BMS-740808

ArtNr	S1571-10
Hersteller	Selleckchem
CAS-Nr.	280118-23-2, 280118-24-3 (TFA)
Menge	10 mg
Kategorie	Inhibitors & Compound Libraries Small Molecules
Typ	Inhibitors
Specific against	other
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	fXa, Rabbit AVshunt, Thrombin;Factor Xa
Lieferbar
Administration	Given as continuous i.v. infusion via the jugular vein
Animal Models	Male rabbit AVShunt thrombosis model.
Chemical Name	7H-Pyrazolo[3, 4-c]pyridin-7-one, 1-(3-amino-1, 2-benzisoxazol-5-yl)-1, 4, 5, 6-tetrahydro-6-[2'-[[(3R)-3-hydroxy-1-pyrrolidinyl]methyl][1, 1'-biphenyl]-4-yl]-3-(trifluoromethyl)-
Description	BMS-740808 is a highly potent, selective inhibitor of blood coagulation factor Xa (fXa) with Ki with 0.03 nM.
Dosages	2 uM
Formulation	BMS-740808 is dissolved in saline.
IC50	0.03 nM (Ki), 0.03 nM (Ki), 0.03 nM (Ki), 0.03 nM (Ki), 0.03 nM (Ki), 0.03 nM (Ki)
In vitro	BMS-740808 is highly potent with a rapid onset of inhibition (2.7, 107 M-1 s-1), selective (>1000-fold over other proteases), efficacious in the AVShunt thrombosis model. BMS-740808 is synthesized by modification of employing bicyclic pyrazolo-pyridinone scaffold to Razaxaban, a pyrazole based fXa inhibitor. Especially for BMS-740808, the introduction of a 3(R)-hydroxyl moiety on the pyrrolidine ring results in a significant enhancement in potency. BMS-740808 also shows the high affinity for thrombin. [1]
In vivo	The pharmacokinetic profile for BMS-740808 is comparable to that of Razaxaban with moderate half life, whereas BMS-740808 shows low clearance, low Vdss, moderate half life and high oral bio-availability, which is quite possibly due to the hydroxyl substituent on the cyclic amino moiety. [1]
Kinase Assay	Ki Determination, FXa (1 nM) is added to a 96-well plate containing BMS-740808 (5 pM to 3 uM) in buffer A (20 mM HEPES, 0.15 M NaCl, 0.1% PEG-8000, 5 mM CaCl2, pH 7.4). S-2765 (N-alpha-Z-d-Arg-Gly-Arg-p Nitroanilide) at 200 uM is added, and substrate hydrolysis is monitored at 405 nm. Data are analyzed by Batch Ki software.
Molecular Weight (MW)	588, 58
Picture ChemicalStructure Description	BMS-740808 Chemical Structure
Storage	2 years -20CPowder, 2 weeks4Cin DMSO, 2 months-80Cin DMSO

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Menge: 10 mg

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