{"product_id":"mk-8245-trifluoroacetate-bhb21900766","title":"MK-8245 Trifluoroacetate","description":"\u003cdiv class=\"bhp-desc\"\u003e\n\u003cstyle\u003e.bhp-desc{font-size:16px;color:#1a1a1a;line-height:1.7}.bhp-desc h2{font-size:18px;font-weight:700;color:#003366;margin:24px 0 10px;padding-bottom:6px;border-bottom:2px solid #003366}.bhp-desc p{margin:0 0 12px}.bhp-desc .bhp-spec-table{width:100%;border-collapse:collapse;margin:12px 0 18px}.bhp-desc .bhp-spec-table th{width:36%;text-align:left;padding:8px 12px;background:#e8f0fb;color:#003366;font-weight:600;vertical-align:top;border:1px solid #ccd9f0}.bhp-desc .bhp-spec-table td{padding:8px 12px;vertical-align:top;border:1px solid #ccd9f0}.bhp-desc .bhp-warning-box{background:#fff8e6;border-left:4px solid #e6a817;padding:10px 14px;margin:10px 0 14px;border-radius:0 4px 4px 0}.bhp-desc .bhp-cat-pill{display:inline-block;background:#003366;color:#fff;border-radius:20px;padding:3px 12px;font-size:13px;margin-bottom:10px}\u003c\/style\u003e\n\u003cspan class=\"bhp-cat-pill\"\u003eInhibitors\u003c\/span\u003e\u003ch2\u003eCompound Overview\u003c\/h2\u003e\n\u003cp\u003eMK-8245 Trifluoroacetate is a liver-targeting inhibitor of stearoyl-CoA desaturase (SCD), with an IC\u003csub\u003e50\u003c\/sub\u003e of 1 nM for human SCD1 and 3 nM for both rat and mouse SCD1, giving it anti-diabetic and anti-dyslipidemic efficacy\u003csup\u003e[1]\u003c\/sup\u003e. Chemically a phenoxy piperidine isoxazole derivative, it carries a tetrazole acetic acid moiety that is key to recognition by OATP transporters and to its liver targeting. In a rat hepatocyte assay containing functional OATPs it shows an IC\u003csub\u003e50\u003c\/sub\u003e of 68 nM, whereas in the OATP-deficient HepG2 cell assay it is only weakly active (IC\u003csub\u003e50\u003c\/sub\u003e ~1 μM), and it is highly selective for SCD over the Δ-5 and Δ-6 desaturases (\u0026gt;100000 μM against rat and human Δ5D and Δ6D)\u003csup\u003e[1]\u003c\/sup\u003e.\u003c\/p\u003e\n\u003cp\u003eIn mice dosed at 10 mg\/kg, MK-8245 Trifluoroacetate concentrates in the liver, with a liver-to-Harderian gland ratio of 21 compared with 1.5 for a systemically distributed compound. Oral dosing in mice, rats, dogs and rhesus monkeys shows distribution mainly to the liver with low exposure in tissues linked to adverse events, giving liver-to-skin ratios greater than 30:1 in all four species. In eDIO mice, it improves glucose clearance before a glucose challenge in a dose-dependent manner, with an ED\u003csub\u003e50\u003c\/sub\u003e of 7 mg\/kg. It is supplied as a light yellow to yellow solid (C19H17BrF4N6O6, MW 581.27) at 98.45% purity.\u003c\/p\u003e\n\u003ch2\u003ePhysical \u0026amp; Chemical Properties\u003c\/h2\u003e\n\u003ctable class=\"bhp-spec-table\"\u003e\u003ctbody\u003e\n\u003ctr\u003e\n\u003cth\u003eCAS Number\u003c\/th\u003e\n\u003ctd\u003e1415559-41-9\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eMolecular Formula\u003c\/th\u003e\n\u003ctd\u003eC19H17BrF4N6O6\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eMolecular Weight\u003c\/th\u003e\n\u003ctd\u003e581.27 g\/mol\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003ePurity\u003c\/th\u003e\n\u003ctd\u003e98.45%\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eAppearance\u003c\/th\u003e\n\u003ctd\u003eSolid\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eColor\u003c\/th\u003e\n\u003ctd\u003eLight yellow to yellow\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eSMILES\u003c\/th\u003e\n\u003ctd\u003eO=C(CN1N=C(N=N1)C2=CC(N3CCC(CC3)OC4=CC(F)=CC=C4Br)=NO2)O.FC(C(O)=O)(F)F\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eSignaling Pathway\u003c\/th\u003e\n\u003ctd\u003eMetabolic Enzyme\/Protease\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eStorage\u003c\/th\u003e\n\u003ctd\u003e4°C, sealed storage, away from moisture. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture).\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eShipping\u003c\/th\u003e\n\u003ctd\u003eRoom temperature in continental US; may vary elsewhere.\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003c\/tbody\u003e\u003c\/table\u003e\n\u003ch2\u003eLiterature Cited\u003c\/h2\u003e\n\u003cp style=\"font-size:14px;color:#555;margin:0 0 10px\"\u003e\u003cem\u003eSources cited in this description. Peer-reviewed publications that used this product are listed under References.\u003c\/em\u003e\u003c\/p\u003e\n\u003cp\u003e [1]. \u003ca target=\"_blank\" rel=\"noopener\" href=\"http:\/\/www.ncbi.nlm.nih.gov\/pubmed\/21661758\"\u003eOballa RM, et al. Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia. J Med Chem. 2011 Jul 28;54(14):5082-96. Epub 2011 Jun 28.\u003c\/a\u003e\u003c\/p\u003e\n\u003ch2\u003eSafety\u003c\/h2\u003e\n\u003cdiv class=\"bhp-warning-box\"\u003e\u003cp\u003e\u003cstrong\u003eFor Research Use Only.\u003c\/strong\u003e Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.\u003c\/p\u003e\u003c\/div\u003e\n\u003c\/div\u003e","brand":"MedChemExpress (MCE)","offers":[{"title":"1 mg","offer_id":67604880654701,"sku":"HY-13077-1MG","price":84.0,"currency_code":"USD","in_stock":true},{"title":"5 mg","offer_id":67605135655277,"sku":"HY-13077-5MG","price":0.0,"currency_code":"USD","in_stock":true},{"title":"10 mg","offer_id":67605135688045,"sku":"HY-13077-10MG","price":0.0,"currency_code":"USD","in_stock":true}],"thumbnail_url":"\/\/cdn.shopify.com\/s\/files\/1\/0949\/7424\/7277\/files\/hy-13077.gif?v=1790972934","url":"https:\/\/www.ebiohippo.com\/products\/mk-8245-trifluoroacetate-bhb21900766","provider":"BioHippo","version":"1.0","type":"link"}