{"product_id":"m19873","title":"Seladelpar","description":"\u003cp style=\"padding-left:1em;\"\u003eSeladelpar (MBX-8025) is an orally active, potent (50% effect concentration EC50 2 nM), and specific PPAR-δ agonist.\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eProduct information\u003c\/strong\u003e\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eCAS Number:\u003c\/strong\u003e 851528-79-5\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eMolecular Weight:\u003c\/strong\u003e 444.46\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eFormula:\u003c\/strong\u003e C21H23F3O5S\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eChemical Name:\u003c\/strong\u003e 2-(4-{[(2R)-2-ethoxy-3-[4-(trifluoromethyl)phenoxy]propyl]sulfanyl}-2-methylphenoxy)acetic acid\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eSmiles:\u003c\/strong\u003e CC1=CC(=CC=C1OCC(O)=O)SC[C@@H](COC1C=CC(=CC=1)C(F)(F)F)OCC\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eInChiKey:\u003c\/strong\u003e JWHYSEDOYMYMNM-QGZVFWFLSA-N\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eInChi:\u003c\/strong\u003e InChI=1S\/C21H23F3O5S\/c1-3-27-17(11-28-16-6-4-15(5-7-16)21(22,23)24)13-30-18-8-9-19(14(2)10-18)29-12-20(25)26\/h4-10,17H,3,11-13H2,1-2H3,(H,25,26)\/t17-\/m1\/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\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;\"\u003eSeladelpar (MBX-8025) is an orally active, potent (2 nM), and specific (\u0026gt;750-fold and \u0026gt;2500-fold compared with PPAR-α or PPAR-γ receptors, respectively) PPAR-δ agonist being developed as a lipid-altering agent. Seladelpar is a potent, and selective PPAR-δ agonist (50% effect concentration human PPAR-δ=2 nM, PPAR-α=1,600 nM) that demonstrates favorable effects on insulin resistance, diabetes, and atherogenic dyslipidemia.\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eIn Vivo:\u003c\/strong\u003e\u003c\/p\u003e\u003cp style=\"padding-left:1em;\"\u003eFrom weaning, female Alms1 mutant (foz\/foz) mice and wild-type littermates are fed an atherogenic diet for 16 weeks; groups (n=8-12) are then randomized to receive Seladelpar (10 mg\/kg) or vehicle (1% methylcellulose) by gavage for 8 weeks. Despite minimally altering body weight, Seladelpar normalizes hyperglycemia, hyperinsulinemia, and glucose disposal in foz\/foz mice. Serum alanine aminotransferase ranges 300-600 U\/L in vehicle-treated foz\/foz mice; Seladelpar reduces alanine aminotransferase by 50%. In addition, Seladelpar normalizes serum lipids and hepatic levels of free cholesterol and other lipotoxic lipids that are increased in vehicle-treated foz\/foz versus wild-type mice. This abolished hepatocyte ballooning and apoptosis, substantially reduce steatosis and liver inflammation, and improve liver fibrosis. In vehicle-treated foz\/foz mice, the mean nonalcoholic fatty liver disease activity score is 6.9, indicating nonalcoholic steatohepatitis (NASH); Seladelpar reverses NASH in all foz\/foz mice (nonalcoholic fatty liver disease activity score 3.13). In atherogenic diet-fed Wt mice, administration of Seladelpar reduces body weight by ∼18% (P\u0026lt;0.05). In contrast, Seladelpar produces minimal effect on body weight in atherogenic diet–fed foz\/foz mice. These animals develope severe hyperglycemia, hyperinsulinemia, and whole-body insulin resistance after 16 weeks (P\u0026lt;0.05); Seladelpar strikingly improves these indices (P\u0026lt;0.05). After intraperitoneal glucose injection, blood glucose reaches ~32 mM in vehicle-treated versus ~14 mM in Seladelpar-treated foz\/foz mice (P\u0026lt;0.05); the area under the blood glucose disappearance curve is correspondingly lower in Seladelpar-treated foz\/foz mice (P\u0026lt;0.05). Seladelpar produces a proportionally similar effect on glucose handling in atherogenic diet–fed Wt mice (P\u0026lt;0.05).\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eProducts are for research use only. Not for human use.\u003c\/strong\u003e\u003c\/p\u003e","brand":"Xcess Biosciences","offers":[{"title":"M19873-C \/ Contact sales@xcessbio.com for quotation","offer_id":39524037558411,"sku":"0","price":100.0,"currency_code":"USD","in_stock":false}],"thumbnail_url":"\/\/cdn.shopify.com\/s\/files\/1\/0389\/1897\/9723\/products\/M19873_1635191616.gif?v=1635191617","url":"https:\/\/www.xcessbio.com\/products\/m19873","provider":"Xcess Biosciences","version":"1.0","type":"link"}