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Submit ReviewCGS 35066 is a potent endothelin-converting enzyme (ECE) inhibitor that displays > 100-fold selectivity over neutral endopeptidase 24.11 (IC50 values are 22 and 2300 nM respectively). Blocks the hypertensive effects induced by big ET-1 in vitro and reduces the magnitude of cerebral vasospasm following subarachnoid hemorrhage (SAH).
分子量 | 349.28 |
公式 | C16H16NO6P |
储存 | Desiccate at RT |
纯度 | ≥99% (HPLC) |
CAS Number | 261619-50-5 |
PubChem ID | 9863167 |
InChI Key | CRUVAUSVWLATAE-ZDUSSCGKSA-N |
Smiles | O=C([C@@H](NCP(O)(O)=O)CC1=CC3=C(C2=CC=CC=C2O3)C=C1)O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
1eq. NaOH | 34.92 | 100 |
以下数据基于产品分子量 349.28。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.86 mL | 14.32 mL | 28.63 mL |
5 mM | 0.57 mL | 2.86 mL | 5.73 mL |
10 mM | 0.29 mL | 1.43 mL | 2.86 mL |
50 mM | 0.06 mL | 0.29 mL | 0.57 mL |
参考文献是支持产品生物活性的出版物。
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 PMID: 10669576
Trapani et al (2000) Pharmacological properties of CGS 35066, a potent and selective endothelin-converting enzyme inhibitor, in conscious rats. J.Cardiovasc.Pharmacol. 36 S40 PMID: 11078331
Kwan et al (2002) Attenuation of SAH-induced cerebral vasospasm by a selective ECE inhibitor. Neuropharmacol.Neurotoxicol. 13 197
If you know of a relevant reference for CGS 35066, please let us know.
关键词: CGS 35066, CGS 35066 supplier, Endothelin-converting, enzyme, ECE, inhibitors, inhibits, Proteases, Proteinases, CGS35066, Other, 2512, Tocris Bioscience
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Piglet Unilateral Ureteral Obstruction model to study kidney injury and role of RAAS pathway.Sample used for NGAL measurement (ELISA) is Urine.Bosentan: dual endothelin receptor antagonistCGS 35066: endothelin-converting enzyme (ECE) inhibitorPyr3:Selective antagonist of the canonical transient receptor potential channel 3 (TRPC3)All compound used intravenously after performing surgery on piglet.
Compound was dissolved in DMSO to make stock and then formulated using 20% captisol in normal saline. However, we can not disclose the dose used to perform study due to confidentiality of data that not yet published.