CCG-222740
目录号: PL10881 纯度: ≥99%
CAS No. :1922098-69-8
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中文名称
CCG-222740
英文名称
CCG-222740
英文别名
N-(4-chlorophenyl)-5,5-difluoro-1-(3-(furan-2-yl)benzoyl)piperidine-3-carboxamide;PMTPYUTZAJWGPE-UHFFFAOYSA-N;s6673;N-(4-Chlorophenyl)-5,5-difluoro-1-[3-(furan-2-yl)benzoyl]piperidine-3-carboxamide;CCG-222740
Cas No.
1922098-69-8
分子式
C23H19ClF2N2O3
分子量
444.86
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
CCG-222740 是一种口服有效的,选择性 Rho/MRTF 途径抑制剂。CCG-222740 也是有效的 α-平滑肌肌动蛋白蛋白表达抑制剂。CCG-222740 有效减少皮肤纤维化并阻止黑色素瘤转移。
生物活性
CCG-222740 is an orally active and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor. CCG-222740 is also a potent inhibitor of alpha-smooth muscle actin protein expression. CCG-222740 effectively reduces fibrosis in skin and blocks melanoma metastasis.
性状
Solid
IC50 & Target[1][2]
Rho/MRTF pathway
体外研究(In Vitro)
CCG-222740 (10, 20 μM; for 72 hours) increases the protein levels of p27 and decreases cyclin D1. CCG-222740 decreases cell viability of CAFs, with an IC50 of ~10?μM.
CCG-222740 (10, 25 μM) is potent at decreasing αSMA protein expression in human conjunctival fibroblasts.
CCG-222740 has an IC50 of 5?μM in a fibroblast-mediated collagen contraction assay, and it is less cytotoxic.
has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
CCG-222740 (oral gavage; 100?mg/kg/day for 7 days) significantly reduces α-SMA levels in the pancreas of caerulein-stimulated KC mice.
has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Leal AS, et al. The Rho/MRTF pathway inhibitor CCG-222740 reduces stellate cell activation and modulates immune cell populations in KrasG12D; Pdx1-Cre (KC) mice. Sci Rep. 2019 May 8;9(1):7072.
[2]. Yu-Wai-Man C, et al. Local delivery of novel MRTF/SRF inhibitors prevents scar tissue formation in a preclinical model of fibrosis. Sci Rep. 2017 Mar 31;7(1):518.
溶解度数据
In Vitro: DMSO : 125 mg/mL (280.99 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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