CCG 203971

Product Description

CCG 203971 is an antifibrotic agent; inhibits fibrosis by targeting the MRTF/SRF gene transcription pathway. Selectively inhibits proliferation of SSc-derived dermal fibroblasts but not that of normal fibroblasts. Inhibits expression of CTGF, α-SMA, and COL1A2 in SSc fibroblasts as well as in LPA and in TGFβ-stimulated fibroblasts. Prevents bleomycin-induced skin thickening and collagen deposition in vivo. Also suppresses PC-3 cell migration in scratch wound assays (IC₅₀ = 4.2 μM).

Solubility

Preparing Stock Solutions for CCG 203971

The following data is based on the product molecular weight 408.88

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.5 mM	4.89 mL	24.46 mL	48.91 mL
2.5 mM	0.98 mL	4.89 mL	9.78 mL
5 mM	0.49 mL	2.45 mL	4.89 mL
25 mM	0.10 mL	0.49 mL	0.98 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Bell Optimization of novel nipecotic bis(amide) inhibitors of the Rho/MKL1/SRF transcriptional pathway as potential anti-metastasis agents. Bioorg.Med.Chem.Lett. 2013 PMID: 23707258
• Haak Targeting the myofibroblast genetic switch: inhibitors of myocardin-related transcription factor/serum response factor-regulated gene transcription prevent fibrosis in a murine model of skin injury. J.Pharmacol.Exp.Ther. 2014 PMID: 24706986
• Michel Hope for disease-modifying treatment of systemic sclerosis/scleroderma. J.Pharmacol.Exp.Ther. 2014 PMID: 25053235