3-Piperidinecarboxamide, N-(4-chlorophenyl)-5,5-difluoro-1-[3-(2-furanyl)benzoyl]-
3-Piperidinecarboxamide, N-(4-chlorophenyl)-5,5-difluoro-1-[3-(2-furanyl)benzoyl]- Basic information
- Product Name:
- 3-Piperidinecarboxamide, N-(4-chlorophenyl)-5,5-difluoro-1-[3-(2-furanyl)benzoyl]-
- Synonyms:
-
- 3-Piperidinecarboxamide, N-(4-chlorophenyl)-5,5-difluoro-1-[3-(2-furanyl)benzoyl]-
- Rho-associated kinase,CCG222740,Rho-kinase,Rho,CCG-222740,CCG 222740,Inhibitor,inhibit,muscle,actin,factor,MRTF,transcription,ROK,metastasis,protein,Rho-associated protein kinase,myocardin-related,fibrosis,Ras,melanoma,orally,expression,ROCK,alpha-smooth
- N-(4-Chlorophenyl)-5,5-difluoro-1-(3-(furan-2-yl)benzoyl)piperidine-3-carboxamide
- CCG-222740, 10 mM in DMSO
- CCG-222740 ，S6673
- CAS:
- 1922098-69-8
- MF:
- C23H19ClF2N2O3
- MW:
- 444.86
- Mol File:
- 1922098-69-8.mol
3-Piperidinecarboxamide, N-(4-chlorophenyl)-5,5-difluoro-1-[3-(2-furanyl)benzoyl]- Chemical Properties
- Boiling point:
- 657.1±55.0 °C(Predicted)
- Density
- 1.40±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:107.0(Max Conc. mg/mL);240.52(Max Conc. mM)
Ethanol:89.0(Max Conc. mg/mL);200.06(Max Conc. mM) - form
- Solid
- pka
- 13.69±0.70(Predicted)
- color
- Light yellow to yellow
3-Piperidinecarboxamide, N-(4-chlorophenyl)-5,5-difluoro-1-[3-(2-furanyl)benzoyl]- Usage And Synthesis
Uses
CCG-222740 is an orally active and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor[1]. CCG-222740 is also a potent inhibitor of alpha-smooth muscle actin protein expression. CCG-222740 effectively reduces fibrosis in skin and blocks melanoma metastasis[2].
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[1].
| Animal Model: | KC mice (LSL-KrasG12D/+; Pdx-1-Cre) of age at 9 weeks[1] |
| Dosage: | 100?mg/kg |
| Administration: | Oral gavage; daily; for 7 days |
| Result: | Reduced α-SMA levels in the pancreas of caerulein-stimulated KC mice. |
References
[1] Leal AS, 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. DOI:10.1038/s41598-019-43430-0
[2] Yu-Wai-Man C, 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. DOI:10.1038/s41598-017-00212-w
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