钙通道调节剂-1

• 常用名: 钙通道调节剂-1
• 英文名: Calcium channel-modulator-1
• CAS号: 136941-70-3
• 分子量: 579.45
• 密度: N/A
• 沸点: N/A
• 分子式: N/A
• 熔点: N/A
• 闪点: N/A

钙通道调节剂-1用途

Calcium channel-modulator-1是钙离子通道 (calcium channel) 调节剂，阻塞主动脉收缩的 IC₅₀ 值为0.8 μM。

钙通道调节剂-1名称

• 中文名: 钙通道调节剂-1
• 英文名: Calcium channel-modulator-1

钙通道调节剂-1生物活性

• 描述: Calcium channel-modulator-1是钙离子通道 (calcium channel) 调节剂,阻塞主动脉收缩的 IC50 值为0.8 μM。
• 相关类别:
  信号通路 >> 跨膜转运 >> 钙通道
  研究领域 >> 心血管疾病
• 靶点实验:

  IC50: 0.8 μM (Aortic contraction)[1]

• 体内研究: 口服钙通道调节剂-1(20mg/kg)导致自发性高血压大鼠收缩压降低35-37％。然而,静脉注射钙通道调节剂-1以麻醉自发性高血压大鼠会导致血压降低,这比硝苯地平更明显和持久[1]。
• 参考文献:

  [1]. Sunkel CE, et al. Synthesis of 3-[(2,3-dihydro-1,1,3-trioxo-1,2-benzisothiazol-2-yl)alkyl] 1,4-dihydropyridine-3,5-dicarboxylate derivatives as calcium channel modulators. J Med Chem. 1992 Jun 26;35(13):2407-14.

钙通道调节剂-1物理化学性质

• 分子量: 579.45
• InChIKey: LNYDIZPHIUSZBB-UHFFFAOYSA-N
• SMILES: COC(=O)C1=C(C)NC(C)=C(C(=O)OCCCN2C(=O)c3ccccc3S2(=O)=O)C1c1cccc(Cl)c1Cl

钙通道调节剂-1靶点实验

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实验名称：Reducing systolic blood pressure in spontaneously hypertensive rats. 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL778476

实验名称：Compound evaluated for reducing diastolic blood pressure in spontaneously hypertensiv... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL778474

实验名称：Recovery of the initial contraction of rabbit aortic strips, blocked at 10e-4 M conce... 来源：ChEMBL 靶标：Oryctolagus cuniculus External Id：CHEMBL772768

实验名称：Relative potency evaluated (relative potency = IC50 of compound / IC50 of nifedipine)... 来源：ChEMBL 靶标：Oryctolagus cuniculus External Id：CHEMBL772769

实验名称：Blockade of calcium-evoked contractions evaluated in depolarized rabbit aortic strips 来源：ChEMBL 靶标：Oryctolagus cuniculus External Id：CHEMBL771385

实验名称：Duration of action in spontaneously hypertensive rats. 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL779105

实验名称：Systolic blood pressure after administration of a single oral dose (20 mg/kg) in spon... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL792939

实验名称：Selectivity index was measured as the IC50 needed to depress the heart beat divided b... 来源：ChEMBL 靶标：Voltage-dependent L-type calcium channel subunit alpha-1C External Id：CHEMBL772772

实验名称：Rate of reversal by Bay K 8644 of the blockade of K+ - stimulated rabbit aortic strip... 来源：ChEMBL 靶标：Voltage-dependent L-type calcium channel subunit alpha-1C External Id：CHEMBL770456

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