388
14
21
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T64414 |
PRI-724
C-82 prodrug,Foscenvivint |
Wnt/beta-catenin | Cytoskeletal Signaling; Stem Cells |
PRI-724 (C-82 prodrug)是β-catenin/CBP 相互作用的选择性小分子抑制剂。 | |||
T64076 |
Spermine Prodrug-1
|
Others | Others |
Spermine Prodrug-1 是一种氧化还原敏感的精胺前药。Spermine Prodrug-1 对野生型 (CMS-24949) 和精胺合酶基因 (SMS) 突变型 (CMS-26559, 和 CMS-6233) 成纤维细胞具有抑制作用, 他们的 IC50 值分别为 326.7, 198.5, 和 244.1 μM。Spermine Prodrug-1 能够用于 Snyder Robinson 综合征的治疗。 | |||
T72406 |
Tofacitinib Prodrug-1
|
Others | Others |
Tofacitinib Prodrug-1 是减轻托法替尼 (Tofacitinib) 全身性不良反应的口服有效前药。Tofacitinib Prodrug-1 能在小鼠模型有效减轻恶唑酮诱导的结肠炎,具有低毒性,是治疗溃疡性结肠炎的潜在候选药物。 | |||
T33281 |
Melflufen
Prodrug J-1, Melflufen, Melphalan flufenamide,Melphalan flufenamide,J 1,J1,J-1 |
||
Melphalen fluoroaniline, also known as melphalen, J-1, or prodrug J-1, is a prodrug of melphalen, in which the alkylating agent melphalen is combined with fluoroaniline and has potential antitumor and antiangiogenic activities. | |||
T3934 |
Isavuconazonium sulfate
|
Antifungal | Microbiology/Virology |
Isavuconazonium sulfate 是一种口服活性抗真菌药,是活性三唑类抗真菌药物 Isavuconazole 的前药,可用于侵袭性曲霉菌病和毛霉菌病。 | |||
T0103 |
Dipivefrin hydrochloride
盐酸地匹福林,Dipivefrin HCL |
Adrenergic Receptor; AChR | GPCR/G Protein; Neuroscience |
Dipivefrin hydrochloride (Dipivefrin HCl) 是抗青光眼前体药物,被角膜中的酯酶水解为其活性化合物肾上腺素。 | |||
T15102 |
Dexamethasone palmitate
地塞米松棕榈酸酯,DXP |
Glucocorticoid Receptor | Endocrinology/Hormones |
Dexamethasone palmitate (DXP) (DXP) 是 Dexamethasone 的前药。Dexamethasone 是糖皮质激素受体激动剂。与Dexamethasone 相比, DXP 对糖皮质激素受体的亲和力低 47 倍。DXP 显示出抗炎活性。 | |||
T19438 |
Myristyl nicotinate
Tetradecyl nicotinate,肉豆蔻醇烟酸酯 |
GPR | Endocrinology/Hormones; GPCR/G Protein |
Myristyl nicotinate (Tetradecyl nicotinate) 是 Nicotinic acid 的亲脂衍生物,是一种酯前药。它能够刺激光损伤的皮肤中的表皮分化,增加皮肤 NAD 含量并增强人皮肤屏障。它被开发用于将烟酸输送到皮肤中,以防止光化性角化病及其发展为皮肤癌。 | |||
T0389 |
Dabigatran etexilate
达比加群酯,BIBR 1048 |
Thrombin | Proteases/Proteasome |
Dabigatran etexilate (BIBR 1048) 是一种 Dabigatran 前药,具有口服活性。它具有抗凝作用,能够预防心房颤动引起的静脉血栓栓塞和中风。 | |||
T1579 |
Mestranol
Devocin,Norquen,美雌醇,Menophase |
Estrogen Receptor/ERR; Estrogen/progestogen Receptor | Endocrinology/Hormones |
Mestranol (Devocin) 是一种雌激素受体激动剂,是一种非活性的前药,在转化为炔雌醇时具有生物活性。动物实验中,它可以与黄体酮联合使用,它可用于更年期激素或月经紊乱的研究。 | |||
T13278 |
Valecobulin hydrochloride
CKD-516 hydrochloride |
Microtubule Associated | Cytoskeletal Signaling |
Valecobulin hydrochloride (CKD-516 hydrochloride) 是 S516 的缬氨酸前体药和血管阻断剂。Valecobulin hydrochloride 对β-微管蛋白聚合有强效的抑制作用,对小鼠和人类的实体肿瘤具有显著的抗肿瘤活性。 | |||
T40475 |
Ceftobiprole medocaril
BAL5788,头孢比普酯 |
Antibacterial | Microbiology/Virology |
Ceftobiprole medocaril (BAL5788) 是 Ceftobiprole 的前药。Ceftobiprole 是一种广谱的头孢菌素,对耐甲氧西林金黄色葡萄球菌具有活性。 | |||
TQ0095 |
Brincidofovir
CMX001,HDP-CDV |
Others; Antiviral; HSV | Immunology/Inflammation; Microbiology/Virology; Others |
Brincidofovir (HDP-CDV) 是 Cidofovir 的一种具有口服活性的亲脂性形式的前体药物,是一种口服长效的抗病毒药物,有广泛的抗 DNA 病毒活性。 | |||
T4190 |
Ticlopidine
PCR 5332,Ticlid,噻氯匹定 |
ATPase; Adiponectin receptor | GPCR/G Protein; Membrane transporter/Ion channel |
Ticlopidine (PCR 5332) 是抗血栓前药。它是CYP2C19人肝细胞色素的抑制剂,抑制 CYP2C9 及 CYP3A4。他是变构CD39的非竞争性抑制剂,能够阻断 NTPDase 同工酶,对NTPDase2和NTPDase3的IC50分别为 170 µM 和 149 µM。 | |||
T7840 |
2',3',5'-triacetyl-5-Azacytidine
Nsc291930,三乙酰基-阿扎胞苷 |
DNA Methyltransferase; Others | Chromatin/Epigenetic; Others |
2',3',5'-triacetyl-5-Azacytidine (Nsc291930) 是 5-Azacytidine 的前药,口服有活性。 5-Azacytidine 是 DNA 甲基转移酶的抑制剂。 | |||
T7387 |
Ceftaroline fosamil
TAK-599,头孢罗林酯,PPI0903 |
Antibacterial; Antibiotic | Microbiology/Virology |
Ceftaroline fosamil (TAK-599) 是一种头孢菌素衍生物,是抗甲氧西林金黄色葡萄球菌 (MRSA) T-91825 的 N-膦酰基前药,可研究 MRSA 感染。 | |||
T1675 |
Adefovir dipivoxil
Hepsera,GS 0840,阿德福韦酯,Preveon |
Others; HBV; Reverse Transcriptase | Microbiology/Virology; Others |
Adefovir dipivoxil (GS 0840) 是一种腺苷类似物,是核苷逆转录酶抑制剂 Adefovir 的口服前药,具有抗乙型肝炎病毒、疱疹病毒和人类免疫缺陷病毒的活性。 | |||
T5133 |
Dabigatran Etexilate Mesylate
甲磺酸达比加群酯,BIBR 1048MS,Dabigatran etexilate methanesulfonate |
Thrombin | Proteases/Proteasome |
Dabigatran Etexilate Mesylate (BIBR 1048MS) 是一种口服具有活性的 Dabigatran 前药,具有抗凝作用,能够预防心房颤动引起的静脉血栓栓塞和中风。 | |||
T2305 |
Isavuconazole
艾沙康唑,BAL-4815,RO-0094815 |
P450; Antibiotic; Antifungal | Metabolism; Microbiology/Virology |
Isavuconazole (RO-0094815) 是一种三唑类前药,对酵母、霉菌和二型真菌具有抗真菌活性。它抑制麦角固醇生物合成,导致真菌膜结构和功能的破坏。它是 CYP3A4抑制剂。 | |||
T24047 |
Etilevodopa hydrochloride
Levodopa ethyl ester,Etilevodopa HCl, L-DOPA ethyl ester |
Others; Dopamine Receptor; Drug Metabolite | GPCR/G Protein; Metabolism; Neuroscience; Others |
Etilevodopa hydrochloride (L-DOPA ethyl ester) 是 Levodopa 的前药,在胃肠道中被非特异性酯酶快速水解产生 Levodopa 和乙醇。Levodopa 是多巴胺的前体,有助于中枢神经系统的渗透和传递多巴胺。Etilevodopa HCl 可用于帕金森病 (PD)的相关研究。 | |||
T1142 |
Clindamycin phosphate
Clindamycin 2-phosphate,Clindamycin 2-dihydrogen phosphate,NSC 618653,U-28508,克林霉素磷酸酯 |
ribosome; Antibacterial; Antibiotic; Parasite | Microbiology/Virology |
Clindamycin phosphate (Clindamycin 2-dihydrogen phosphate) 是一种抗生素,抑制微生物的核糖体作用。可研究厌氧菌感染和原虫疾病。 | |||
T5954 |
Methyldopa hydrate
L-甲基多巴,Alpha-Methyldopa Sesquihydrate,L-(-)-α-Methyldopa hydrate,MK-351 hydrate,Methyldopa Sesquihydrate |
Dopamine Receptor; Adrenergic Receptor | GPCR/G Protein; Neuroscience |
Methyldopa hydrate (MK-351 hydrate) 是一种前药,在中枢神经系统中被代谢成 α-Methylepinephrine。它是一种 α-肾上腺素能激动剂,对α2-adrenergic receptors 有选择性。 | |||
T3085 |
Piperacetazine
Psymod,Piperacetazinum,Quide,哌西他嗪 |
Dopamine Receptor; 5-HT Receptor | GPCR/G Protein; Neuroscience |
Piperacetazine (Piperacetazinum) 是抗精神病试剂的前体,可用于研究精神分裂症。 | |||
T17218 |
Varespladib methyl
A-002,LY333013 |
Others; Phospholipase | Metabolism; Others |
Varespladib methyl (LY333013) 是 Varespladib 的生物可利用前药,是一种特异性 II 组分泌型磷脂酶 A2 抑制剂。 | |||
T9472 |
Rebamipide mofetil
|
COX | Immunology/Inflammation; Neuroscience |
Rebamipide mofetil 是 Rebamipide 的口服活性前药,是一种粘膜保护剂。 | |||
T13365 |
YHO-13351 free base
|
BCRP | Membrane transporter/Ion channel |
YHO-13351 free base 是 YHO-13177 的水溶性前药,YHO-13177 是 BCRP 的抑制剂。 | |||
T39476 |
NLG802
|
Indoleamine 2,3-Dioxygenase (IDO) | Metabolism |
NLG802 是 indoximod 的前药,indoximod 是一种口服活性的吲哚胺2,3-双加氧酶(IDO)抑制剂。 | |||
T8238 |
Fosamprenavir Calcium Salt
福沙那伟钙,Diallyl Trisulfide,GW433908G |
HIV Protease | Microbiology/Virology; Proteases/Proteasome |
Fosamprenavir Calcium Salt (GW433908G) 是抗逆转录病毒蛋白酶抑制剂 Amprenavir 的磷酸酯前药,具有改善的溶解性和抗HIV 感染作用。 | |||
T23667 |
AGN-201904
AGN201904,AGN 201904 |
ATPase | Membrane transporter/Ion channel |
AGN-201904 是质子泵抑制剂,是一种奥美拉唑前药,可延缓衰老,可用于预防和治疗消化性溃疡。 | |||
T2419 |
BMS-794833
|
VEGFR; c-Met/HGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
BMS794833 是一种 VEGFR2 和 Met 的抑制剂,它们的 IC50值分别为 15 和 1.7 nM。 | |||
T5186 |
Oseltamivir acid
GS 4071,oseltamivir carboxylate,奥斯他伟酸,Ro 64-0802 |
Influenza Virus; Drug Metabolite | Metabolism; Microbiology/Virology |
Oseltamivir acid (GS 4071) 是Oseltamivir phosphate 的活性代谢产物,是一种有效的流感病毒神经氨酸酶抑制剂和 GS4071 的前药。 | |||
T6998 |
Tedizolid Phosphate
TR-701FA,Torezolid phosphate,磷酸特地唑胺 |
Antibacterial; Antibiotic | Microbiology/Virology |
Tedizolid Phosphate (TR-701FA) 是 MAO-A 和 MAO-B 抑制剂,具有抗革兰氏阳性菌的活性。 | |||
T26686 |
AV-101
L-4-Cl-KYN,L-4-chlorokynurenine,4-Cl-KYN,4ClKYN,4-Chlorokynurenine,(S)-4-Chlorokynurenine |
NMDAR | Neuroscience |
AV-101 (4-Cl-KYN) 是 NMDA 受体甘氨酸位点的前药拮抗剂,具有抗抑郁活性,可减少 MPTP 猴子中左旋多巴诱导的运动障碍。 | |||
T68120 |
Ot-730
QLT 091568 |
Others | Others |
ot-730(QLT 091568) 是一种新型选择性β阻滞剂前药,可用于研究眼部疾病。 | |||
T36526 |
IL-17 modulator 4
|
Interleukin | Immunology/Inflammation |
IL-17 modulator 4 是 IL-17 modulator 1 的前药,IL-17 modulator 1 是 IL-17 的有效调节剂。 | |||
T5328 |
Fosfluconazole
|
Antifungal | Microbiology/Virology |
Fosfluconazole 是 fluconazole 的水溶性磷酸盐前药。 它是一种抗真菌药物。 | |||
T4061 |
LY2334737
|
Nucleoside Antimetabolite/Analog; Others; Virus Protease | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology; Others |
LY2334737 是一种具有口服活性的 Gemcitabine 的前药,也是核苷类似物。它抑制肠道病毒 A71 感染,有抗病毒和抗癌活性。 | |||
T7282 |
Tenofovir alafenamide hemifumarate
GS-7340 (hemifumarate),Tenofovir alafenamide fumarate,替诺福韦艾拉酚胺富马酸盐 |
HIV Protease; Reverse Transcriptase | Microbiology/Virology; Proteases/Proteasome |
Tenofovir alafenamide hemifumarate (GS-7340 hemifumarate) 是 HIV 逆转录酶核苷酸抑制剂替诺福韦的口服膦酰胺前药。 | |||
T7854 |
Bortezomib-pinanediol
|
Proteasome | Proteases/Proteasome; Ubiquitination |
Bortezomib-pinanediol 是一种蛋白酶体抑制剂。是硼替佐米的前药。 | |||
T22304 |
Desciclovir
BW A515U,地昔洛韦,6-Deoxyacyclovir,DCV |
Antifection | Microbiology/Virology |
Desciclovir (DCV) 是抗疱疹药物阿昔洛韦的前药,口服有活性,在体内被黄嘌呤氧化酶转化成为阿昔洛韦。 | |||
T24540 |
NO-711ME
NO711ME,NO711 Methyl ester,N-O711 Methyl ester,N O711 Methyl ester |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
NO-711ME (N-O711 Methyl ester) 是 NO-711 的前药。它也是一种有效的选择性 GABA 摄取抑制剂。 | |||
T7066 |
Fosphenytoin disodium
Fosphenytoin sodium,ACC-9653,磷苯妥英钠 |
Sodium Channel | Membrane transporter/Ion channel |
Fosphenytoin disodium (ACC-9653) 是 phenytoin 的前体药物,具有抗惊厥等活性。它是电压门控钠通道阻滞剂。 | |||
T68171 |
Zabicipril
|
RAAS | Endocrinology/Hormones |
Zabicipril 是一种新型可口服的血管紧张转换酶抑制剂,是一种前药,在体内脱酯后具有抗高血压活性。 | |||
T0907 |
Sulfasalazine
柳氮磺吡啶,NSC 667219,Azulfidine |
Apoptosis; Ferroptosis; NF-κB; COX; Antibacterial; Antibiotic; Autophagy | Apoptosis; Autophagy; Immunology/Inflammation; Microbiology/Virology; Neuroscience; NF-κB |
Sulfasalazine (Azulfidine) 是一种合成的水杨酸衍生物,对含有弹性蛋白的结缔组织具有亲和力,并配制成前药。 | |||
T40276 |
GS-621763
|
SARS-CoV | Microbiology/Virology |
GS-621763 是具有口服活性的 GS-441524 前药,在小鼠体内具有抗SARS-CoV-2病毒活性。 | |||
T12042 |
Minnelide
|
Apoptosis; Virus Protease | Apoptosis; Microbiology/Virology |
Minnelide 是水溶性雷公藤内酯前药,具有抗癌症抗肿瘤活性,可诱导细胞凋亡,可预防足细胞损伤。Minnelide 通过阻断 HPV 诱导的 p53 和 pRb 变化来抑制宫颈癌的生长。 | |||
T1645 |
Ramipril
HOE-498,Tritace,雷米普利,Altace,Carasel |
Apoptosis; RAAS | Apoptosis; Endocrinology/Hormones |
Ramipril (Altace) 是一种ACE 抑制剂,IC50为5 nM。 | |||
T0319 |
Suxibuzone
琥布宗,Calibene,Suxibuzonum,Suxibuzona |
COX | Immunology/Inflammation; Neuroscience |
Suxibuzone (Suxibuzona) 是非甾体类抗炎药 Phenylbutazone 的前药,可用于关节和肌肉疼痛研究。 | |||
T4627 |
SPI--112Me
|
Others | Others |
SPI--112Me 是 SPI-112 的前药,在无细胞试验中,它优先抑制 Shp2 的 PTPase 活性超过 Shp1 和 PTP1B 20 倍。 | |||
T68120L |
Ot-730 HCl
Ot-730 HCl(870809-51-1 Free base) |
Others | Others |
ot-730 HCl 是一种新型选择性β阻滞剂前药,可用于研究眼部疾病。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TC0025 |
Testosterone acetate
NSC523836,NSC-523836,NSC 523836,醋酸睾酮 |
Others | Others |
Testosterone acetate (NSC-523836) 是一种 Testosterone 前药,是一种天然存在的雄激素睾酮酯。它可用于阳痿、虚弱、疲劳和性腺机能减退的研究。 | |||
T0505 |
Methyldopa
L-(-)-α-Methyldopa,MK-351,甲基多巴 |
Dopamine Receptor; Adrenergic Receptor | GPCR/G Protein; Neuroscience |
L-(-)-α-Methyldopa (MK-351) 是一种前药,在中枢神经系统中被代谢成 α-Methylepinephrine。它是 α-肾上腺素能激动剂,对 α2- adrenergic receptors 有选择性。 | |||
T19676 |
Tributyrin
NSC661583,NSC 661583,NSC-661583,甘油三丁酸酯 |
Apoptosis | Apoptosis |
Tributyrin (Glyceryl tributyrate) 是一种中性短链脂肪酸甘油三酯,是一种稳定且吸收迅速的丁酸前药。 它通过生物膜扩散并被细胞内脂肪酶代谢,在体内将有效的丁酸直接释放到细胞中,有抗增殖、促凋亡和诱导分化作用。 | |||
T8160 |
EGCG Octaacetate
乙酰化表没食子儿茶素没食子酸酯,乙酰化EGCG |
Others; Antibacterial | Microbiology/Virology; Others |
EGCG Octaacetate 是表没食子儿茶素没食子酸酯的前药,对革兰氏阳性菌和革兰氏阴性菌有潜在抗菌可能。它可下调 PI3K/Akt/NFκB 磷酸化和 p65 乙酰化来降低促炎介质水平,减少小鼠结肠炎引起的结肠癌。 | |||
T0132 |
Etoposide
VP-16,依托泊苷,依托泊甙,VP-16-213 |
Apoptosis; Mitophagy; Topoisomerase; Antibacterial; Antibiotic; Autophagy | Apoptosis; Autophagy; DNA Damage/DNA Repair; Microbiology/Virology |
Etoposide (VP-16-213) 是一种拓扑异构酶 II 的抑制剂,通过与拓扑异构酶 II 和 DNA 形成复合物来抑制 DNA 合成 (IC50=60.3 μM)。Etoposide 具有抗肿瘤活性,可以诱导细胞凋亡、自噬。 | |||
TN7246 |
3-Sulfopropanoic acid
3-SPA |
Drug Metabolite | Metabolism |
3-Sulfopropanoic acid 是曲吡罗酯及其前药ALZ-801的主要代谢产物,是存在于AD患者的脑脊液(CSF)中的内源性分子,可抑制 Aβ42 寡聚体的形成。 | |||
T3S2007 |
MRE-269
3-氧代-12-烯-28-乌苏酸,MRE 269,ACT-333679,MRE269 |
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
MRE-269 (ACT-333679) 是一种口服的长效前列环素受体激动剂前药,是 Selexipag 的活性代谢物,用于治疗肺动脉高压。 | |||
T1273 |
Diacerein
双醋瑞因,Diacerhein,Fisiodar,Diacetylrhein |
IL Receptor; Interleukin | Immunology/Inflammation |
Diacerein (Fisiodar) 是一种慢效具有白介素-1β 抑制效果的蒽醌类化合物。 | |||
T6272 |
Fosbretabulin Disodium
Combretastatin A4 Phosphate,CA 4DP,CA 4P,福他布林,Combretastatin A4 disodium phosphate,Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium |
Apoptosis; Microtubule Associated | Apoptosis; Cytoskeletal Signaling |
Fosbretabulin Disodium (CA 4P) 是一种微管蛋白去稳定剂,是 Combretastatin A4 前药,可选择性靶向内皮细胞,诱导新生肿瘤新血管消退,减少肿瘤血流量并引起中央肿瘤坏死。 | |||
T1591 |
Ancitabine hydrochloride
NSC 145668 HCl,盐酸环胞苷,Cyclocytidine hydrochloride,Cyclo-CMP hydrochloride,Cyclocytidine HCl,Cyclo-C |
Others; DNA/RNA Synthesis; Autophagy | Autophagy; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Others |
Ancitabine hydrochloride (NSC 145668 HCl) 是一种天然的抗白血病药物。 | |||
T0486L |
Irinotecan Hydrochloride
盐酸伊立替康,伊立替康盐酸盐,Camptothecin 11 hydrochloride,CPT-11 hydrochloride |
Topoisomerase; Autophagy | Autophagy; DNA Damage/DNA Repair |
Irinotecan Hydrochloride (CPT-11 hydrochloride) 是喜树碱半合成衍生物的盐酸盐,是一种拓扑异构酶 I 抑制剂,可研究结肠癌和直肠癌。 | |||
T0848 |
L-DOPA
左旋多巴,Levodopa,3,4-Dihydroxyphenylalanine |
Dopamine Receptor; Endogenous Metabolite | GPCR/G Protein; Metabolism; Neuroscience |
L-DOPA (Levodopa) 是的神经递质多巴胺的代谢前体,具有口服活性。Levodopa 能够透过血脑屏障,并在大脑中转化为多巴胺。Levodopa 具有抗痛觉过敏作用。Levodopa 还具有帕金森氏病的研究潜力。 | |||
T20976 |
Clostebol acetate
Clostebolacetate,Clostene,Alfa-Trofodermin,4-CLTA |
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Clostebol acetate is a synthetic anabolic-androgenic steroid (AAS) and a derivative of testosterone. It acts as a prodrug of clostebol in the body. | |||
T15255 |
Etilevodopa
Levodopa ethyl ester,L-DOPA ethyl ester |
Others | Others |
Etilevodopa is an ethyl-ester prodrug of Levodopa which is used for the treatment of Parkinson's disease (PD). It is rapidly hydrolyzed to Levodopa and ethanol by nonspecific esterases in the gastrointestinal tract. Levodopa is the direct precursor of dop |
Cat. No. | Product Name | Target | Signaling Pathways |
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T40915 |
L-Aspartic acid 13C
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L-Aspartic acid 13C is a 13C labeled L-Aspartic acid. L-Aspartic acid is is an amino acid, shown to be a suitable prodrug for colon-specific drug deliverly. | |||
T11679 |
Isavuconazole-d4
BAL-4815 D4,RO-0094815 D4,Isavuconazole D4 |
Others | Others |
Isavuconazole D4 is a deuterium labeled Isavuconazole. Isavuconazole is a triazole prodrug with antifungal activity against yeasts, molds, and dimorphic fungi. | |||
TMIJ-0097 |
Sulfasalazine-d4
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Sulfasalazine-d4 是 Sulfasalazine 的氘代化合物。Sulfasalazine 的 CAS 号为 599-79-1。Sulfasalazine 是一种合成的水杨酸衍生物,对含有弹性蛋白的结缔组织具有亲和力,并配制成前药。 | |||
TMID-0295 |
Fosphenytoin Sodium-d10
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Fosphenytoin Sodium-d10 是 Fosphenytoin Sodium 的氘代化合物。Fosphenytoin Sodium 的 CAS 号为 92134-98-0。Fosphenytoin sodium 是 phenytoin 的前体药物,具有抗惊厥等活性。它是电压门控钠通道阻滞剂。 | |||
TMIJ-0071 |
Oseltamivir-13C-d3 Acid
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Oseltamivir-13C-d3 Acid 是 Oseltamivir Acid 的 13C 和氘代化合物。Oseltamivir Acid 的 CAS 号为 187227-45-8。Oseltamivir acid是Oseltamivir phosphate 的活性代谢产物,是一种有效的流感病毒神经氨酸酶抑制剂和 GS4071 的前药。 | |||
TMIH-0354 |
Molnupiravir-d7
EIDD-2801-d7 |
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Molnupiravir-d7 是 Molnupiravir 的氘代化合物。Molnupiravir 的 CAS 号为 2349386-89-4。EIDD-2801 是核糖核苷类似物 N 4-羟基胞苷 (EIDD-1931) 的异丙酯前药,已显示出广泛的流感病毒和多种冠状病毒活性。 | |||
T71205 |
Fosinopril-d7 sodium salt
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Fosinopril-d7 is intended for use as an internal standard for the quantification of fosinopril by GC- or LC-MS. Fosinopril is a prodrug form of the angiotensin-converting enzyme inhibitor fosinoprilat. Oral administration of fosinopril inhibits angiotensin I-induced pressor responses in normotensive rats, dogs, and monkeys when administered at doses of 15, 15, and 10 µmol/kg, respectively. Fosinopril reduces fractional shortening and decreases left ventricular size in a porcine model of congesti... | |||
T71065 |
Quinapril-d5
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Quinapril-d5 is intended for use as an internal standard for the quantification of quinapril by GC- or LC-MS. Quinapril is a prodrug form of the angiotensin converting enzyme (ACE) inhibitor quinaprilat. In vivo, quinapril reduces mean arterial pressure in renal hypertensive and spontaneously hypertensive rats. It inhibits angiotensin I-induced pressor responses in normotensive rats and dogs. Quinapril prevents left ventricular heart failure in CHF 14.6 cardiomyopathic hamsters. Formulations con... | |||
TMIH-0187 |
Dexlansoprazole-d4
(R)-Lansoprazole-d4 |
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Dexlansoprazole-d4 是 Dexlansoprazole 的氘代化合物。Dexlansoprazole 的 CAS 号为 138530-94-6。(R)-Lansoprazole 是Lansoprazole 的R型异构体。Lansoprazole 是口服有效的质子泵抑制剂,能抑制胃酸生成。Lansoprazole 是中性鞘磷脂酶(N-SMase)的抑制剂(外泌体抑制剂),能透过血脑屏障。 | |||
T69758 |
Flutamide-d7
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Flutamide-d7 is intended for use as an internal standard for the quantification of flutamide by GC- or LC-MS. Flutamide is an androgen receptor antagonist and prodrug form of 2-hydroxy flutamide. Flutamide is converted to 2-hydroxy flutamide by the cytochrome P450 (CYP) isoform CYP1A2 in human liver microsomes. It is cytotoxic to PC3 and LNCaP prostate cancer cells with IC50 values of 98.8 and 81.8 µM, respectively. Flutamide (50 mg/kg per day) reduces tumor growth in a PC-82 mouse xenograft mo... | |||
T71145 |
Racecadotril-d5
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Racecadotril-d5 is intended for use as an internal standard for the quantification of racecadotril by GC- or LC-MS. Racecadotril is a prodrug form of the neprilysin (NEP) inhibitor thiorphan. In vivo, racecadotril reduces or prevents castor oil-induced diarrhea without delaying intestinal transit in rats when administered at doses of 80 or 100 mg/kg, respectively. It also decreases the duration of diarrhea and increases body weight gain in a neonatal gnotobiotic pig model of human rotavirus-indu... | |||
T70883 |
Moexipril-d5
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Moexipril-d5 intended for use as an internal standard for the quantification of moexipril by GC- or LC-MS. Moexipril is a prodrug form of the angiotensin converting enzyme (ACE) inhibitor moexiprilat. It is converted to moexiprilat in vivo by side chain ester hydrolysis. Moexipril inhibits ACE in a cell-free assay (IC50 = 2.7 µM for the rabbit enzyme). It also inhibits phosphodiesterase 4 (IC50s = 38, 160, and 230 µM for PDE4B2, PDE4A5 and PDE4D5, respectively). Moexipril (0.1-30 mg/kg per day) ... | |||
TMIH-0519 |
Selexipag Active Metabolite-d7
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Selexipag Active Metabolite-d7 是 Selexipag Active Metabolite 的氘代化合物。Selexipag Active Metabolite 的 CAS 号为 475085-57-5。MRE269 是一种口服的长效前列环素受体激动剂前药,是 Selexipag 的活性代谢物,用于治疗肺动脉高压。 | |||
T36408 |
Rhein-13C4
Rhein-13C4 |
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Rhein-13C4 is intended for use as an internal standard for the quantification of rhein by GC- or LC-MS. Rhein is an anti-inflammatory anthraquinone found in rhubarb and is the bioactive derivative of its prodrug diacerein . At 10 μM, rhein inhibits IL-1β signaling, suppressing signaling through NF-κB, and reduces the expression of the matrix metalloproteases MMP-1 and MMP-13.1 It inhibits IKKβ (IC50 = 11.8 μM), decreasing iNOS and IL-6 expression in LPS-stimulated macrophages but paradoxically i... | |||
TMID-0290 |
Cefpodoxime proxetil-d3
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Cefpodoxime proxetil-d3 是 Cefpodoxime proxetil 的氘代化合物。Cefpodoxime proxetil 的 CAS 号为 87239-81-4。Cefpodoxime Proxetil 是一种口服的广谱型抗生素。它与青霉素结合蛋白结合,抑制肽聚糖的合成,干扰细菌细胞壁的生物合成。 | |||
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。 | |||
TMIJ-0139 |
Ticagrelor-d7
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Ticagrelor-d7 是 Ticagrelor 的氘代化合物。Ticagrelor 的 CAS 号为 274693-27-5。Ticagrelor (AZD6140) 是可逆的,可口服的P2Y12受体拮抗剂,可抑制血小板聚集。 | |||
TMIJ-0274 |
Sulindac-d3
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Sulindac-d3 是 Sulindac 的氘代化合物。Sulindac 的 CAS 号为 38194-50-2。Sulindac 是一种非甾体类抗炎剂,可抑制COX-2的活性,也可抑制 COX-2 的过表达。它是一种亚磺酰基茚衍生物前药,具有潜在的抗肿瘤活性。 | |||
TMID-0242 |
Capecitabine-d11
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Capecitabine-d11 是 Capecitabine 的氘代化合物。Capecitabine 的 CAS 号为 154361-50-9。Capecitabine 是一种可口服的前药,可由胸苷磷酸化酶催化转变为其活性代谢物 Fluorouracil。 | |||
TMID-0078 |
Irinotecan-d10 Hydrochloride
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Irinotecan-d10 Hydrochloride 是 Irinotecan Hydrochloride 的氘代化合物。Irinotecan Hydrochloride 的 CAS 号为 100286-90-6。Irinotecan Hydrochloride 是喜树碱半合成衍生物的盐酸盐,是一种拓扑异构酶 I 抑制剂,可研究结肠癌和直肠癌。 | |||
TMIJ-0312 |
L-Dopa-2,5,6-d3
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L-Dopa-2,5,6-d3 是 L-Dopa 的氘代化合物。L-Dopa 的 CAS 号为 59-92-7。Levodopa 是的神经递质多巴胺的代谢前体,具有口服活性。Levodopa 能够透过血脑屏障,并在大脑中转化为多巴胺。Levodopa具有抗痛觉过敏作用。Levodopa还具有帕金森氏病的研究潜力。 |