WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H596765
CAS#: 170902-47-3
Description: Roxifiban is a prodrug whose methyl-ester is hydrolysed following oral adminstration to form the GPIIb/GPIIIA antagonist XV459.
Hodoodo Cat#: H596765
Name: Roxifiban
CAS#: 170902-47-3
Chemical Formula: C21H29N5O6
Exact Mass: 447.21
Molecular Weight: 447.490
Elemental Analysis: C, 56.37; H, 6.53; N, 15.65; O, 21.45
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Synonym: Roxifiban; DMP754; DMP 754; DMP-754;
IUPAC/Chemical Name: methyl (S)-2-((butoxycarbonyl)amino)-3-(2-((R)-3-(4-carbamimidoylphenyl)-4,5-dihydroisoxazol-5-yl)acetamido)propanoate
InChi Key: IRAXRQFCCSHQDX-WBVHZDCISA-N
InChi Code: InChI=1S/C21H29N5O6/c1-3-4-9-31-21(29)25-17(20(28)30-2)12-24-18(27)11-15-10-16(26-32-15)13-5-7-14(8-6-13)19(22)23/h5-8,15,17H,3-4,9-12H2,1-2H3,(H3,22,23)(H,24,27)(H,25,29)/t15-,17+/m1/s1
SMILES Code: O=C(OC)[C@H](CNC(C[C@H]1CC(C2=CC=C(C(N)=N)C=C2)=NO1)=O)NC(OCCCC)=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 447.49 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
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6: Mousa SA, Ahmad S. Platelet GPIIb/IIIa antagonist, XV459, in heparin-induced thrombocytopenia. Am J Hematol. 2007 Apr;82(4):276-82. PubMed PMID: 17039513.
7: Mousa SA, Bozarth JM, Seiffert D, Feuerstein GZ. Using thrombelastography to determine the efficacy of the platelet glycoprotein IIb/IIIa antagonist, roxifiban, on platelet/fibrin-mediated clot dynamics in humans. Blood Coagul Fibrinolysis. 2005 Apr;16(3):165-71. PubMed PMID: 15795533.
8: Murphy J, Wright RS, Gussak I, Williams B, Daly RN, Cain VA, Pieniaszek HJ, Sy SK, Ebling W, Simonson K, Wilcox RA, Kopecky SL. The use of roxifiban (DMP754), a novel oral platelet glycoprotein IIb/IIIa receptor inhibitor, in patients with stable coronary artery disease. Am J Cardiovasc Drugs. 2003;3(2):101-12. PubMed PMID: 14727937.
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13: Bayes M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2003 Jun;25(5):387-408. PubMed PMID: 12851663.
14: Serebruany VL, Malinin AI, O'connor CM, Gurbel PA; Roxifiban Oral Compound Kinetics Evaluation Trial-I Platelet Substudy. Effects of roxifiban on platelet aggregation and major receptor expression in patients with coronary artery disease for the Roxifiban Oral Compound Kinetics Evaluation Trial-I (ROCKET-I Platelet Substudy). Am Heart J. 2003 Jul;146(1):91-8. PubMed PMID: 12851613.
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18: Pedicord DL, Dicker I, O'Neil K, Breth L, Wynn R, Hollis GF, Billheimer JT, Stern AM, Seiffert D. CD32-dependent platelet activation by a drug-dependent antibody to glycoprotein IIb/IIIa antagonists. Thromb Haemost. 2003 Mar;89(3):513-21. PubMed PMID: 12624636.
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20: Billheimer JT, He B, Spitz SM, Stern AM, Seiffert D. Effects of glycoprotein IIb/IIIa antagonists on platelet activation: development of a transfer method to mimic peak to trough receptor occupancy. Thromb Res. 2002 Sep 15;107(6):303-17. PubMed PMID: 12565717.