1398065-69-4
Chemical Structure
Roflumilast-d4
Synonym(s): APTA-2217-d4;BYK 20869-d4;B9302-107-d4
- CAS No.: 1398065-69-4
- Formula:C17H10D4Cl2F2N2O3
- Molecular Weight:407.23
IUPAC Name: 3-((cyclopropyl-2,2,3,3-d4)methoxy)-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)benzamide
InChIKey: MNDBXUUTURYVHR-LNLMKGTHSA-N
SMILES: FC(OC1=C(C=C(C=C1)C(NC2=C(C=NC=C2Cl)Cl)=O)OCC3C([2H])(C3([2H])[2H])[2H])F
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Roflumilast-d4 | 97.26% | 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. | ||||||||||||||||||||
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Roflumilast (Standard) | ≥98% | Roflumilast (Standard) is the analytical standard of Roflumilast. This product is intended for research and analytical applications. Roflumilast (APTA-2217) 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. | ||||||||||||||||||||
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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. | |||||||||||||||||||||
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Roflumilast | 99.98% | Roflumilast (APTA-2217) is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDE4A4, PDE4B1, and PDE4B2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells. | ||||||||||||||||||||
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- [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]
