Roflumilast-d3

Modify Date: 2024-01-10 21:28:47

Roflumilast-d3 structure	Common Name	Roflumilast-d3
	CAS Number	1189992-00-4	Molecular Weight	406.23
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₁₇H₁₁D₃Cl₂F₂N₂O₃	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of Roflumilast-d3

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.

Name	N-(3,5-dichloropyridin-4-yl)-3-[dideuterio-(1-deuteriocyclopropyl)methoxy]-4-(difluoromethoxy)benzamide
Synonym	More Synonyms

Description	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.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE) Signaling Pathways >> Anti-infection >> RSV Research Areas >> Inflammation/Immunology
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].
References	[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [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. [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. [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. [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. [6]. Ding H, et al. Treatment of obesity-associated overactive bladder by the phosphodiesterase type-4 inhibitor roflumilast. Int Urol Nephrol. 2017 Jul 29.

Molecular Formula	C₁₇H₁₁D₃Cl₂F₂N₂O₃
Molecular Weight	406.23
Exact Mass	405.05400
PSA	63.68000
LogP	4.45280

Roflumilast-d3

Roflumilast-d3

Use of Roflumilast-d3

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Roflumilast-d3 Biological Activity

Chemical & Physical Properties

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