吡咯咪唑
|
|
|
- CAS号:
- 442-52-4
- 英文名:
- Clemizole
- 英文别名:
- Histacur;Histakool;Depocural;NSC 46261;Lergopenin;Clemizole USP/EP/BP;Clemizole (free base);1-p-Chlorobenzyl-2-pyrrolidino-methylbenzimidazole;1-(p-Chlorobenzyl)-2-pyrrolidylmethylenebenzimidazole;1-p-Chlorobenzyl-2-[1-pyrrolidinylmethyl] benzimidazole
- 中文名:
- 吡咯咪唑
- 中文别名:
- 吡咯咪唑;吡咯咪唑盐酸盐;1-[(4-氯苯基)甲基]-2-(吡咯烷-1-基甲基)苯并咪唑
- CBNumber:
- CB3875322
- 分子式:
- C19H20ClN3
- 分子量:
- 325.84
- MOL File:
- 442-52-4.mol
|
|
|
吡咯咪唑化学性质
-
熔点:
-
239-241℃
-
|
-
沸点:
-
506.1±40.0 °C(Predicted)
-
|
-
密度:
-
1.25±0.1 g/cm3(Predicted)
-
|
-
储存条件:
-
Store at -20°C
-
|
-
溶解度:
-
insoluble in H2O; ≥16.2 mg/mL in DMSO; ≥95.8 mg/mL in EtOH
-
|
-
形态:
-
solid
-
|
-
酸度系数(pKa):
-
9.08±0.20(Predicted)
-
|
吡咯咪唑性质、用途与生产工艺
吡咯咪唑又叫1-[(4-氯苯基)甲基]-2-(吡咯烷-1-基甲基)苯并咪唑，克立咪唑，具有抗组胺作用，具有中等度的镇静作用及明显的止痒作用。最新研究表明其具有抗丙型肝炎病毒的作用。本品能延长心房肌有效不应期，有治疗房扑的报道。
Clemizole是第一代组胺受体(H1 receptor)拮抗剂，是有效的行为性和电生理癫痫活性的抑制剂。它对丙型肝炎的感染具有潜在疗效，能有效地抑制TRPC5离子通道。
| Target | Value |
H1 receptor
()
|
TRPC5
()
|
Clemizole hydrochloride is found to inhibit HCV RNA replication in cell culture that is mediated by its suppression of NS4B’s RNA binding, with little toxicity for the host cell. The EC
50
of Clemizole on the W55R mutant J6/JFH RNA is ~18 µM (2.25 times the EC
50
of the wild-type RNA). Clemizole is a novel inhibitor of TRPC5 channels. Clemizole efficiently blocks TRPC5 currents and Ca
2+
entry in the low micromolar range (IC
50
=1.0-1.3 µM). Clemizole exhibits a six-fold selectivity for TRPC5 over TRPC4β (IC
50
=6.4 µM), the closest structural relative of TRPC5, and an almost 10-fold selectivity over TRPC3 (IC
50
=9.1 µM) and TRPC6 (IC
50
=11.3 µM). Clemizole hydrochloride as a novel blocker of TRPC5 with a half-maximal inhibitory concentration of 1.1 µM. The concentration-response curves confirmed a concentration-dependent block of TRPC5 by Clemizole and revealed an apparent IC
50
of 1.1±0.04 µM.
Clemizole hydrochloride has an unexpectedly short plasma half-life (measured at 0.15 hours); it is very rapidly biotransformed into a glucuronide (M14) and a dealkylated metabolite (M12) and into a variety of lesser metabolites in C57BL/6J mice.
吡咯咪唑
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | S6410 | 吡咯咪唑
Clemizole | 442-52-4 | 5mg | 794.57元 |
| 2023/03/20 | S6410 | 吡咯咪唑
Clemizole | 442-52-4 | 25mg | 1613.85元 |
442-52-4, 吡咯咪唑 相关搜索:
- API intermediates
- Inhibitors
- 药靶配体
- 合成有机化合物配体
- 原料药
- 小分子抑制剂
- 微生物Microbiology
- 小分子抑制剂，天然产物
- C19H20ClN3
- 吡咯咪唑
- 吡咯咪唑盐酸盐
- 1-[(4-氯苯基)甲基]-2-(吡咯烷-1-基甲基)苯并咪唑
- 442-52-4
- Clemizole,Histamine Receptor,TRP Channel,inhibit,Hepatitis C virus,Transient receptor potential channels,HCV,Inhibitor,HCV Protease
- Clemizole USP/EP/BP
- Clemizole (free base)
- 1-(4-Chlorobenzyl)-2-(pyrrolidin-1-ylmethyl)-1H-benzo[d]imidazole
- 1H-Benzimidazole,1-[(4-chlorophenyl)methyl]-2-(1-pyrrolidinylmethyl)-
- 1-(p-Chlorobenzyl)-2-pyrrolidylmethylenebenzimidazole
- 1-p-Chlorobenzyl-2-[1-pyrrolidinylmethyl] benzimidazole
- NSC 46261
- Lergopenin
- Histakool
- Depocural
- 1-p-Chlorobenzyl-2-pyrrolidino-methylbenzimidazole
- 1-(4-CHLOROBENZYL)-2-(PYRROLIDIN-1-YLMETHYL)-1H-BENZO[D]IMIDAZOLE HYDROCHLORIDE
- 1-[(4-chlorophenyl)methyl]-2-(1-pyrrolidinylmethyl)-1H-benzimidazole
- 1-[(4-chlorophenyl)methyl]-2-(pyrrolidin-1-ylmethyl)benzimidazole
- 1-(4-chlorobenzyl)-2-(pyrrolidin-1-ylmethyl)benzimidazole
- Histacur
- 1-(p-Chlorobenzyl)-2-(1-pyrrolidinylmethyl)-1H-benzimidazole
- 1-(4-Chlorobenzyl)-2-(pyrrolizinomethyl)-1H-benzimidazole
- 1-[(4-chlorophenyl)methyl]-2-(1-pyrrolidinylmethyl)-1H-benzimidazole
(Clemizole)