AR-H067637
| Code | Size | Price |
|---|
| TAR-T26657-5mg | 5mg | £1,332.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
| TAR-T26657-50mg | 50mg | £2,625.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
| TAR-T26657-100mg | 100mg | £3,524.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃
Documents
Further Information
Bioactivity:
AR-H067637 is a rapid-binding, reversible and potent (inhibition constant K(i) = 2-4 nM), competitive inhibitor of thrombin, as well as of thrombin bound to fibrin (clot-bound thrombin) or to thrombomodulin. The total amount of free thrombin generated in platelet-poor clotting plasma was inhibited concentration-dependently by AR-H067637, with a concentration giving half maximal inhibition (IC(50)) of 0.6 microM. AR-H067637 also inhibited thrombin-induced platelet activation (by glycoprotein IIb/IIIa exposure, IC(50) 8.4 nM) and aggregation (IC(50) 0.9 nM).
CAS:
433937-74-7
Formula:
C21H21ClF2N4O4
Molecular Weight:
466.87
Purity:
0.98
SMILES:
O=C([C@H]1N(C([C@@H](C2=CC(OC(F)F)=CC(Cl)=C2)O)=O)CC1)NCC3=CC=C(C(N)=N)C=C3
References
1. Pehrsson S, Johansson K, Kjaer M, Elg M. Evaluation of AR-H067637, the active metabolite of the new direct thrombin inhibitor AZD0837, in models of venous and arterial thrombosis and bleeding in anaesthetised rats. Thromb Haemost. 2010 Dec;104(6):1242-9. doi: 10.1160/TH09-10-0744. PubMed PMID: 20806126.
2. Deinum J, Mattsson C, Inghardt T, Elg M. Biochemical and pharmacological effects of the direct thrombin inhibitor AR-H067637. Thromb Haemost. 2009 Jun;101(6):1051-9. PubMed PMID: 19492147.
3. Lip GY, Rasmussen LH, Olsson SB, Jensen E, Hamr?n B, Eriksson UG, W?hlander K. Exposure-response for biomarkers of anticoagulant effects by the oral direct thrombin inhibitor AZD0837 in patients with atrial fibrillation. Br J Clin Pharmacol. 2015 Dec;80(6):1362-73. doi: 10.1111/bcp.12719. PubMed PMID: 26174611; PubMed Central PMCID: PMC4693476.
4. Dun?r K, Hulthe J, Tranberg M. Determination of the thrombin inhibitor AZD0837 and its metabolites in human bile using mixed mode solid phase extraction and LC-MS/MS. J Chromatogr B Analyt Technol Biomed Life Sci. 2012 Sep 1;904:29-34. doi: 10.1016/j.jchromb.2012.06.026. PubMed PMID: 22871267.