CCG-222740

CCG-222740 is a potent MRTF/SRF inhibitor. CCG-222740 markedly decreased SRF reporter gene activity and showed a greater inhibitory effect on MRTF/SRF target genes than the previously described MRTF-A inhibitor CCG-203971. CCG-222740 was also five times more potent, with an IC50 of 5 μM, in a fibroblast-mediated collagen contraction assay, was less cytotoxic, and a more potent inhibitor of alpha-smooth muscle actin protein expression than CCG-203971.

Product information

CAS Number: 1922098-69-8

Molecular Weight: 444.86

Formula: C23H19ClF2N2O3

Chemical Name: N-(4-chlorophenyl)-5,5-difluoro-1-(3-(furan-2-yl)benzoyl)piperidine-3-carboxamide

Smiles: O=C(C1=CC(=CC=C1)C1=CC=CO1)N1CC(CC(F)(F)C1)C(=O)NC1C=CC(Cl)=CC=1

InChiKey: PMTPYUTZAJWGPE-UHFFFAOYSA-N

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)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

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.

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.

References:

1. Tagalakis AD, Madaan S, Larsen SD, Neubig RR, Khaw PT, Rodrigues I, Goyal S,Lim KS, Yu-Wai-Man C. In vitro and in vivo delivery of a sustained releasenanocarrier-based formulation of an MRTF/SRF inhibitor in conjunctival fibrosis.J Nanobiotechnology. 2018 Nov 27;16(1):97. doi: 10.1186/s12951-018-0425-3. PubMed PMID: 30482196; PubMed Central PMCID: PMC6258153.
2. Yu-Wai-Man C, Spencer-Dene B, Lee RMH, Hutchings K, Lisabeth EM, Treisman R, Bailly M, Larsen SD, Neubig RR, Khaw PT. Local delivery of novel MRTF/SRFinhibitors prevents scar tissue formation in a preclinical model of fibrosis. SciRep. 2017 Mar 31;7(1):518. doi: 10.1038/s41598-017-00212-w. PubMed PMID:28364121; PubMed Central PMCID: PMC5428058.

Products are for research use only. Not for human use.