CGS 35066 (CAS 261619-50-5)
备用名:
α-[(S)-(Phosphonomethyl)amino]-3-dibenzofuranpropanoic acid
应用；
CGS 35066 is a potent endothelin-converting enzyme (ECE) inhibitor
CAS号码:
261619-50-5
纯度:
>98%
分子量:
349.28
分子式:
C16H16NO6P
仅供科研使用。不可用于诊断或治疗。
CGS 35066 is a a potent endothelin-converting enzyme (ECE) inhibitor. When compared to neutral endopeptidase 24.11, it displays > 100-fold selectivity (IC50 values are 22 and 2300 nM respectively). Another interesting property of CGS 35066 is that it blocks the hypertensive effects induced by big ET-1 n vitro and is able to reduce the magnitude of cerebral vasospasm following subarachnoid hemorrhage (SAH).
参考文献
De Lombaert et al (2000) Potent and selective non-peptidic inhibitors of endothelin-converting enzyme-1 with sustained duration of action. J.Med.Chem. 43 488. Trapani et al (2000) Pharmacological properties of CGS 35066, a potent and selective endothelin-
物理状态
:
Solid
溶解度
:
Soluble in 1eq. NaOH (100 mM).
保存
:
Desiccate at room temperature
熔点
:
304.03° C (Predicted)
沸点
:
~638.89° C at 760 mmHg (Predicted)
密度
:
~1.5 g/cm3 (Predicted)
折射率
:
n20D 1.70 (Predicted)
IC50
:
neutral endopeptidase 24: IC50 = 22 nM; neutral endopeptidase 11: IC50 = 3300 nM; Endothelin-converting enzyme 1: IC50 = 22 nM (human); Neprilysin: IC50 = 2300 nM (human); Neprilysin: IC50 = 2300 nM (Rattus norvegicus)
pK值
:
pKa: 0.79, pKb: 10.58
仅供科研使用。不可用于诊断或治疗。
PubChem CID
:
MDL 号码
:
MFCD09971085
SMILES
:
C1=CC=C2C(=C1)C3=C(O2)C=C(C=C3)C[[email protected]@H](C(=O)O)NCP(=O)(O)O
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