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CWHM-12

产品编号 TQ0250 CAS 1564286-55-0

CWHM-12 是 αV 整合素的有效抑制剂，抑制αvβ8、αvβ3、αvβ6和αvβ1，IC50 为 0.2、0.8、1.5 和 1.8 nM。

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CWHM-12, CAS 1564286-55-0

规格	价格/CNY	货期
1 mg	￥ 559	现货
2 mg	￥ 775	现货
5 mg	￥ 969	现货
10 mg	￥ 1,570	现货
25 mg	￥ 2,970	现货
50 mg	￥ 4,390	现货
100 mg	￥ 6,280	现货
1 mL * 10 mM (in DMSO)	￥ 1,280	现货

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纯度: 98.25%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	CWHM-12 is a potent inhibitor of αV integrins (IC50s of 0.2/0.8/1.5/1.8 nM for αvβ8/αvβ3/αvβ6/αvβ1).
靶点活性	αvβ8 integrin:0.2 nM, αvβ1 integrin:1.8 nM, αvβ5 integrin:61 nM, αvβ6 integrin:1.5 nM, αvβ3 integrin:0.8 nM
体外活性	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.
体内活性	Mice are treated with CCl4 for 3 weeks to establish fibrotic disease and then treated with CWHM-12 or vehicle for the final 3 weeks of CCl4. CWHM-12 significantly reduces liver fibrosis even after the fibrotic disease has been established. Digital image quantitation demonstrates significantly reduced p-SMAD3 signaling in the livers of CWHM-12 treated mice compared 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, the administration of CWHM-12 significantly inhibited the progression of pulmonary fibrosis.
激酶实验	Functions of integrins αvβ1, αvβ8, α2β1, and α10β1 are measured using cell-free receptor-ligand interaction assays using purified recombinant human integrins. Ligands used are human fibronectin for αvβ1, human LAP for αvβ8, bovine collagen II for α2β1, and murine laminin I for α10β1. 96-well plates are coated with the predetermined optimal concentration of ligand overnight, washed 3X with TBS+++ (25 mM Tris pH7.4, 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1 mM MnCl2, 1mM CaCl2), and blocked with TBS+++/1%BSA. Purified integrin is diluted in TBS+++/0.1%BSA with or without compounds (e.g., CWHM-12), and the solution added to empty wells of the washed ligand-coated plate according to a standard template, with each sample repeated in triplicate. After incubation for 2 hr at room temperature, the plate is washed 3X with TBS+++. Biotin-labeled antibody against the αv subunit (αvβ1, αvβ8 assays) or β1 subunit (α2β1, α10β1 assays) is applied for 1 hr. The plate is washed 3X with TBS/0.1%BSA. Streptavidin-conjugated horseradish peroxidase is added to the wells, and the plate incubated for 20 min at room temperature. Following a 3X TBS+++ wash, bound integrin is detected using streptavidin-conjugated horseradish peroxidase and TMB substrate with absorbance measured at 650 nm. For assay of αIIbβ3 (IIbIIIa) function, plates are coated with the purified human integrin overnight, washed 3X with TBS+++, and blocked with TBS+++/1%BSA. Alexa Fluor647-labeled purified human fibrinogen is diluted in TBS+++/0.1%BSA with or without compounds, and the solutions are added to the integrin-coated plate. After 2 hr incubation, the plate is washed 3X with TBS+++, and the bound ligand is detected by absorbance measured at 640/668nm. For all assays, concentration-response curves are constructed by non-linear regression analysis and IC50 values are calculated using GraphPad Prism software.
细胞实验	The stably transfected human 293 cells over-expressing human αvβ3 or αvβ5 are pre-incubated in HBSS buffer containing 200 μM MnCl2 for 30 min at 37°C with 3-fold dilutions of compound (e.g., CWHM-12). Each sample is then added to triplicate wells of a 96-well plate which has been coated overnight at 4°C with a predetermined optimal concentration of purified vitronectin, washed, blocked by 1 hr incubation with BSA, and washed again. Cells are allowed to attach for 30 min at 37°C, and non-adherent cells are removed by washing. Remaining attached cells are measured by endogenous alkaline phosphatase activity using para-nitrophenyl phosphate and reading absorbance signal at 405 nM. The same procedure is used to measure adhesion of αvβ6-expressing human HT-29 cells to purified human latency-associated peptide, and α5β1-expressing human K562 cells to human plasma fibronectin. In all cell-based assays, binding by the expected integrin is verified by the testing activity of corresponding isotype-matched positive (function-blocking) and negative control antibodies.
动物实验	The mTmG (Td tomato/EGFP) and Ai14 (Rosa-CAG-LSL-tdTomato-WPRE) mice are used and crossed with Pdgfrb-Cre mice. Wild type C57/BL6 mice, Itgavflox/flox mice, and itgb8flox/flox mice are used. Mice used for all experiments are 8-12 weeks old and are housed under specific pathogen-free conditions. For all studies, CWHM-12 and CWHM-96 are solubilized in 50% DMSO (in sterile water) and dosed to 100 mg/kg/day. Drug or vehicle (50% DMSO) is delivered by implantable ALZET osmotic minipumps. For CCl4-induced fibrosis, pumps are inserted subcutaneously either before the first dose of CCl4 (prophylactic) or after 3 weeks of treatment (therapeutic) and livers are harvested after 6 weeks. For Bleomycin-induced fibrosis pumps are inserted 14 days after treatment with Bleomycin or saline and lungs are harvested at 28 days.

分子量	590.47
分子式	C26H32BrN5O6
CAS No.	1564286-55-0

存储

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

溶解度

DMSO: 10 mg/mL (16.93 mM), Sonification and heating are 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	1.6936 mL	8.4678 mL	16.9357 mL	42.3392 mL
	5 mM	0.3387 mL	1.6936 mL	3.3871 mL	8.4678 mL
	10 mM	0.1694 mL	0.8468 mL	1.6936 mL	4.2339 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

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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.

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。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

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。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

CWHM-12 1564286-55-0 Cytoskeletal Signaling Integrin CWHM 12 Inhibitor CWHM12 inhibit inhibitor

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CWHM-12

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords