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CXCR7 modulator 2

产品编号 T10907 CAS 2227426-37-9

CXCR7 modulator 2 is a 7-type C-X-C chemokine receptor (CXCR7) modulator with a Ki of 13 nM.

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CXCR7 modulator 2, CAS 2227426-37-9

规格	价格/CNY	货期
2 mg	￥ 3,290	5日内发货
5 mg	￥ 5,390	5日内发货
25 mg	￥ 18,900	10-14周
50 mg	￥ 24,600	10-14周
100 mg	￥ 39,500	10-14周
1 mL * 10 mM (in DMSO)	￥ 6,530	5日内发货

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	CXCR7 modulator 2 is a 7-type C-X-C chemokine receptor (CXCR7) modulator with a Ki of 13 nM.
靶点活性	CXCR7:13 nM (ki)
体外活性	CXCR7 modulator 2 showed strong CXCR7 binding affinity (Ki = 13 nM) and β-arrestin activity (EC50 = 11 nM). Compared with 11c, CXCR7 modulator 2 also showed improved selectivity in the GPCR panel and showed a higher therapeutic index in the hERG patch clamp assay. CXCR7 modulator 2 exhibited medium to high in vitro turnover in NADPH- supplemented mouse liver microsomes (MLM, 93 μL / min / mg) and hepatocytes (28 μL / min per million cells), which was shown to be more comparable in MDCK Poor passive absorption permeability type II permeability measurement method, and has good water solubility. CXCR7 regulator 2 is rapidly absorbed, with an average maximum plasma concentration (Cmax) of 682 ng / mL, which appears at 0.25 h (Tmax). The corresponding average area under the plasma concentration-time curve (AUC) is 740 ng / mL / h.
体内活性	The administration of isoproterenol for 9 days will lead to the development of cardiac fibrosis. This is because the amount of collagen deposition detected by Pixirius red staining has increased by about 4 times relative to that of the control group. proven. Treatment with CXCR7 modulator 2 can lead to a statistically significant reduction in cardiac fibrosis, thus demonstrating that CXCR7 modulator 2 has a protective effect on CXCR7 modulation in isoproterenol-induced cardiac injury.

分子量	522.68
分子式	C29H42N6O3
CAS No.	2227426-37-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 250 mg/mL (478.30 mM), Sonication is recommended.

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9132 mL	9.5661 mL	19.1322 mL	47.8304 mL
	5 mM	0.3826 mL	1.9132 mL	3.8264 mL	9.5661 mL
	10 mM	0.1913 mL	0.9566 mL	1.9132 mL	4.783 mL
	20 mM	0.0957 mL	0.4783 mL	0.9566 mL	2.3915 mL
	50 mM	0.0383 mL	0.1913 mL	0.3826 mL	0.9566 mL
	100 mM	0.0191 mL	0.0957 mL	0.1913 mL	0.4783 mL

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参考文献

1. Menhaji-Klotz E, et al. Discovery of a Novel Small-Molecule Modulator of C-X-C Chemokine Receptor Type 7 as a Treatment for Cardiac Fibrosis. J Med Chem. 2018 Apr 26;61(8):3685-3696.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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