生物活性：Roflumilast-d3 is deuterium labeled Roflumilast. Roflumilast is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells.
体外研究(In Vitro)：Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
试剂家 has not independently confirmed the accuracy of these methods. They are for reference only.
Roflumilast-d3 相关抗体:
Acetyl CoA synthetase Antibody
PDE1B Antibody (YA1553)
PDE4B Antibody (YA2932)
PDE2A Antibody (YA2989)
PDE4D Antibody (YA1714)
分子量：406.23
Formula：C17H11D3Cl2F2N2O3
CAS 号：1189992-00-4
非标记 CAS：162401-32-3
中文名称：罗氟司特-d3
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.
纯度 & 产品资料
Data Sheet (531 KB)
产品使用指南 (1538 KB)
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
 [Content Brief]
[2]. Hatzelmann A, et al. The preclinical pharmacology of roflumilast--a selective, oral phosphodiesterase 4 inhibitor in development for chronic obstructive pulmonary disease. Pulm Pharmacol Ther. 2010 Aug;23(4):235-56.
 [Content Brief]
[3]. Rabe KF. Update on roflumilast, a phosphodiesterase 4 inhibitor for the treatment of chronic obstructive pulmonary disease. Br J Pharmacol. 2011 May;163(1):53-67.
 [Content Brief]
[4]. Hatzelmann A, et al. Anti-inflammatory and immunomodulatory potential of the novel PDE4 inhibitor roflumilast in vitro. J Pharmacol Exp Ther. 2001 Apr;297(1):267-79.
 [Content Brief]
[5]. Richmond BW, et al. Airway bacteria drive a progressive COPD-like phenotype in mice with polymeric immunoglobulin receptor deficiency. Nat Commun. 2016 Apr 5;7:11240.
 [Content Brief]
[6]. Ding H, et al. Treatment of obesity-associated overactive bladder by the phosphodiesterase type-4 inhibitor roflumilast. Int Urol Nephrol. 2017 Jul 29.
 [Content Brief]