Description
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.
Product information
CAS Number: 1207113-88-9
Molecular Weight: 478.82
Formula: C21H17ClF6N2O2
Chemical Name: 1-[3, 5-bis(trifluoromethyl)benzoyl]-N-(4-chlorophenyl)piperidine-3-carboxamide
Smiles: O=C(C1C=C(C=C(C=1)C(F)(F)F)C(F)(F)F)N1CC(CCC1)C(=O)NC1C=CC(Cl)=CC=1
InChiKey: MOQCFMZWVKQBAP-UHFFFAOYSA-N
InChi: InChI=1S/C21H17ClF6N2O2/c22-16-3-5-17(6-4-16)29-18(31)12-2-1-7-30(11-12)19(32)13-8-14(20(23,24)25)10-15(9-13)21(26,27)28/h3-6,8-10,12H,1-2,7,11H2,(H,29,31)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 100 mg/mL (208.85 mM; Need ultrasonic).
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-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.
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.
Products are for research use only. Not for human use.
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