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 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.
|Incubation time||2 h|
|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|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO 60 mg/mL|
|Related Factor Xa Products|
Ozagrel(OKY-046) sodium salt is an antiplatelet agent working as a thromboxane A2 synthesis inhibitor.
Ozagrel is a potent and selective thromboxane A2 synthetase inhibitor with an IC50 of 4 nM.
|Edoxaban Tosylate Monohydrate
Edoxaban is a selective factor Xa inhibitor with Ki of 0.561 nM, >10 000-fold selectivity over thrombin and FIXa, and is also an orally bioavailable anticoagulant compound.
Betrixaban is a highly potent, selective, and orally efficacious factor Xa inhibitor with IC50 of 1.2 nM(inhibition of Factor 10a).
Apixaban is a highly selective, reversible and direct factor Xa inhibitor with an IC50 of 0.22±0.02 µM.
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