Ivacaftor-d9(Synonyms: VX-770-d9)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Ivacaftor-d9 (Synonyms: VX-770-d9)

Ivacaftor-D9 (CTP-656) 是一种有效的 CFTR 调节剂,在 G551D/F508del HBE 细胞中 CFTR 增强的 EC50 值为 255 nM。Ivacaftor- d9 作为一种具有口服活性和改良的 Ivacaftor 氘化物用于囊性纤维化研究。

Ivacaftor-d9(Synonyms: VX-770-d9)

Ivacaftor-d9 Chemical Structure

CAS No. : 1413431-07-8

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生物活性

Ivacaftor-D9 (CTP-656) is a potent CFTR modulator and exhibits an EC50 value of 255 nM for CFTR potentiation in G551D/F508del HBE Cells. Ivacaftor-D9 acts as an orally active and improved deuterated Ivacaftor analog for cystic fibrosis research[1].

体内研究
(In Vivo)

In PK study, CTP-656 (oral gavage; 10 mg/kg; single dose) shows a superior pharmacokinetic profile, The plasma levels of compound were measured over 72 hours,exhibits the parameters Cmax, AUC0-24 hr, C24hr and t1/2 of 1970 ng/ml (15%), 24,260 hr*ng/ml(17%), 413 ng/ml (19%) and 13.9 hours, respectively in Male Sprague-Dawley rats.
CTP-656 (oral gavage; 3 mg/kg; single dose) exhibits the parameters Cmax, AUC0-24 hr, C24hr and t1/2 of 3643 ng/ml (9%), 49,782 hr*ng/ml(31%), 1418 ng/ml (31%) and 22.8 hours, respectively in Male Beagle Dogs (3.0 mg/kg).

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

401.55

Formula

C24H19D9N2O3

CAS 号

1413431-07-8

中文名称

依伐卡托 D9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Scott L Harbeson, et al. Altering Metabolic Profiles of Drugs by Precision Deuteration 2: Discovery of a Deuterated Analog of Ivacaftor with Differentiated Pharmacokinetics for Clinical Development. J Pharmacol Exp Ther. 2017 Aug;362(2):359-367.

    [2]. Scott L Harbeson, et al. Altering Metabolic Profiles of Drugs by Precision Deuteration 2: Discovery of a Deuterated Analog of Ivacaftor with Differentiated Pharmacokinetics for Clinical Development. J Pharmacol Exp Ther. 2017 Aug;362(2):359-367.

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