Description
BYK 49187 is a potent inhibitor of PARP-1 and PARP-2 with pIC50 value pIC50 values of 8.36 and 7.50 for cell-free recombinant PARP-1 and murine PARP-2 respectively . Poly (ADP-ribose) polymerase (PARP) is a family of proteins involved in a number of cellular processes involving mainly DNA repair and programmed cell death . BYK 49187 is a potent inhibitor of human PARP and displays no selectivity for PARP1/2 . PAR formation in A549, C4I, and H9c2 cells was inhibited by BYK49187 with pIC50 values of 7.80, 7.02, and 7.65, respectively. BYK 49187 displays potent inhibitory activity against human PARP-1 in cell-free and cellular assays in vitro . In the test of effect of BYK 49187 on myocardial infarct size in the rat, intravenous administration of the lower dose of BYK 49187 was nearly ineffective (only 6% reduction in infarct size), whereas the higher dose (3 mg/kg followed by 3 mg/kg/h) caused a significant reduction in infarct size of 22% compared with vehicle. Blood samples of rats treated with 3 mg/kg i.v. BYK49187 significantly inhibited PARP-1 by 80% compared with sham operation .
Product information
CAS Number: 163120-31-8
Molecular Weight: 335.40
Formula: C19H21N5O
Chemical Name: 2-[4-(4-methyl-1H-imidazol-5-yl)piperidin-1-yl]-1,3-diazatricyclo[6.3.1.0⁴,¹²]dodeca-2,4,6,8(12)-tetraen-9-one
Smiles: CC1N=CNC=1C1CCN(CC1)C1=NC2=CC=CC3C(=O)CCN1C=32
InChiKey: YKJJROIKVYSPDH-UHFFFAOYSA-N
InChi: InChI=1S/C19H21N5O/c1-12-17(21-11-20-12)13-5-8-23(9-6-13)19-22-15-4-2-3-14-16(25)7-10-24(19)18(14)15/h2-4,11,13H,5-10H2,1H3,(H,20,21)
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
Products are for research use only. Not for human use.
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