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Chemical Structure| 1207113-88-9 Chemical Structure| 1207113-88-9

Structure of CCG-100602
CAS No.: 1207113-88-9

Chemical Structure| 1207113-88-9

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CCG-100602 is a selective MRTF-A/SRF signaling inhibitor that inhibits the activity of fibrogenic transcription factors by blocking the nuclear localization of MRTF-A, used in studies of fibrosis and related diseases.

Synonyms: CCG-100602

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Product Details of CCG-100602

CAS No. :1207113-88-9
Formula : C21H17ClF6N2O2
M.W : 478.81
SMILES Code : O=C(C1CN(C(C2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2)=O)CCC1)NC3=CC=C(Cl)C=C3
Synonyms :
CCG-100602

Safety of CCG-100602

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of CCG-100602

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
NIH3T3 cells 0.3 μM 24 h To evaluate the effect of CCG-100602 on MRTF-A/SRF-mediated transcriptional activity. Results showed that CCG-100602 significantly reduced SRF reporter activity. PLoS One. 2015 Aug 21;10(8):e0136242
Vascular Smooth Muscle Cells (VSMCs) 25 μM 24 h Inhibit SRF/myocardin signaling pathway and reduce VSMC stiffness Cardiovasc Res. 2017 Feb;113(2):171-182
human adipose stem cells (hASCs) 10 μM or 12 μM 7 days, 14 days, or 21 days To study the effect of MRTF-A inhibition on hASCs differentiation, results showed that MRTF-A inhibition enhanced adipogenesis and reduced osteogenesis. Stem Cells Int. 2020 Sep 22;2020:8853541
human colonic myofibroblasts (CCD-18co cells) 25 μM 48 h Inhibition of TGF-β-mediated MRTF-A nuclear translocation, reduction of MKL1 (MRTF-A) mRNA levels, significant repression of ACTA2 and col1A1 transcription and α SMA protein expression. Inflamm Bowel Dis. 2014 Jan;20(1):154-65.
human colonic myofibroblasts (CCD-18co cells) 25 μM 24 h Inhibition of matrix stiffness-induced actin stress fiber formation and MRTF-A nuclear translocation, reduction of MYLK and MKL1 (MRTF-A) mRNA levels, significant repression of ACTA2 and col1A1 transcription and α SMA protein expression. Inflamm Bowel Dis. 2014 Jan;20(1):154-65.
human primary intestinal myofibroblasts (HIMFs) 40 μmol/L 48 h CCG-100602 significantly reduced TGF-β1-induced COL1A1, FN1, ACTA2, MRTFA, and SRF mRNA expression and decreased the protein levels of Procol1A1, FN, α-SMA, MRTF-A, and SRF. Stem Cell Res Ther. 2019 Sep 23;10(1):291

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Spontaneously Hypertensive Rats (SHR) and Wistar-Kyoto (WKY) rats Spontaneously Hypertensive Rat model Subcutaneous osmotic pump 1.5 mg/kg Continuously for 2 weeks Evaluate the effect of CCG-100602 on aortic stiffness and blood pressure Cardiovasc Res. 2017 Feb;113(2):171-182

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.09mL

0.42mL

0.21mL

10.44mL

2.09mL

1.04mL

20.89mL

4.18mL

2.09mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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