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CCG-222740
Axon 3069
CAS:
1922098-69-8
Purity:
98%
- Soluble in DMSO
- MF: C23H19ClF2N2O3
- MW: 444.86
Description
CCG-222740 is a potent and selective second-generation MRTF/SRF inhibitor with an IC50 value of 5 μM in a fibroblast-mediated collagen contraction assay. CCG-222740 is more potent at preventing alpha-smooth muscle actin protein expression, is less cytotoxic, and effectively prevents scar tissue formation in a preclinical model of fibrosis (vs CCG-203971).
More Information
| Parent CAS No. | 1922098-69-8 |
|---|---|
| Chemical Name | N-(4-Chlorophenyl)-5,5-difluoro-1-(3-(furan-2-yl)benzoyl)piperidine-3-carboxamide |
| SMILES | C1(C2=CC=CO2)C=C(C(N2CC(C(=O)NC3C=CC(Cl)=CC=3)CC(F)(F)C2)=O)C=CC=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C23H19ClF2N2O3/c24-18-6-8-19(9-7-18)27-21(29)17-12-23(25,26)14-28(13-17)22(30)16-4-1-3-15(11-16)20-5-2-10-31-20/h1-11,17H,12-14H2,(H,27,29) |
| InChiKey | PMTPYUTZAJWGPE-UHFFFAOYSA-N |
| CID | 121317937 |
| Short Description | Rho/MRTF/SRF inhibitor |
References
- AS Leal 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.
- AD Tagalakis et al. In vitro and in vivo delivery of a sustained release nanocarrier-based formulation of an MRTF/SRF inhibitor in conjunctival fibrosis. J Nanobiotechnology. 2018 Nov 27;16(1):97.
- C Yu-Wai-Man 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.
- KM Hutchings et al. Pharmacokinetic optimitzation of CCG-203971: Novel inhibitors of the Rho/MRTF/SRF transcriptional pathway as potential antifibrotic therapeutics for systemic scleroderma. Bioorg Med Chem Lett. 2017 Apr 15;27(8):1744-1749.
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