{"product_id":"m6488","title":"Anacetrapib - CAS# 875446-37-0","description":"\u003cp style=\"padding-left:1em;\"\u003eAnacetrapib, also known as MK-0859, CAS No. 875446-37-0, is a CETP inhibitor being developed to treat hypercholesterolemia (elevated cholesterol levels) and prevent cardiovascular disease.\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eProduct information\u003c\/strong\u003e\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eCAS Number:\u003c\/strong\u003e 875446-37-0\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eMolecular Weight:\u003c\/strong\u003e 637.51\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eFormula:\u003c\/strong\u003e C30H25F10NO3\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eSynonym:\u003c\/strong\u003e\u003c\/p\u003e\u003cp style=\"padding-left:1em;\"\u003eMK0859\u003c\/p\u003e\u003cp style=\"padding-left:1em;\"\u003eAnacetrapib\u003c\/p\u003e\u003cp style=\"padding-left:1em;\"\u003eMK-0859\u003c\/p\u003e\u003cp style=\"padding-left:1em;\"\u003eMK 0859\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eChemical Name:\u003c\/strong\u003e (4S,5R)-5-(3,5-bis(trifluoromethyl)phenyl)-3-((4'-fluoro-5'-isopropyl-2'-methoxy-4-(trifluoromethyl)-[1,1'-biphenyl]-2-yl)methyl)-4-methyloxazolidin-2-one.\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eSmiles:\u003c\/strong\u003e CC(C)C1=CC(=C(C=C1F)OC)C1=CC=C(C=C1CN1[C@@H](C)[C@H](OC1=O)C1C=C(C=C(C=1)C(F)(F)F)C(F)(F)F)C(F)(F)F\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eInChiKey:\u003c\/strong\u003e MZZLGJHLQGUVPN-HAWMADMCSA-N\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eInChi:\u003c\/strong\u003e InChI=1S\/C30H25F10NO3\/c1-14(2)22-11-23(25(43-4)12-24(22)31)21-6-5-18(28(32,33)34)9-17(21)13-41-15(3)26(44-27(41)42)16-7-19(29(35,36)37)10-20(8-16)30(38,39)40\/h5-12,14-15,26H,13H2,1-4H3\/t15-,26-\/m0\/s1\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eTechnical Data\u003c\/strong\u003e\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eAppearance:\u003c\/strong\u003e Solid Power\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003ePurity:\u003c\/strong\u003e ≥98% (or refer to the Certificate of Analysis)\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eSolubility:\u003c\/strong\u003e Soluble in DMSO, not in water\u003c\/p\u003e\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\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\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eShelf Life:\u003c\/strong\u003e ≥12 months if stored properly.\u003c\/p\u003e\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\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eDrug Formulation:\u003c\/strong\u003e To be determined.\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eHS Tariff Code:\u003c\/strong\u003e 382200\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eHow to use\u003c\/strong\u003e\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eIn Vitro:\u003c\/strong\u003e\u003c\/p\u003e\u003cp style=\"padding-left:1em;\"\u003eAnacetrapib dose-dependently and significantly decreases the transfer of CE from HDL3 to HDL2 (P\u0026lt;0.001 for concentrations equal to and higher than 0.1 µM). Excess Anacetrapib (25 µM) decreases the amount of [14C]Torcetrapib (0.25 µM) binds to immobilized rhCETP by 82% and 60%, respectively. Anacetrapib decreases pre-β-HDL formation by more than 46% (P\u0026lt;0.001) at all concentrations tested (0.1, 1, 3, and 10 µM). A significant reduction of PCSK9 promoter activity by Anacetrapib (ANA) is detected at 3 µM concentration (−22%, p\u0026lt;0.01) and further lowered to 68% of control at 10 µM. Likewise, luciferase activity of B11 cells are decreased by Anacetrapib at 3 µM concentration and reached to a maximal reduction of 38% of control at 10 µM. At 10 µM concentration, Anacetrapib loweres PCSK9 mRNA level to 60% of control and LDLR mRNA level to 67% of control.\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eIn Vivo:\u003c\/strong\u003e\u003c\/p\u003e\u003cp style=\"padding-left:1em;\"\u003eHamsters are given Anacetrapib for 7 days before injection of [3H]cholesterol-labeled macrophages (day 0). Treatment with Anacetrapib leads to significant increases in HDL-C levels at day 0. At day 3, [3H]cholesterol radioactivity in the HDL fraction is significantly increased from control values for Anacetrapib. Anacetrapib (ANA) treatment modestly elevates serum total serum cholesterol levels ~10% (p\u0026lt;0.05) and increases serum LDL-C by 26% (p\u0026lt;0.05) as compared to vehicle control. After an intravenous dose of 0.5 mg\/kg, the mean values for systemic plasma clearance, steady-state volume of distribution, and terminal half-life are 2.3 mL\/min\/kg, 1.1 L\/kg, and 12 h, respectively. After oral dosing at 5 mg\/kg, the bioavailability of Anacetrapib is 38%. Exposures (AUC) increases in a less than dose-proportional manner from 23 μM•h at 5 mg\/kg to 362 μM•h at 500 mg\/kg. In this dose range, the peak plasma level (Cmax) ranges from 5 to 26 μM and the time to reach peak plasma level (Tmax) ranged from 3 to 4.5 h.\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eReferences:\u003c\/strong\u003e\u003c\/p\u003e\u003col style=\"padding-left:1em;\"\u003e\n\u003cli\u003eKrishna R, Stypinski D, Ali M, Garg A, Cote J, Maes A, Degroot B, Liu Y, Li S, Connolly SM, Wagner JA, Stoch SA. Lack of a meaningful effect of anacetrapib on the pharmacokinetics and pharmacodynamics of warfarin in healthy subjects. Br J Clin Pharmacol. 2012 Jul;74(1):116-24. doi: 10.1111\/j.1365-2125.2012.04171.x. PubMed PMID: 22243494.\u003c\/li\u003e\n\u003cli\u003eHooper AJ, Burnett JR. Anacetrapib, a cholesteryl ester transfer protein inhibitor. Expert Opin Investig Drugs. 2012 Jan;21(1):103-9. Epub 2011 Dec 22. PubMed PMID: 22191425.\u003c\/li\u003e\n\u003cli\u003eKrauss RM, Wojnooski K, Orr J, Geaney JC, Pinto CA, Liu Y, Wagner JA, Luk JM, Johnson-Levonas AO, Anderson MS, Dansky HM. Changes in lipoprotein subfraction concentration and composition in healthy individuals treated with the CETP inhibitor anacetrapib. J Lipid Res. 2012 Mar;53(3):540-7. Epub 2011 Dec 17. PubMed PMID: 22180633; PubMed Central PMCID: PMC3276477.\u003c\/li\u003e\n\u003c\/ol\u003e\u003cp\u003e\u003cstrong\u003eProducts are for research use only. Not for human use.\u003c\/strong\u003e\u003c\/p\u003e","brand":"xcessbio","offers":[{"title":"M6488-2 \/ 2mg solid","offer_id":57068107628870,"sku":"30","price":52.0,"currency_code":"USD","in_stock":true},{"title":"M6488-10 \/ 10mg solid","offer_id":57068107661638,"sku":"30","price":124.0,"currency_code":"USD","in_stock":true}],"thumbnail_url":"\/\/cdn.shopify.com\/s\/files\/1\/0998\/9102\/0102\/files\/Anacetrapib_bc629730-3dc2-4f67-9a83-83797483a07c.png?v=1785915795","url":"https:\/\/luckpolly.com\/products\/m6488","provider":"luck Polly","version":"1.0","type":"link"}