Item no. |
S1571-10 |
Manufacturer |
Selleckchem
|
CASRN |
280118-23-2, 280118-24-3 (TFA) |
Amount |
10 mg |
Category |
|
Type |
Inhibitors |
Specific against |
other |
ECLASS 10.1 |
32160490 |
ECLASS 11.0 |
32160490 |
UNSPSC |
12000000 |
Alias |
fXa, Rabbit AVshunt, Thrombin;Factor Xa |
Available |
|
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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