PF-0463481 succinate 是一种有效的具有口服活性的双效 CCR2/CCR5 拮抗剂，对人和啮齿类动物的 CCR2 效价相当 (rat IC50=20.8 nM)，对 CCR2 的效价是 CCR5 的 10-20 倍 (rat IC50=470 nM)。PF-0463481 succinate 安全、耐受性好，有潜力用于研究糖尿病肾病。
货号:ajcx16744
CAS:2140301-98-8
分子式:C29H42F3N5O7
分子量：629.67
溶解度:Soluble in DMSO
纯度：98%
存储：Store at -20°C
库存：现货

Background:

PF-0463481 succinate is a potent and orally active dual CCR2/CCR5 antagonist with comparable human and rodent CCR2 potency (rat IC50=20.8 nM), and displays 10-20 fold less rodent CCR5 potency (rat IC50=470 nM). PF-0463481 succinate is safe and well-tolerated and has the potential for the study of diabetic nephropathy[3].

[1]. Tesch GH, et al. Combined inhibition of CCR2 and ACE provides added protection against progression of diabetic nephropathy in Nos3-deficient mice.Am J Physiol Renal Physiol. 2019 Dec 1;317(6):F1439-F1449. [2]. Gale JD, et al. A CCR2/5 Inhibitor, PF-04634817, Is Inferior to Monthly Ranibizumab in the Treatment of Diabetic Macular Edema. Invest Ophthalmol Vis Sci. 2018 May 1;59(6):2659-2669. [3]. Gale JD, et al. Effect of PF-04634817, an Oral CCR2/5 Chemokine Receptor Antagonist, on Albuminuria in Adults with Overt Diabetic Nephropathy. Kidney Int Rep. 2018 Aug 3;3(6):1316-1327.