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Tocris/CCG 203971/5277/50/50 mg

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货号: 5277/50

品牌: Tocris

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Description: Inhibits the MRTF/SRF gene transcription pathway; antifibrotic agent

Chemical Name: N-(4-Chlorophenyl)-1-[3-(2-furanyl)benzoyl]-3-piperidinecarboxamide

Purity: ≥98% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Antifibrotic agent; inhibits fibrosis by targeting the MRTF/SRF gene transcription pathway. Selectively inhibits proliferation of SSc-derived dermal fibroblasts but not that of normal fibroblasts. Inhibits expression of CTGF, α-SMA, and COL1A2 in SSc fibroblasts as well as in LPA and in TGFβ-stimulated fibroblasts. Prevents bleomycin-induced skin thickening and collagen deposition in vivo. Also suppresses PC-3 cell migration in scratch wound assays (IC₅₀ = 4.2 μM).

Technical Data

M. Wt	408.88
Formula	C₂₃H₂₁ClN₂O₃
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	1443437-74-8
PubChem ID	71681561
InChI Key	HERLZBNILRVHQN-UHFFFAOYSA-N
Smiles	O=C(N2CCCC(C(NC3=CC=C(Cl)C=C3)=O)C2)C1=CC=CC(C4=CC=CO4)=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	20.44	50

Preparing Stock Solutions

The following data is based on the product molecular weight 408.88. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.45 mL	12.23 mL	24.46 mL
5 mM	0.49 mL	2.45 mL	4.89 mL
10 mM	0.24 mL	1.22 mL	2.45 mL
50 mM	0.05 mL	0.24 mL	0.49 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Michel et al (2014) Hope for disease-modifying treatment of systemic sclerosis/scleroderma. J.Pharmacol.Exp.Ther. 350 480 PMID: 25053235

Bell et al (2013) Optimization of novel nipecotic bis(amide) inhibitors of the Rho/MKL1/SRF transcriptional pathway as potential anti-metastasis agents. Bioorg.Med.Chem.Lett. 23 3826 PMID: 23707258

Haak et al (2014) 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. 349 480 PMID: 24706986

Keywords: CCG 203971, supplier, CCG203971, antifibrotic, agent, inhibits, fibrosis, inhibitors, MRTF/SRF, gene, transcription, pathway, myocarin-related, transcription, factor, Systemic, sclerosis, connective, tissue, PC-3, cell, migration, Other, Transcription, Factors, Other, Transcription, Factors, Tocris Bioscience

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