CCG 203971

Modify Date: 2024-01-14 08:44:51

CCG 203971 Structure
CCG 203971 structure
Common Name CCG 203971
CAS Number 1443437-74-8 Molecular Weight 408.877
Density 1.3±0.1 g/cm3 Boiling Point 656.0±55.0 °C at 760 mmHg
Molecular Formula C23H21ClN2O3 Melting Point N/A
MSDS Chinese USA Flash Point 350.5±31.5 °C
Symbol GHS07
GHS07
Signal Word Warning

 Use of CCG 203971


CCG-203971 is a second-generation RhoA/myocardin-related transcription factor A (MRTF-A) inhibitor. CCG-203971 potently targets RhoA/C-activated serum response element (SRE)-luciferase (IC50=6.2 μM).

 Names

Name N-(4-chlorophenyl)-1-(3-(furan-2-yl)benzoyl)piperidine-3-carboxamide
Synonym More Synonyms

 CCG 203971 Biological Activity

Description CCG-203971 is a second-generation RhoA/myocardin-related transcription factor A (MRTF-A) inhibitor. CCG-203971 potently targets RhoA/C-activated serum response element (SRE)-luciferase (IC50=6.2 μM).
Related Catalog
Target

RhoA/MRTF-A[1]

In Vitro CCG-203971, a second-generation Ras homolog gene family, member A (RhoA)/myocardin-related transcription factor A (MRTF-A)/serum response factor (SRF) pathway inhibitor, represses both matrix-stiffness and transforming growth factor beta–mediated fibrogenesis as determined by protein and gene expression in a dose-dependent manner. CCG-203971 significantly represses TGF-β- induced MKL1 expression at 25 μM concentration[1]. Human dermal fibroblasts are plated onto 96-well plates and allowed to grow for 3 days in the presence of 30 μM CCG-203971 or DMSO vehicle. Viable cell density is assessed through enzymatic reduction of the water-soluble tetrazolium dye WST-1. Scleroderma dermal fibroblasts proliferate faster than normal cells, and this is inhibited by CCG-203971[2].
In Vivo CCG-203971 is tested in a Bleomycin skin injury model. Bleomycin is administered in 50 μL of DMSO intraperitoneally. Preliminary studies show that Bleomycin administered in this manner is well tolerated at 100 mg/kg twice a day. Intradermal Bleomycin for 2 weeks along with the DMSO control (50 μL i.p.) results in marked dermal thickening (P<0.0001) compared with the PBS+DMSO group, which does not receive Bleomycin. CCG-203971 treatment strongly and significantly (P<0.001) suppresses the Bleomycin-induced skin thickening in this model. Skin collagen amounts, assessed by measurement of hydroxyproline content, show similar results. Bleomycin injections promote collagen deposition (P<0.01) and CCG-203971 is able to block this effect (P<0.05)[2].
Cell Assay Human dermal fibroblasts (2.0×104) are plated into a 96-well plate and grown overnight in DMEM containing 10% FBS. Media are removed and replaced with DMEM containing 2% FBS and 30 μM CCG-203971 or 0.1% DMSO control. After 72 hours WST-1 dye is added to each well, and after 60 minutes absorbance at 490 nm is read using a Wallac Victor2 plate reader[2].
Animal Admin Mice[2] Skin fibrosis is induced in C57BL/6 mice (female, 8 weeks old) by local intracutaneous injection of 100 μL of Bleomycin (1 mg/mL) in phosphate-buffered saline (PBS), every day for 2 weeks in a defined area (~1 cm2) on the upper back. Intracutaneous injection of 100 μL of PBS is used as a control. Three groups of mice with a total of 21 mice are used. One group receives injections of PBS and the other two are challenged with Bleomycin. Twice-a-day intraperitoneal administration of CCG-203971 (100 mg/kg in 50 μL of DMSO) is initiated together with the first challenge of Bleomycin and continues for 2 weeks. DMSO is used as the vehicle control. The three groups of animals are: (1) PBS/DMSO; (2) Bleomycin/DMSO; and (3) Bleomycin/CCG-203971. After treatment, animals are humanely killed by cervical dislocation, and tissue is collected[2].
References

[1]. Johnson LA, et al. Novel Rho/MRTF/SRF inhibitors block matrix-stiffness and TGF-β-induced fibrogenesis in human colonic myofibroblasts. Inflamm Bowel Dis. 2014 Jan;20(1):154-65.

[2]. Haak AJ, et al. 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 Jun;349(3):480-6.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 656.0±55.0 °C at 760 mmHg
Molecular Formula C23H21ClN2O3
Molecular Weight 408.877
Flash Point 350.5±31.5 °C
Exact Mass 408.124084
PSA 62.55000
LogP 3.76
Vapour Pressure 0.0±2.0 mmHg at 25°C
Index of Refraction 1.633
Storage condition -20℃

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302
Precautionary Statements P301 + P312 + P330
RIDADR NONH for all modes of transport

 Synonyms

N-(4-Chlorophenyl)-1-[3-(2-furyl)benzoyl]-3-piperidinecarboxamide
3-Piperidinecarboxamide, N-(4-chlorophenyl)-1-[3-(2-furanyl)benzoyl]-
CCG-203971
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