Description
Win 58237 is a cyclic nucleotide phosphodiesterase (PDE) inhibitor, with Ki of 170 nM for PDE V, possessing vasorelaxant activity.
Product information
CAS Number: 158001-76-4
Molecular Weight: 295.34
Formula: C16H17N5O
Chemical Name: 1-cyclopentyl-3-methyl-6-(pyridin-4-yl)-1H,4H,7H-pyrazolo[3,4-d]pyrimidin-4-one
Smiles: CC1=NN(C2CCCC2)C2NC(=NC(=O)C=21)C1C=CN=CC=1
InChiKey: GODZWYONGRENHA-UHFFFAOYSA-N
InChi: InChI=1S/C16H17N5O/c1-10-13-15(21(20-10)12-4-2-3-5-12)18-14(19-16(13)22)11-6-8-17-9-7-11/h6-9,12H,2-5H2,1H3,(H,18,19,22)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Win 58237 is a competitive inhibitor of cGMP PDE V from canine aorta, with a Ki value of 170 nM. Win 58237 is a potent inhibitor of PDE V isolated from vascular tissue with an IC50 value of 240 nM. It is a relatively less potent inhibitor of calmodulin-sensitive PDE I and cGMP-inhibitable cyclic AMP PDE III; but does inhibit cyclic AMP PDE IV with an IC50 value of approximately 300 nM. Win 58237 possesses vasorelaxant activity in the presence of an intact endothelium or nitric oxide.
In Vivo:
Win 58237 (0.3-3.0 mg/kg i.v.) decreases mean arterial pressure in conscious spontaneously hypertensive rats with an associated increase in vascular (aortic) cGMP content in vivo. Win 58237 (10 mg/kg i.v.) increases plasma cGMP levels, from basal levels of 6.7 ± 1.0 to 31.4 ± 3.5 fmol/μL.
Products are for research use only. Not for human use.
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