Clemastine-d5 (fumarate)_product_DataBase

Bioactivity	Clemastine-d5 (fumarate) is the deuterium labeled Clemastine fumarate. Clemastine fumarate (HS-592 fumarate) is a selective histamine H1 receptor antagonist with IC50 of 3 nM.
Invitro	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].
Name	Clemastine-d5 (fumarate)
Formula	C25H25D5ClNO5
Molar Mass	464.99
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]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Seifert, R., et al., Histamine increases cytosolic Ca2+ in dibutyryl-cAMP-differentiated HL-60 cells via H1 receptors and is an incomplete secretagogue. Mol Pharmacol, 1992. 42(2): p. 227-34. [3]. Schran, H.F., et al., The pharmacokinetics and bioavailability of clemastine and phenylpropanolamine in single-component and combination formulations. J Clin Pharmacol, 1996. 36(10): p. 911-22.

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