R-1663

TargetMol
Product Code: TAR-T28491
Supplier: TargetMol
CodeSizePrice
TAR-T28491-5mg5mg£1,091.00
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TAR-T28491-50mg50mg£2,143.00
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Quantity:
TAR-T28491-100mg100mg£2,801.00
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Overview

Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃

Images

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Further Information

Bioactivity:
R-1663 is a factor Xa inhibitor. R-1663 prolonged clotting times, inhibited thrombin generation (peak height and endogenous thrombin potential [ETP]) and anti-factor Xa activity in a concentration-dependent manner without increasing bleeding time. Pharmacodynamic parameters were strongly correlated to R-1663 plasma concentrations. The inhibition was more pronounced on peak height (IC?? = 194 ng/ml) than on ETP (2790 ng/ml).
CAS:
865451-66-7
Formula:
C22H23ClN4O5
Molecular Weight:
458.9
Purity:
0.98
SMILES:
O=C(N1[C@@H](C(NC2=CC=C(N3C(COCC3)=O)C=C2)=O)C[C@@H](O)C1)NC4=CC=C(Cl)C=C4

References

1. Schmitt C, Pannier A, McIntyre C, Zandt H, Ciorciaro C, Winters K, Pepper T. Crossover dose escalation study to assess safety, pharmacokinetics, and pharmacodynamics of single doses of R1663, an oral factor Xa inhibitor, in healthy male volunteers. J Clin Pharmacol. 2012 Apr;52(4):499-510. doi: 10.1177/0091270011401621. PubMed PMID: 21566199. 2. Schmitt C, Charoin-Pannier A, McIntyre C, Zandt H, Ciorciaro C, Zweigler L, Winters K, Pepper T. Effect of food on the pharmacokinetics and pharmacodynamics of R1663, an oral factor Xa inhibitor, in healthy male volunteers. Int J Clin Pharmacol Ther. 2012 Aug;50(8):566-72. doi: 10.5414/CP201697. PubMed PMID: 22735461. 3. Schmitt C, Charoin-Pannier A, McIntyre C, Zandt H, Ciorciaro C, Winters K, Pepper T. Safety, pharmacokinetics and pharmacodynamics of multiple ascending doses of R1663, an oral factor Xa inhibitor, in healthy young subjects coupled with exploration of influence of gender and age. Thromb Haemost. 2012 Jul;108(1):54-64. doi: 10.1160/TH12-01-0023. PubMed PMID: 22552265. 4. Farhy LS, Bowers CY, Veldhuis JD. Model-projected mechanistic bases for sex differences in growth hormone regulation in humans. Am J Physiol Regul Integr Comp Physiol. 2007 Apr;292(4):R1577-93. PubMed PMID: 17185408.