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

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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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