BMS-740808 is a highly potent, selective, efficacious, and orally bioavailable blood coagulation factor Xa inhibitor with a Ki of 30 pM. It has a rapid onset of inhibition (2.7 × 107 M−1 /s) in vitro, selective (>1000-fold over other proteases), efficacious in the AVShunt thrombosis model, and orally bioavailable inhibitor of blood coagulation factor Xa.
| Molecular Weight | 588.58 |
| Formula | C31H27F3N6O3 |
| CAS Number | 280118-23-2 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Factor Xa Products |
|---|
| Suc-Ile-Glu(γ-pip)-Gly-Arg-pNA hydrochloride
Suc-Ile-Glu(γ-pip)-Gly-Arg-pNA hydrochloride is a factor Xa specific chromogenic substrate. |
| D-Pro-Phe-Arg-Chloromethylketone
D-Pro-Phe-Arg-Chloromethylketone, a inhibitor of coagulation factor XII and plasma kallikrein, plays an important role in thrombosis and inflammation. |
| Methoxycarbonyl-D-Nle-Gly-Arg-pNA
Methoxycarbonyl-D-Nle-Gly-Arg-pNA is a synthetic trypsin that can serve as a substrate for coagulation factors IXa (FIXa) and Xa (FXa). |
| Boc-Ile-Glu-Gly-Arg-AMC
Boc-Ile-Glu-Gly-Arg-AMC (IEGR-AMC) is an activated factor X (FXa) specific fluorogenic peptide substrate used for Factor VIII determination. |
| Delparantag
Delparantag (PMX-60056) is a salicylamide derivative and an effective unfractionated heparin (UFH) and low molecular weight heparin (LMWH) reversing agent. |
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