PF-04634817 succinate

目录号: GC39501纯度: >98%
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。

PF-04634817 succinate
Cas No.: 2140301-98-8
规格价格库存数量操作
1mg¥1,053.00现货
1
5mg¥2,795.00现货
1
10mg¥4,455.00现货
1

文献被引

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产品描述 Description

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.

产品文档 Product Documents

化学性质Chemical Properties

CAS 号
2140301-98-8
SMILES
O=C(N1[C@@]2([H])C[C@@]([H])(C1)N(C3=NC=NC(C(F)(F)F)=C3)C2)[C@@]4(C[C@@H](CC4)N[C@@H]5[C@@H](COCC5)OC)C(C)C.OC(CCC(O)=O)=O
分子式
C29H42F3N5O7
分子量
629.67 g/mol
溶解性
Soluble in DMSO
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol