An inhibitor of the Rho/MRTF/SRF transcriptional pathway
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CCG-232601

Item No. 24382

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(4-chlorophenyl)-5,5-difluoro-1-[3-(4-pyridinyl)benzoyl]-3-piperidinecarboxamide
CAS Number
1922099-21-5
Molecular Formula
C24H20ClF2N3O2
Formula Weight
455.9
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml
λmax
250 nm
SMILES
O=C(N1CC(F)(F)CC(C(NC2=CC=C(Cl)C=C2)=O)C1)C3=CC(C4=CC=NC=C4)=CC=C3
InChi Code
InChI=1S/C24H20ClF2N3O2/c25-20-4-6-21(7-5-20)29-22(31)19-13-24(26,27)15-30(14-19)23(32)18-3-1-2-17(12-18)16-8-10-28-11-9-16/h1-12,19H,13-15H2,(H,29,31)
InChi Key
MKJLDLGLVZUENS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $120

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    5 mg

    $530

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    Product Description

    CCG-232601 is an inhibitor of the Rho/MRTF/SRF transcriptional pathway and a derivative of CCG-203971 (Item No. 15075).1 CCG-232601 inhibits MRTF-dependent transcription in HEK293T cells (IC50 = 0.55 µM in a luciferase reporter assay). It also reduces expression of α-smooth muscle actin (α-SMA) in TGF-β-stimulated human dermal fibroblasts to 31% of control when used at a concentration of 10 µM. CCG-232601 (50 mg/kg) inhibits increases in dermal thickness and hydroxyproline content in a mouse model of dermal fibrosis induced by bleomycin (Item No. 13877).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hutchings, K.M., Lisabeth, E.M., Rajeswaran, W., et al. Pharmacokinetic optimitzation of CCG-203971: Novel inhibitors of the Rho/MRTF/SRF transcriptional pathway as potential antifibrotic therapeutics for systemic scleroderma. Bioorg. Med. Chem. Lett. 27(8), 1744-1749 (2017).