货号	规格	价格	上海	北京	珠海	重庆	武汉
S83597-2mg买3赠1	98.00%	￥420.00 S83597-2mg ￥420.00 现货（买3赠1）	8 8	-	-	-	-
S83597-5mg促销	98.00%	￥630.00 ￥504.00 S83597-5mg ￥504.00 现货	10 10	-	-	-	-
S83597-10mg促销	98.00%	￥950.00 ￥760.00 S83597-10mg ￥760.00 现货	10 10	-	-	-	-
S83597-50mg促销	≥98%	￥3240.00 ￥2590.00 S83597-50mg ￥2590.00 2-3天	0 货期：2-3天	-	-	-	-
S83597-100mg促销	≥98%	￥5510.00 ￥4950.00 S83597-100mg ￥4950.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

CWHM-12 is a potent inhibitor of αV integrins with IC50s of 0.2, 0.8, 1.5, and 1.8 nM for αvβ8, αvβ3, αvβ6, and αvβ1.

靶点：

IC50: 0.2 nM (αvβ8), 0.8 nM (αvβ3), 1.5 nM (αvβ6), 1.8 nM (αvβ1), 61 nM (αvβ5);Integrin

体外研究：

CWHM-12 (CWHM 12) also less potently inhibits αvβ5 (IC50=61 nM) and αIIbβ3/α2β1/α10β1 (IC50>5000 nM). CWHM-12 demonstrates high potency against all of the five possible β subunit binding partners (αvβ1, αvβ3, αvβ5, αvβ6 and αvβ8) in in vitro ligand-binding assays, with somewhat less potency against αvβ5 than against the other αv integrins

体内研究：

Mice are treated with CCl4 for 3 weeks to establish fibrotic disease and then treated with CWHM-12 (CWHM 12) or vehicle for the final 3 weeks of CCl4. CWHM-12 significantly reduces liver fibrosis even after fibrotic disease have been established. Digital image quantitation demonstrates significantly reduced p-SMAD3 signaling in the livers of CWHM-12 treated mice compare to controls, demonstrating that the protection from CCl4-induced hepatic fibrosis observed in CWHM-12 treated mice is due at least in part to a reduction in TGF-β activation by αv integrins. Besides, administration of CWHM-12 significantly inhibited progression of pulmonary fibrosis

参考文献：

1. Henderson NC, et al. Targeting of αv integrin identifies a core molecular pathway that regulates fibrosis in several organs. Nat Med. 2013 Dec;19(12):1617-24. 2. Basta J, Robbins L, Stout L, Prinsen MJ, Griggs DW, Rauchman M. Pharmacologic inhibition of RGD-binding integrins ameliorates fibrosis and improves function following kidney injury. Physiol Rep. 2020;8(7):e14329

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.694 ml	8.468 ml	16.936 ml
5 mM	0.339 ml	1.694 ml	3.387 ml
10 mM	0.169 ml	0.847 ml	1.694 ml
50 mM	0.034 ml	0.169 ml	0.339 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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