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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C23H21ClN2O3 |
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分子量 | 408.88 | CAS No. | 1443437-74-8 | |
Solubility (25°C)* | 体外 | DMSO | 81 mg/mL (198.1 mM) | |
Ethanol | 4 mg/mL (9.78 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | CCG-203971 is a novel small-molecule inhibitor of the Rho/MRTF/SRF pathway with the IC50 value of 0.64 μM for SRE.L. It inhibits Rho-mediated gene transcription. |
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in vitro | 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[2]. |
in vivo | CCG-203971 exhibits promising anti-fibrotic activity both in vitro and in vivo in several animal models of disease, including intestinal fibrosis, pulmonary fibrosis and dermal fibrosis. The half-life of CCG-203971 in mouse liver microsomes (MLM) is only 1.6 min, indicating high susceptibility to oxidative metabolism[1]. In vivo treatment with CCG-203971 also preventes bleomycin-induced skin thickening and collagen deposition[2]. |
細胞アッセイ | 細胞株 | Dermal fibroblasts |
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濃度 | 30 μM | |
反応時間 | 72 h | |
実験の流れ | 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 was read. |
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動物実験 | 動物モデル | C57BL/6 mice |
投薬量 | 100 mg/kg | |
投与方法 | i.p. |
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Persistent Hypoxia with Intermittent Aggravation Causes Imbalance in Smad3/Myocardin-Related Transcription Factor Signaling with Consequent Endothelial Senescence and Pulmonary Arterial Remodeling [ Biomedicines, 2023, 11(9)2351] | PubMed: 37760802 |
MKL1 mediates TGF-β-induced CTGF transcription to promote renal fibrosis. [ J Cell Physiol, 2020, 235(5):4790-4803] | PubMed: 31637729 |
Targeting effector pathways in RAC1P29S-driven malignant melanoma. [ Small GTPases, 2020, 10.1080/21541248] | PubMed: 32043900 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。