| Bioactivity | Tezacaftor-d4 (VX-661-d4) is the deuterium-labeled Tezacaftor (HY-15448), a F508del CFTR corrector. Tezacaftor helps CFTR protein reach the cell surface[1][2]. | |||||||||
| Invitro | 氢、碳和其他元素的稳定重同位素已被掺入药物分子中，主要用作药物开发过程中定量的示踪剂。氘代因其可能影响药物的药代动力学和代谢特征而受到关注[1]。然而，Ivacaftor (VX-770，HY-13017) 这种 CFTR 增效剂，有助于延长细胞表面 CFTR 蛋白通道的开放时间。Tezacaftor 与 Ivacaftor 结合，显示出对囊性纤维化和 CFTR Phe508del 突变纯合子疾病的有力效果。此外，Elexacaftor (VX-445，HY-111772) 也是一种 CFTR 校正器。 Elexacaftor-Tezacaftor-Ivacaftor 针对至少有一个 Phe508del 突变的囊性纤维化（CF），通常可避免肺移植适应症[3][4]。 | |||||||||
| Name | Tezacaftor-d4 | |||||||||
| CAS | 1961280-24-9 | |||||||||
| Formula | C26H23D4F3N2O6 | |||||||||
| Molar Mass | 524.52 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
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| Reference | [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Treatment with VX-661 and Ivacaftor in a Phase 2 Study Resulted in Statistically Significant Improvements in Lung Function in People with Cystic Fibrosis Who Have Two Copies of the F508del Mutation. April 18, 2013 [3]. Taylor-Cousar JL, et al. Tezacaftor-Ivacaftor in Patients with Cystic Fibrosis Homozygous for Phe508del. N Engl J Med. 2017 Nov 23;377(21):2013-2023. [4]. Burgel PR, et al. Rapid Improvement after Starting Elexacaftor-Tezacaftor-Ivacaftor in Patients with Cystic Fibrosis and Advanced Pulmonary Disease. Am J Respir Crit Care Med. 2021 Jul 1;204(1):64-73. |
Tezacaftor-d4
CAS: 1961280-24-9 F: C26H23D4F3N2O6 W: 524.52
Tezacaftor-d4 (VX-661-d4) is the deuterium-labeled Tezacaftor (HY-15448), a F508del CFTR corrector. Tezacaftor helps CFT
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