货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
V56662-1ml	10mM in DMSO	￥1010.00 V56662-1ml ￥1010.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

V56662-1ml

10mM in DMSO

￥1010.00

货期：3-5天

产品描述：

C-021 is a potent CC chemokine receptor-4 (CCR4) antagonist. C-021 potently inhibits functional chemotaxis in human and mouse with IC50s of 140 nM and 39 nM, respectively. C-021 effectively prevents human CCL22-derived [35S]GTPγS from binding to the receptor with an IC50 of 18 nM

靶点：

CCR4;CCR

体外研究：

The in vitro oxidative metabolic stability of C-021 (Compound 1b) is evaluated by measuring the rate of drug consumption in human liver microsomes (HML), thus providing intrinsic clearance values (CLint). C-021 exhibits CLint value of 17,377 mL/h/kg.

体内研究：

The potency of C-021 (Compound 1b) is evident after subcutaneous administration in the murine oxazolone-induced contact hypersensitivity test, a known model of acute skin inflammation. When C-021 is administered orally, however, very little inhibition is observed.

C-021 (1 mg/kg; i.p.; daily; for 3 days) significantly less microgliosis in acute liver failuremice. Animal Model: Male C57Bl/6 mice (20-25 g) with acute liver failure Dosage: 1 mg/kg Administration: i.p.; daily; for 3 days Result: Significantly less microgliosis, and significantly reduced the pERK1/2 to tERK1/2 ratio.

参考文献：

1. Yokoyama K, et al. Potent and orally bioavailable CCR4 antagonists: Synthesis and structure-activity relationship study of 2-aminoquinazolines. Bioorg Med Chem. 2009 Jan 1;17(1):64-73.

2. Matthew McMillin, et al. Neuronal CCL2 is upregulated during hepatic encephalopathy and contributes to microglia activation and neurological decline. J Neuroinflammation. 2014 Jul 10;11:121.

溶解性：

Soluble in DMSO

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.138 ml	10.692 ml	21.384 ml
5 mM	0.428 ml	2.138 ml	4.277 ml
10 mM	0.214 ml	1.069 ml	2.138 ml
50 mM	0.043 ml	0.214 ml	0.428 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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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

质量

浓度

体积

分子摩尔量

计算重置

C-021

2-[1,4'-Bipiperidin]-1'-yl-N-cycloheptyl-6,7-dimethoxy-4-quinazolinaminedihydrochloride

参考文献

质检证书(COA)

如何获取质检证书(COA)?

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)