIV Protease; Endogenous Metabolite; Parasite; Autophagy | Apoptosis; Autophagy; Endocrinology/Hormones; Metabolism; Microbiology/Virology; Proteases/Proteasome |
Kaempferol (Robigenin) 属于天然类黄酮,是一种 ERRα 和 ERRγ 的反向激动剂。Kaempferol 具有抗肿瘤、抗炎、抗氧化、抗菌和抗病毒等多种活性。 |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPK-01299 |
CEACAM5 Protein, Cynomolgus, Recombinant (aa 35-685, His)
Carcinoembryonic,CEA,CEACD66e,DKFZp781M2392,CEACAM-5,CD66e,M... |
Cynomolgus | HEK293 Cells |
Carcinoembryonic antigen-related cell adhesion molecule 5 (CEACAM5) was identified as a metastatic driver. CEACAM5 overproduction enriched for an epithelial gene expression pattern and facilitated tumor outgrowth at metastatic sites. Tissues from patients with metastatic breast cancer confirmed elevated levels of CEACAM5 in lung metastases relative to breast tumors, and an inverse correlation between CEACAM5 and the mesenchymal marker vimentin was demonstrated. | |||
TMPY-04100 |
MMP-26 Protein, Human, Recombinant
matrix metallopeptidase 26,MMP26 |
Human | E. coli |
MMP26 (Matrix Metallopeptidase 26) is a Protein Coding gene. MMP26 is a member of matrix metalloproteinases (MMPs) and has been reported to be highly expressed in many cancers. The protein differs from most MMP family members in that it lacks a conserved C-terminal protein domain. It may hydrolyze collagen type IV, fibronectin, fibrinogen, beta-casein, type I gelatin, and alpha-1 proteinase inhibitor, and is also able to activate progelatinase B. MMP26 is a target gene of miR-125b, and the expre... | |||
TMPY-00055 |
LCAT Protein, Human, Recombinant (His)
lecithin-cholesterol acyltransferase |
Human | HEK293 Cells |
Lecithin: cholesterol acyltransferase (LCAT) is the sole enzyme that esterifies cholesterol in plasma, thus determining the maturation of high-density lipoproteins. Because it maintains an unesterified cholesterol gradient between peripheral cells and extracellular acceptors, for a long time, LCAT has been considered as a key enzyme in reverse cholesterol transport. Lecithin cholesterol acyltransferase (LCAT) plays a pivotal role in HDL metabolism.LCAT is intimately involved in HDL maturation an... | |||
TMPY-02029 |
CDO Protein, Human, Recombinant (His)
CDON1,HPE11,cell adhesion associated, oncogene regulated,CDO... |
Human | HEK293 Cells |
Cell adhesion molecule-related, down-regulated by oncogenes (CDON), also known as CDO, is an Ig superfamily member, is a component of a cell surface receptor that positively regulates skeletal myogenesis. Brother of CDO (BOC) is a cell surface receptor that derives its name from the structurally related protein, CDON. They are components of a cell surface receptor that positively regulates myogenesis in vitro. Expression of Cdo and Boc in myoblast cell lines is downregulated by the ras oncogene,... | |||
TMPY-02299 |
ALDH3A1 Protein, Human, Recombinant (His)
ALDHIII,aldehyde dehydrogenase 3 family, member A1,ALDH3 |
Human | Baculovirus Insect Cells |
Aldehyde dehydrogenase 3A1 (ALDH3A1) is a metabolic enzyme that catalyzes the oxidation of various aldehydes. Certain types of epithelial tissues in mammals, especially those continually exposed to environmental stress (e.g., corneal epithelium), express ALDH3A1 at high levels and its abundance in such tissues is perceived to help to maintain cellular homeostasis under conditions of oxidative stress. Metabolic as well as non-metabolic roles for ALDH3A1 have been associated with its mediated resi... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TMIJ-0338 |
Pitolisant-d6 HCl
|
||
Pitolisant-d6 HCl 是 Pitolisant HCl 的氘代化合物。Pitolisant HCl 的 CAS 号为 903576-44-3。Pitolisant hydrochloride 是一种有效的、选择性的组胺 H3 受体反向激动剂,Ki为0.16 nM。 | |||
TMIH-0435 |
Pimavanserin-d3
|
||
Pimavanserin-d3 是 Pimavanserin 的氘代化合物。Pimavanserin 的 CAS 号为 706779-91-1。Pimavanserin 是特异性的 5-HT2A 受体反向激动剂,在基于细胞的功能测定中,平均 pIC50值为8.7。它是非典型抗精神病药,用于治疗帕金森病患者的幻觉和精神病。 |