| CAS NO: | 1443437-74-8 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| Molecular Weight (MW) | 408.88 |
|---|---|
| Formula | C23H21ClN2O3 |
| CAS No. | 1443437-74-8 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 81 mg/mL (198.1 mM) |
| Water: < 1mg/mL | |
| Ethanol: 4 mg/mL (9.8 mM) | |
| Solubility (In vivo) | 10% DMSO : 40% PEG300 : 5% Tween-80 : 45% saline: ≥ 2.5 mg/mL |
| Synonyms | CCG203971; CCG 203971; CCG-203971. |
| SMILES Code | O=C(C1CN(C(C2=CC=CC(C3=CC=CO3)=C2)=O)CCC1)NC4=CC=C(Cl)C=C4 |
| In Vitro | In vitro activity: CCG-203971 inhibits expression of connective tissue growth factor (CTGF), α-smooth muscle actin (α-SMA), and collagen 1 (COL1A2) in both SSc fibroblasts and in lysophosphatidic acid (LPA)-and transforming growth factor β (TGFβ)-stimulated fibroblasts. 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. |
|---|---|
| In Vivo | CCG-203971 was tested in a Bleomycin skin injury model. Bleomycin was 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). |
| Animal model | Skin fibrosis is induced in C57BL/6 mice (female, 8 weeks old) |
| Formulation & Dosage | 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. |
| References | J Pharmacol Exp Ther. 2014 Jun;349(3):480-6. |
m.cnreagent.com