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Roflumilast (B9302-107) - 10mM in DMSO, high purity , CAS No.162401-32-3(DMSO), Phosphodiesterase 4 inhibitor

COA

Grade & Purity:

Moligand™

10mM in DMSO

Cas Number: 162401-32-3(DMSO)
Molecular Weight: 403.21

In stock

Item Number

R408998

Grouped product items
SKU	Size	Availability	Price	Qty
R408998-1ml	1ml	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$146.90

PDE4 Selective Inhibitors

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Compound libraries (12325)

Basic Description

Synonyms	APTA 2217, BY 217, BYK 20869 \| 3-(cyclopropylmethoxy)-N-(3,5-dichloro-4-pyridinyl)-4-(difluoromethoxy)-benzamide
Specifications & Purity	Moligand™, 10mM in DMSO
Biochemical and Physiological Mechanisms	Roflumilast (APTA 2217, B9302-107, BY 217, BYK 20869) is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM in a cell-free assay.
Storage Temp	Store at -80°C
Shipped In	Ice chest + Ice pads This product requires cold chain shipping. Ground and other economy services are not available.
Grade	Moligand™
Action Type	INHIBITOR
Mechanism of action	Phosphodiesterase 4 inhibitor
Product Description	Information Roflumilast (APTA 2217, B9302-107, BY 217, BYK 20869) is a selective inhibitor ofPDE4withIC50of 0.2-4.3 nM in a cell-free assay. In vitro Roflumilast displays anti-inflammatory and immunomodulatory in vitro. Roflumilast inhibits LTB4 synthesis in human neutrophil with IC50 of 2 nM. Roflumilast inhibits fMLP-stimulated ROS formation as luminol-enhanced CL in human neutrophils or eosinophils with IC35 of 4 nM, and 7 nM, repectively. Roflumilast inhibits LPS-stimulated TNF-α synthesis in monocytes with IC40 of 21 nM. Roflumilast inhibits TNF-α synthesis in monocyte-derived dendritic cells with IC20 of 5 nM. Rolfumilast inhibits anti-CD3 and anti-CD28 antibody-stimulated proliferation of CD4+ T cells with IC30 of 7 nM. Rolfumilast inhibits anti-CD3 and anti-CD28 antibody-stimulated synthesis of IL-2, IL-4, IL-5, and IFN-v in CD4+ T cells with IC20 of 1 nM, IC30 of 7 nM, IC25 of 13 nM, and IC35 of 8 nM, respectively. In vivo Roflumilast is activity against pulmonary inflammatory response related to COPD in animal model. Roflumilast (5 mg/kg/day) induces reduction of neutrophils, macrophages, DC, B-cells, CD4⁺ T cells, CD8⁺ T cells in the lung of mice exposed to tobacco smoke for 7 month by 78%, 82%, 48%, 100%, 98%, and 88%, respectively. Roflumilast is an efficient inhibitor of lung fibrotic remodeling. Roflumilast dose-dependently diminishes total lung hydroxyproline after bleomycin, attaining about 47% inhibition at 5 mg/kg/day, paralleled by a reduction in lung αI(I) collagen transcripts and fibrotic lesions. Roflumilast reduces oxidative stress in vivo. Roflumilast (5 mg/kg/day) moderately reduces an increase in BAL fluid lipid hydroperoxides measured at day 14 after intratracheal bleomycin administration in mice. Cell Data cell lines：mixed neuronal/glial cell cultures Concentrations： Incubation Time： Powder Purity:≥99%

Associated Targets(Human)

PDE4D Tclin cAMP-specific 3',5'-cyclic phosphodiesterase 4D (14 Activities)

Discover Target: PDE4D

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PDE4C Tclin cAMP-specific 3',5'-cyclic phosphodiesterase 4C (1 Activities)

Discover Target: PDE4C

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PDE4A Tclin cAMP-specific 3',5'-cyclic phosphodiesterase 4A (3 Activities)

Discover Target: PDE4A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PDE4B Tclin cAMP-specific 3',5'-cyclic phosphodiesterase 4B (26 Activities)

Discover Target: PDE4B

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

Smiles	FC(F)OC1=CC=C(C=C1OCC2CC2)C(=O)NC3=C(Cl)C=NC=C3Cl
Molecular Weight	403.21

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):

Analytical Chart:

Chemical and Physical Properties

Solubility	Solubility (25°C) In vitro DMSO: 74 mg/mL (199.84 mM); Water: 74 mg/mL (199.84 mM); Ethanol: 74 mg/mL (199.84 mM);

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