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Ivacaftor hydrate Sale

(Synonyms: VX-770 hydrate;VX 770 hydrate;VX770 hydrate;Kalydeco hydrate) 目录号 : GC13316

A CFTR potentiator

Ivacaftor hydrate Chemical Structure

Cas No.:1134822-07-3

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5mg
¥450.00
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25mg 待询 待询
100mg
¥1,215.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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产品描述

Description: IC50 Value: 25 nM (F508del-CFTR);100 nM (G551D-CFTR) [1] Ivacaftor (VX-770) is a CFTR Potentiator approved for patients with the G551D mutation of cystic fibrosis, which accounts for 4-5% cases of cystic fibrosis. in vitro: In recombinant cells VX-770 increased CFTR channel open probability (P(o)) in both the F508del processing mutation and the G551D gating mutation. VX-770 also increased Cl(-) secretion in cultured human CF bronchial epithelia (HBE) carrying the G551D gating mutation on one allele and the F508del processing mutation on the other allele by approximately 10-fold, to approximately 50% of that observed in HBE isolated from individuals without CF [1]. in vivo: At day 28, in the group of subjects who received 150 mg of VX-770, the median change in the nasal potential difference (in response to the administration of a chloride-free isoproterenol solution) from baseline was -3.5 mV (range, -8.3 to 0.5; P=0.02 for the within-subject comparison, P=0.13 vs. placebo), and the median change in the level of sweat chloride was -59.5 mmol per liter (range, -66.0 to -19.0; P=0.008 within-subject, P=0.02 vs. placebo) [2]. Toxicity: Six severe adverse events occurred in two subjects (diffuse macular rash in one subject and five incidents of elevated blood and urine glucose levels in one subject with diabetes). All severe adverse events resolved without the discontinuation of VX-770 [2]. Clinical trial: Roll-Over Study of Ivacaftor in Cystic Fibrosis Pediatric Subjects With a CFTR Gating Mutation. Phase 3

Chemical Properties

Cas No. 1134822-07-3 SDF
别名 VX-770 hydrate;VX 770 hydrate;VX770 hydrate;Kalydeco hydrate
化学名 (Z)-N-(2,4-di-tert-butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carbimidic acid hydrate
Canonical SMILES CC(C)(C1=CC(C(C)(C)C)=C(O)C=C1/N=C(O)/C2=CNC3=CC=CC=C3C2=O)C.O
分子式 C24H30N2O4 分子量 410.51
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.436 mL 12.18 mL 24.3599 mL
5 mM 0.4872 mL 2.436 mL 4.872 mL
10 mM 0.2436 mL 1.218 mL 2.436 mL
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