CCG-100602|cas:1207113-88-9|西域试剂

CCG-100602,99.66%

产品编号：Bellancom-120855| CAS NO：1207113-88-9| 分子式：C₂₁H₁₇ClF₆N₂O₂| 分子量：478.82

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货号	价格	库存与货期
Bellancom-120855	￥600.00	杭州北京（现货）
Bellancom-120855	￥1300.00	杭州北京（现货）
Bellancom-120855	￥2200.00	杭州北京（现货）
Bellancom-120855	￥3500.00	杭州北京（现货）

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CCG-100602

产品介绍

CCG-100602 是心肌蛋白相关转录因子 A/血清反应因子 (MRTF-A/SRF) 信号转导的特异性抑制剂。CCG-100602 特异性阻断 MRTF-A 核定位，从而抑制纤维生成转录因子 SRF。

生物活性

CCG-100602 is a specific inhibitor of myocardin-related transcription factor A/serum response factor (MRTF-A/SRF) signaling. CCG-100602 specifically block MRTF-A nuclear localization and thus inhibit the fibrogenic transcription factor SRF.

体外研究

CCG-100602 (3-30 μM) decreases the number of adherent hASC cells.
CCG-100602 blocks the expression of MRTF-A/SRF-activated genes.
CCG-100602 (5-40 μM) diminishes the TGF-β1 (5 ng/mL)-induced increase in COL1A1, FN1, and ACTA2 transcription in a dose-dependent manner.
CCG-100602 (5-40 μM) reduces the TGF-β1-induced increase in MRTFA and SRF mRNA expression in the HIMFs in a dose-dependent manner .
CCG-100602 (5-40 μM) significantly reduces the protein expression levels of the ECM and α-SMA in TGF-β1 (5 ng/mL)-stimulated cells in a dose-dependent manner.
CCG-100602 (5-40 μM) also significantly represses the MRTF-A and SRF protein expression, which were induced by TGF-β1, in the nuclear fraction of the HIMFs in a dose-responsive manner.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	Human adipose stem cell (hASC)
Concentration:	3, 8, 15, or 30 μM
Incubation Time:	7 days
Result:	The number of adherent cells decreased as a response to increasing inhibitor amount. The effect was also dependent on the culture media because the osteogenic medium condition supported the viability over basic culture medium and adipogenic medium conditions.

RT-PCR

Cell Line:	Human intestinal myofibroblasts (HIMFs)
Concentration:	5, 10, 20, and 40 μM
Incubation Time:	30 min prior to the addition of TGF-β1 (5 ng/mL) for 24 hours
Result:	Diminished the TGF-β1-induced increase in COL1A1, FN1, and ACTA2 transcription in a dose-dependent manner. Reduced the TGF-β1-induced increase in MRTFA and SRF mRNA expression in the HIMFs in a dose-dependent manner.

Western Blot Analysis

Cell Line:	Human intestinal myofibroblasts (HIMFs)
Concentration:	5, 10, 20, and 40 μM
Incubation Time:	30 min prior to the addition of TGF-β1 (5 ng/mL) for 48 hours
Result:	The protein expression levels of the ECM and α-SMA in TGF-β1-stimulated cells are significantly reduced. Repressed the MRTF-A and serum response factor (SRF) protein expression, which were induced by TGF-β1, in the nuclear fraction of the HIMFs.

体内研究
(In Vivo)

Treatment with CCG-100602 (7.5 mg/kg/day, continuously administered for 2 weeks by osmotic minipumps) abrogates the increase of aortic stiffness represented by reduced arterial compliance and strain, indicating a significant anti-stiffening effect resulting from the inhibition of SRF/myocardin.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Adult (4 month-old) male spontaneously hypertensive rats (SHR) and normotensive control Wistar-Kyoto (WKY) rats
Dosage:	7.5 mg/kg/day
Administration:	Continuously administered for 2 weeks by osmotic minipumps.
Result:	Abrogated the increase of aortic stiffness represented by reduced arterial compliance and strain.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Adult (4 month-old) male spontaneously hypertensive rats (SHR) and normotensive control Wistar-Kyoto (WKY) rats
Dosage:	7.5 mg/kg/day
Administration:	Continuously administered for 2 weeks by osmotic minipumps.
Result:	Abrogated the increase of aortic stiffness represented by reduced arterial compliance and strain.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Adult (4 month-old) male spontaneously hypertensive rats (SHR) and normotensive control Wistar-Kyoto (WKY) rats
Dosage:	7.5 mg/kg/day
Administration:	Continuously administered for 2 weeks by osmotic minipumps.
Result:	Abrogated the increase of aortic stiffness represented by reduced arterial compliance and strain.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (208.85 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0885 mL	10.4423 mL	20.8847 mL
5 mM	0.4177 mL	2.0885 mL	4.1769 mL
10 mM	0.2088 mL	1.0442 mL	2.0885 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制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

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 0.83 mg/mL (1.73 mM); Clear solution

此方案可获得 ≥ 0.83 mg/mL (1.73 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 0.83 mg/mL (1.73 mM); Clear solution

此方案可获得 ≥ 0.83 mg/mL (1.73 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。