Rivaroxaban (Xarelto, BAY 59-7939) is oral direct factor Xa inhibitor with an IC50 value of 2.1nM. Rivaroxaban (Xarelto,BAY 59-7939) inhibits endogenous FXa more potently in human and rabbit plasma (IC50 = 21 nM) than in rat plasma (IC50 = 290 nM).Rivaroxaban (Xarelto,BAY 59-7939) also shows a similar affinity to purified human and rabbit FXa (IC50=0.7 nM and 0.8 nM, respectively), but a lesser potency against purified rat FXa (IC50 3.4 nM).
| Cell Experiment | |
|---|---|
| Cell lines | L-MDR1 and Caco-2 cells line |
| Preparation method | Calculation of the Apparent Permeability Coefficient Values for Rivaroxaban. The apparent permeability coefficient (Papp) was calculated using eq. 1:where Papp is the apparent permeability, Vr is the volume of medium in the receiver chamber, C0 is the concentration of the test drug in the donor chamber at t = 0 h, S is the surface area of the monolayer, C2 is the concentration of the test drug in the acceptor chamber after 2 h of incubation, and t is the incubation time. For reference compounds, peak heights were used instead of concentrations.where Papp(B–A) and Papp(A–B) represent the apparent permeability of the test compound from the basolateral to apical and apical to basolateral sides of the cellular monolayer, respectively. The S.D. for the efflux ratio was calculated using eq. 3:where SD Papp(B–A) and SD Papp(A–B) represent the standard deviations of the apparent permeability of test compound from the basolateral to apical and apical to basolateral side of the cellular monolayer, respectively. |
| Concentrations | 2 μM |
| Incubation time | 2 h |
| Animal Experiment | |
|---|---|
| Animal models | Rat venous stasis model |
| Formulation | dissolved in polyethylene glycol/H2O/ glycerol (996 g/100 g/60 g) |
| Dosages | 0.03, 0.1 and 0.3mg/kg |
| Administration | intravenous (i.v.) bolus injection into a tail vein |
| Molecular Weight | 435.88 |
| Formula | C19H18ClN3O5S |
| CAS Number | 366789-02-8 |
| Solubility (25°C) | DMSO 60 mg/mL |
| 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 |
|---|
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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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