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Roflumilast-d4

CAT: 0804-HY-15455SSize: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-15455SSize:1 mg
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Description
Roflumilast-d4 is the 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[1][2].
CAS Number
1398065-69-4
Product Name Alternative
APTA-2217-d4; BYK 20869-d4; B9302-107-d4
UNSPSC
12352005
Hazard Statement
H315, H319, H335
Target
Isotope-Labeled Compounds; Phosphodiesterase (PDE) ; RSV
Type
Isotope-Labeled Compounds
Related Pathways
Anti-infection; Metabolic Enzyme/Protease; Others
Applications
COVID-19-anti-virus
Field of Research
Inflammation/Immunology
Purity
97.26
Solubility
10 mM in DMSO
Smiles
FC(OC1=C(C=C(C=C1)C(NC2=C(C=NC=C2Cl)Cl)=O)OCC3C([2H])(C3([2H])[2H])[2H])F
Molecular Formula
C17H10D4Cl2F2N2O3
Molecular Weight
407.23
Precautions
H315, H319, H335
References & Citations
[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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Isotope-Labeled Compounds
Clinical Information
No Development Reported

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