{"product_id":"m14456","title":"Sibrafiban","description":"\u003cp style=\"padding-left: 1em;\"\u003eSibrafiban (RO 48-3657) is the orally active, nonpeptide, double-prodrug of Ro 44-3888 and a selective glycoprotein IIb\/IIIa receptor antagonist. Sibrafiban inhibits platelet aggregation.\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eProduct information\u003c\/strong\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eCAS Number:\u003c\/strong\u003e 172927-65-0\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eMolecular Weight:\u003c\/strong\u003e 420.46\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eFormula:\u003c\/strong\u003e C20H28N4O6\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eSynonym:\u003c\/strong\u003e\u003c\/p\u003e\n\u003cp style=\"padding-left: 1em;\"\u003eRO 48-3657\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eChemical Name:\u003c\/strong\u003e ethyl 2-({1-[(2S)-2-({4-[(Z)-N'-hydroxycarbamimidoyl]phenyl}formamido)propanoyl]piperidin-4-yl}oxy)acetate\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eSmiles:\u003c\/strong\u003e C[C@H](NC(=O)C1C=CC(=CC=1)\/C(\/N)=N\/O)C(=O)N1CCC(CC1)OCC(=O)OCC\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eInChiKey:\u003c\/strong\u003e WBNUCLPUOSXSNJ-ZDUSSCGKSA-N\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eInChi:\u003c\/strong\u003e InChI=1S\/C20H28N4O6\/c1-3-29-17(25)12-30-16-8-10-24(11-9-16)20(27)13(2)22-19(26)15-6-4-14(5-7-15)18(21)23-28\/h4-7,13,16,28H,3,8-12H2,1-2H3,(H2,21,23)(H,22,26)\/t13-\/m0\/s1\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eTechnical Data\u003c\/strong\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eAppearance:\u003c\/strong\u003e Solid Power\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003ePurity:\u003c\/strong\u003e ≥98% (or refer to the Certificate of Analysis)\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eShipping Condition:\u003c\/strong\u003e Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eStorage Condition:\u003c\/strong\u003e Dry, dark and -20 \u003csup\u003eo\u003c\/sup\u003eC for 1 year or refer to the Certificate of Analysis.\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eShelf Life:\u003c\/strong\u003e ≥12 months if stored properly.\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eStock Solution Storage:\u003c\/strong\u003e 0 - 4 \u003csup\u003eo\u003c\/sup\u003eC for 1 month or refer to the Certificate of Analysis.\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eDrug Formulation:\u003c\/strong\u003e To be determined\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eHS Tariff Code:\u003c\/strong\u003e 382200\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eHow to use\u003c\/strong\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eIn Vitro:\u003c\/strong\u003e\u003c\/p\u003e\n\u003cp style=\"padding-left: 1em;\"\u003eThe effects of site occupancy by Sibrafiban on platelet activation are assessed using P-selectin expression, fibrinogen binding and microaggregate formation. Sibrafiban inhibits ADP and TRAP-stimulated fibrinogen binding and microaggregate formation in a concentration-dependent manner, whereas P-selectin expression is relatively unaltered. A decrease in site occupancy from peak to trough of Sibrafiban does not result in increased activation of platelets.\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eIn Vivo:\u003c\/strong\u003e\u003c\/p\u003e\n\u003cp style=\"padding-left: 1em;\"\u003eThe effects of Ro 44-3888 on the platelet aggregation response to ADP (17 μmol) and on cutaneous bleeding times is determined in 8 rhesus monkeys given Sibrafiban 0.25 mg\/kg\/day or 0.5 mg\/kg\/day orally for 8 days. The maximum inhibition of ex vivo platelet aggregation and prolongation of bleeding time by Ro 44-3888 are dose dependent.\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eReferences:\u003c\/strong\u003e\u003c\/p\u003e\n\u003col style=\"padding-left: 1em;\"\u003e\n\u003cli\u003eM Dooley, et al. Sibrafiban. Drugs. 1999 Feb;57(2):225-30; discussion 231-2.\u003c\/li\u003e\n\u003cli\u003eB Wittke, et al. Pharmacokinetics and pharmacodynamics of sibrafiban alone or in combination with ticlopidine and aspirin. Br J Clin Pharmacol. 2000 Mar;49(3):231-9.\u003c\/li\u003e\n\u003cli\u003eJeffrey T Billheimer, et al. 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.\u003c\/li\u003e\n\u003c\/ol\u003e\n\u003cp\u003e\u003cstrong\u003eProducts are for research use only. Not for human use.\u003c\/strong\u003e\u003c\/p\u003e","brand":"Xcess Biosciences","offers":[{"title":"M14456-2 \/ Contact sales@xcessbio.com for quotation","offer_id":39462441353355,"sku":"","price":100.0,"currency_code":"USD","in_stock":true}],"thumbnail_url":"\/\/cdn.shopify.com\/s\/files\/1\/0389\/1897\/9723\/files\/1686549592517.png?v=1686549620","url":"https:\/\/www.xcessbio.com\/products\/m14456","provider":"Xcess Biosciences","version":"1.0","type":"link"}