CWHM-12 is a small molecule inhibitor of αV integrins with IC50s of 1.8/0.8/1.5/0.2 nM for αvβ1/αvβ3/αvβ8, and is less potency on αvβ5 (IC50=61 nM) and on inhibition on αIIbβ3/α2β1/α10β1.
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产品名称 | Integrin ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Tirofiban | ✔ | 99%+ | |||||||||||||||||
ATN-161 | ✔ | 98% | |||||||||||||||||
RGD | ✔ | 98% | |||||||||||||||||
A-205804 |
++
E-selectin, IC50: 20 nM ICAM-1, IC50: 25 nM |
98% | |||||||||||||||||
SB-273005 |
++++
αvβ3 receptor, IC50: 1.2 nM αvβ5 receptor, IC50: 0.3 nM |
98+% | |||||||||||||||||
Lifitegrast | ✔ | 97% | |||||||||||||||||
Cilengitide TFA |
+++
αvβ3 receptor, IC50: 4.1 nM αvβ5 receptor, IC50: 79 nM |
99%+ | |||||||||||||||||
Cyclo(-RGDfK) TFA | ✔ | 99%+ | |||||||||||||||||
Cyclo(RGDyK) trifluoroacetate |
++
αVβ3 integrin, IC50: 20 nM |
99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | CWHM-12 exhibits selective inhibition towards a range of integrins, demonstrating significant potency against αvβ1, αvβ3, αvβ6, and αvβ8 in vitro ligand-binding assays. It shows a reduced potency against αvβ5 with an IC50 value of 61 nM, while showing much less effectiveness against αIIbβ3, α2β1, and α10β1, where the IC50 values exceed 5000 nM. This highlights CWHM-12's targeted inhibitory action mainly towards the αv integrin family[1]. |
Animal study | In experimental models, mice subjected to CCl4 treatment for three weeks to induce fibrotic disease, followed by administration of CWHM-12 or a control vehicle during the last three weeks of CCl4 exposure, show that CWHM-12 significantly mitigates liver fibrosis. This reversal of fibrosis is partly attributed to the reduced activation of TGF-β by αv integrins, as evidenced by decreased p-SMAD3 signaling in the livers of CWHM-12-treated mice[1]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
1.69mL 0.34mL 0.17mL |
8.47mL 1.69mL 0.85mL |
16.94mL 3.39mL 1.69mL |
CAS号 | 1564286-55-0 |
分子式 | C26H32BrN5O6 |
分子量 | 590.47 |
SMILES Code | O=C(O)C[C@@H](C1=CC(C(C)(C)C)=CC(Br)=C1)NC(CNC(C2=CC(NC3=NCC(O)CN3)=CC(O)=C2)=O)=O |
MDL No. | MFCD28385850 |
别名 | |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place, sealed in dry, 2-8°C |
溶解方案 |
请根据您的动物给药指南选择适当的溶解方案。 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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