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Ivacaftor hydrate (Synonyms: VX-770 hydrate;VX 770 hydrate;VX770 hydrate;Kalydeco hydrate)

Catalog No.GC13316

A CFTR potentiator

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Ivacaftor hydrate Chemical Structure

Cas No.: 1134822-07-3

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100mg
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25mg
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5mg
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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
Synonyms VX-770 hydrate;VX 770 hydrate;VX770 hydrate;Kalydeco hydrate
Chemical Name (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
Formula C24H30N2O4 M.Wt 410.51
Solubility Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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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Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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