AC 261066 - CAS 870773-76-5
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
AC 261066 is a potent RARβ2 agonist (pEC50 = 8.1).
Brife Description:
RARβ2 agonist
≥98% by HPLC
AC261066; AC 261066; AC-261066; 4-[4-(2-Butoxyethoxy-)-5-methyl-2-thiazolyl]-2-fluorobenzoic acid
Canonical SMILES:
1.Discovery of a potent, orally available, and isoform-selective retinoic acid beta2 receptor agonist.
Lund BW;Piu F;Gauthier NK;Eeg A;Currier E;Sherbukhin V;Brann MR;Hacksell U;Olsson R J Med Chem. 2005 Dec 1;48(24):7517-9.
4'-Octyl-4-biphenylcarboxylic acid (1g, AC-55649) was identified as a highly isoform-selective agonist at the human RARbeta2 receptor in a functional intact cell-based screening assay. The subsequent hit to lead optimization transformed the lipophilic, poorly soluble hit into a more potent and orally available compound (2, AC-261066) with retained beta2 selectivity and greatly improved physiochemical properties. Being an isoform-selective RARbeta2 receptor agonist that discriminates between nuclear receptor isoforms having identical ligand binding domains, 2 will be useful as a pharmacological research tool but also a valuable starting point for drug development.
2.A Retinoic Acid
Marino A;Sakamoto T;Tang XH;Gudas LJ;Levi R J Pharmacol Exp Ther. 2018 Aug;366(2):314-321. doi: 10.1124/jpet.118.250605. Epub 2018 Jun 15.
We previously discovered that oral treatment with AC261066, a synthetic selective agonist for the retinoic acid ;β;2;-receptor, decreases oxidative stress in the liver, pancreas, and kidney of mice fed a high-fat diet (HFD). Since hyperlipidemic states are causally associated with myocardial ischemia and oxidative stress, we have now investigated the effects of AC261066 in an ex vivo ischemia/reperfusion (I/R) injury model in hearts of two prototypic dysmetabolic mice. We found that a 6-week oral treatment with AC261066 in both genetically hypercholesterolemic (ApoE;-/-;) and obese (HFD-fed) wild-type mice exerts protective effects when their hearts are subsequently subjected to I/R ex vivo in the absence of added drug. In ApoE;-/-; mice this cardioprotection ensued without hyperlipidemic changes. Cardioprotection consisted of attenuation of infarct size, diminution of norepinephrine (NE) spillover, and alleviation of reperfusion arrhythmias. This cardioprotection was associated with a reduction in oxidative stress and mast cell (MC) degranulation. We suggest that the reduction in myocardial injury and adrenergic activation, and the antiarrhythmic effects, result from decreased formation of oxygen radicals and toxic aldehydes known to elicit the release of MC-derived renin, promoting the activation of the local renin-angiotensin system leading to enhanced NE release and reperfusion arrhythmias.
3.Amelioration of Diabetic Nephropathy Using a Retinoic Acid Receptor
Trasino SE;Tang XH;Shevchuk MM;Choi ME;Gudas LJ J Pharmacol Exp Ther. 2018 Oct;367(1):82-94. doi: 10.1124/jpet.118.249375. Epub 2018 Jul 27.
Vitamin A (VA) and its derivatives, known as retinoids, play critical roles in renal development through retinoic acid receptor ;β;2 (RAR;β;2). Disruptions in VA signaling pathways are associated with the onset of diabetic nephropathy (DN). Despite the known role of RAR;β;2 in renal development, the effects of selective agonists for RAR;β;2 in a high-fat diet (HFD) model of DN are unknown. Here we examined whether AC261066 (AC261), a highly selective agonist for RAR;β;2, exhibited therapeutic effects in a HFD model of DN in C57BL/6 mice. Twelve weeks of AC261 administration to HFD-fed mice was well tolerated with no observable side effects. Compared with HFD-fed mice, HFD + AC261-treated mice had improved glycemic control and reductions in proteinuria and urine albumin-to-creatinine ratio. Several cellular hallmarks of DN were mitigated in HFD + AC261-treated mice, including reductions in tubule lipid droplets, podocyte (POD) effacement, endothelial cell collapse, mesangial expansion, and glomerular basement membrane thickening. Mesangial and tubule interstitial expression of the myofibroblast markers ;α;-smooth muscle actin (;α;-SMA) and type IV collagen (Col-IV) was lower in HFD + AC261-treated mice compared with HFD alone.
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CAS 870773-76-5 AC 261066

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