| Bioactivity | Ivacaftor-d9 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]. |
| 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). |
| Name | Ivacaftor-d9 |
| CAS | 1413431-07-8 |
| Formula | C24H19D9N2O3 |
| Molar Mass | 401.55 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |
Ivacaftor-d9
CAS: 1413431-07-8 F: C24H19D9N2O3 W: 401.55
Ivacaftor-d9 is a potent CFTR modulator and exhibits an EC50 value of 255 nM for CFTR potentiation in G551D/F508del HBE
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