Cenicriviroc

製品コードS8512 バッチS851202

印刷

化学情報

Chemical Structure Synonyms TAK-652, CVC, TBR-652 Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C41H52N4O4S
分子量 696.94 CAS No. 497223-25-3
Solubility (25°C)* 体外 DMSO 100 mg/mL (143.48 mM)
Ethanol 100 mg/mL (143.48 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Cenicriviroc is a potent, orally active dual inhibitor of CC chemokine receptor 2 (CCR2) and CCR5. Cenicriviroc also inhibits HIV-1 and HIV-2 with potent anti-inflammatory and antiinfective activity.
in vitro

Migration of mouse monocytes in response to CCL2, the most potent mediator of chemotaxis for activated macrophages, is reduced following pre-treatment with Cenicriviroc at a concentration of 1 μM.[2]
in vivo

Cenicriviroc significantly reduces monocyte/macrophage recruitment in vivo at doses >= 20 mg/kg/day (p < 0.05). At these doses, Cenicriviroc shows antifibrotic effects, with significant reductions in collagen deposition (p < 0.05), and collagen type 1 protein and mRNA expression across the three animal models of fibrosis. In the NASH model, Cenicriviroc significantly reduces the nonalcoholic fatty liver disease activity score (p < 0.05 vs. controls). Cenicriviroc treatment has no notable effect on body or liver/kidney weight.[2]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 activated macrophages
濃度 1 μM
反応時間 2 h
実験の流れ

TG is injected intraperitoneally into male C57BL/6 mice and activated macrophages are collected 48 hours later by peritoneal lavage. Chemotaxis is assayed using a Transwell1 Chamber with a 5 μm-pore size polycarbonate filter. Briefly, cells are incubated for 2 hours in the presence of 1 nM CCL2 and/or 1 μM Cenicriviroc (dissolved in dimethyl sulfoxide with 0.5% acetic acid and diluted 1:1000 with serum-free Roswell Park Memorial Institute-1640 medium and 0.5% bovine serum albumin). Cells are harvested from the lower compartment and analyzed by flow cytometry to enumerate F4/80+CD11b+ macrophages using a 3-laser BD FACSCanto. Results are analyzed using FlowJo software.
動物実験 動物モデル 8–10 weeks old male C57BL/6 mice, 10–12 weeks old male Sprague-Dawley rats
投薬量 5 mg/kg, 20 mg/kg, 100 mg/kg, 30 mg/kg
投与方法 Oral gavage, IP

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

C-C motif chemokine receptor 2 inhibition reduces liver fibrosis by restoring the immune cell landscape [ Int J Biol Sci, 2023, 19(8):2572-2587] PubMed: 37215993
Targeted Deletion of Rictor in BMSCs Reduces the Biological Activity of K7M2 Cells and Mitigates OS-Induced Bone Destruction [ Stem Cells, 2023, 41(6):672-683] PubMed: 37099695
Proteomic analysis reveals microvesicles containing NAMPT as mediators of radioresistance in glioma [ Life Science Alliance, 2023, 6(6)] PubMed: None
Proteomic analysis reveals microvesicles containing NAMPT as mediators of radioresistance in glioma [ Life Sci Alliance, 2023, 6(6)e202201680] PubMed: 37037593
Cancer-associated fibroblasts facilitate premetastatic niche formation through lncRNA SNHG5-mediated angiogenesis and vascular permeability in breast cancer [ Theranostics, 2022, 12(17):7351-7370] PubMed: 36438499
Deficiency of Lactoferrin aggravates lipopolysaccharide-induced acute inflammation via recruitment macrophage in mice [ Biometals, 2022, 1-14] PubMed: 35650365
C-reactive protein protects against acetaminophen-induced liver injury by preventing complement overactivation [ Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00191-0] PubMed: 34536564

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。

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