241499-17-2
- CAS号:241499-17-2
- 英文名:N-type calcium channel blocker-1
- 中文名:241499-17-2
- CBNumber:CB44797087
- 分子式:C31H47N3
- 分子量:461.73
- MOL File:241499-17-2.mol
- 沸点 :569.9±50.0 °C(Predicted)
- 密度 :1.013±0.06 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 溶解度 :Soluble in DMSO
- 酸度系数(pKa) :8.89±0.10(Predicted)
241499-17-2性质、用途与生产工艺
- 生物活性 N-type calcium channel blocker-1是有口服活性的麻醉剂,可阻断N型钙离子通道 (N-type calcium channels),在IMR32试验中 IC50 值为0.7 μM。
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靶点
IC50: 0.7 μM (N-type calcium channels)
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体外研究
N-type calcium channel blocker-1 shows good activities in the IMR32 assay (IC 50 =0.7 μM). N-type calcium channel blocker-1 is the most orally active N-type calcium channel blocker for analgesia found in a series of compounds.
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体内研究
N-type calcium channel blocker-1 shows good activities in the acetic acid anti-writhing model (ED 50 =4 mg/kg, iv). N-type calcium channel blocker-1 exhibits oral activity (ED 50 =12 mg/kg, po). A time course study of N-type calcium channel blocker-1 in the anti-writhing model indicates that the CF-1 mice have maximal effect at 120 min after oral dosing at 60 mg/kg. Further evaluation of N-type calcium channel blocker-1 demonstrates several important and advantageous features: the pharmacokinetic profile of N-type calcium channel blocker-1 is improved (Versus of 5.9 L/kg and CL of 26 mL/min/kg) and the logPn of 26 is favorable for CNS agent (logPn measured to be 3.20).
- 公司名称:TargetMol Chemicals Inc.
- 联系电话:+1-781-999-5354 +1-00000000000
- 电子邮件:marketing@targetmol.com
- 国家:美国
- 产品数:19892
- 优势度:58
- 公司名称:MedChemExpress
- 联系电话:--
- 电子邮件:sales@medchemexpress.com
- 国家:美国
- 产品数:6398
- 优势度:58