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Rivaroxaban

Cat. No. M1776
Rivaroxaban Structure
Synonym:

Xarelto, BAY 59-7939

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 59  USD59 In stock
10mg USD 82  USD82 In stock
50mg USD 160  USD160 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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).

Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 435.88
Formula C19H18ClN3O5S
CAS Number 366789-02-8
Purity >99%
Solubility DMSO 60 mg/mL
Storage at -20°C
References

[1] Paikin JS, et al. Expert Rev Cardiovasc Ther. Rivaroxaban for stroke prevention in atrial fibrillation: a critical review of the ROCKET AF trial.

[2] Haynes LM, et al. Arterioscler Thromb Vasc Biol. Rivaroxaban Delivery and Reversal at a Venous Flow Rate.

[3] Turpie AG, et al. Thromb Haemost. Management consensus guidance for the use of rivaroxaban - an oral, direct factor Xa inhibitor.

[4] Douxfils J, et al. Thromb Res. Assessment of the impact of rivaroxaban on coagulation assays: Laboratory recommendations for the monitoring of rivaroxaban and review of the literature.

[5] Gnoth MJ, et al. J Pharmacol Exp Ther. In vitro and in vivo P-glycoprotein transport characteristics of rivaroxaban.

[6] Perzborn E, et al. J Thromb Haemost. In vitro and in vivo studies of the novel antithrombotic agent BAY 59-7939--an oral, direct Factor Xa inhibitor.

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Keywords: Rivaroxaban, Xarelto, BAY 59-7939 supplier, Factor Xa, inhibitors

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