Candesartan (CV-11974), AT 1 受体拮抗剂

血管紧张素受体拮抗剂
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C408360-1ml
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Compound libraries (12326)

基本描述

别名 坎地沙坦(CV-11974)
英文别名 1H-Benzimidazole-7-carboxylic acid, 2-ethoxy-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-
规格或纯度 Moligand™, 10mM in DMSO
英文名称 Candesartan (CV-11974)
生化机理 坎地沙坦(CV-11974)是一种血管紧张素 II 受体拮抗剂,IC50 值为 0.26 nM。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 拮抗剂
作用机制 AT 1 受体拮抗剂
产品介绍

Candesartan 是angiotensin II(血管紧张素II)受体拮抗剂, IC50为0.26 nM。A selective angiotensin II receptor antagonist.

Information

Candesartan (CV-11974) Candesartan (CV-11974) is an angiotensin II receptor antagonist with IC50 of 0.26 nM.
In vitro

Candesartan binds with high specificity to the angiotensin II AT1 receptors in CHO-AT1 cells with K−1 of 0.001 min−1. Candesartan does not affect cell viability or proliferation but increases the expression of VEGF and interleukin-8 in the cultured medium of KU-19-19 cells. Candesartan (0.1 nM) could reduce the maximal contractile response to angiostensin II by approximately 50%.

In vivo

Candesartan (10 mg/kg) inhibits the growth of engrafted tumors and reduces the microvessel density and VEGF expression in a mouse KU-19-19 xenograft model Candesartan (0.5 mg/kg) decreases blood pressure and inhibits AT1 binding in the subfornical organ (SFO), paraventricular nucleus of the hypothalamus (PVN), nucleus of the solitary tract (NTS) and area postrema (AP) in WKY rats. Candesartan (0.3 mg/kg) pretreatment decreases the infarct area by 31% in adult spontaneously hypertensive rats, reduces the CBF decrease at the peripheral area of ischemia and the cortical volume of severe ischemic lesion.
Cell Data

cell lines:NCI-H2228 cells

Concentrations:10 μM

Incubation Time:48 hours

Powder Purity:≥99%

关联靶点(人)

AGTR1 Tclin 1型血管紧张素II受体(Type-1 angiotensin II receptor) (4 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

分子类型 小分子
Canonical SMILES CCOC1=NC2=C([N]1CC3=CC=C(C=C3)C4=CC=CC=C4C5=N[NH]N=N5)C(=CC=C2)C(O)=O
分子量 440.45

安全和危险性(GHS)

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Concentration(Compounding value)
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