RG-239
RG-239 is an orally active TGR5 agonist with an EC50 of 120 nM, significantly outperforming Betulinic acid (HY-10529) (EC50 = 1.04 μM). RG-239 demonstrates higher selectivity for TGR5 compared to the FXRα. RG-239 increases mitochondrial activity in adipocytes and promotes neurite outgrowth at higher concentrations. RG-239 inhibits LPS (HY-D1056)-induced iNOS expression and nitrite production in Raw264.7 and microglia cells. RG-239 can be used for the study of type 2 diabetes[1][2][3][4][5].
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1199222-56-4
- 分子式: C33H52O3
- 分子量:496.76
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
生物活性
RG-239 (Compound 18 dia 2) (10 μM) increases mitochondrial activity in adipocytes as demonstrated by the increase in cytochrome c oxidase activity in 3T3L1 adipocyte cells[2].
RG-239 (1-10 μM) induces a neurite length of 9.5 μm at 1 μM significantly lower than induced by Retinoic acid (RA) (HY-14649), but the median neurite length is 37.0 μm at 10 μM, almost identical to that induced by Deoxycholic acid (DCA) (HY-N0593) in NSC-34 cells[3].
RG-239 (2 μM, 24 h) inhibits LPS-induced iNOS expression and nitrite production in Raw264.7 and microglia cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
RG-239 (Compound 18 dia 2) (30 mg/kg/day, p.o., 3 weeks) decreases the plasma glucose level in obese mice induced by a 10-week high-fat (HF) diet (60% kcal from fat)[2].
RG-239 (10 mg/kg/day, p.o., 2 weeks) decreases the expression of the inflammatory genes Tnfα, IL-6 and IL-1β in the livers of B6J mice induced by a 10-week high-fat (HF) diet (60% kcal from fat)[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:7 weeks male C57BL/6J mice with high fat diet (60% kcal Fat)[2]
-
Dosage:30 mg/kg/day
-
Administration:p.o. for 3 weeks
-
Result:Decreased the plasma glucose level.
-
Animal Model:6 weeks B6J mice with high fat diet (60% kcal Fat)[5]
-
Dosage:10 mg/kg/day
-
Administration:p.o. for 2 weeks
-
Result:Decreased the expression of the inflammatory genes Tnfα, IL-6, and IL-1β in the livers of B6J mice.
化学情報
-
CAS 番号 1199222-56-4
-
分子量 496.76
-
分子式 C33H52O3
-
SMILES
OC([C@]12[C@@]([C@@H](CC2)C(C)=C)([H])[C@]3([H])[C@@](CC1)([C@]4([C@]([C@@]5([C@@](C(C)([C@](O)(CC=C)CC5)C)([H])CC4)C)([H])CC3)C)C)=O
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Genet C, et al. Redefining the TGR5 triterpenoid binding pocket at the C-3 position. ChemMedChem. 2010 Dec 3;5(12):1983-8. [Content Brief]
[2]. Genet C, et al. Structure-activity relationship study of betulinic acid, a novel and selective TGR5 agonist, and its synthetic derivatives: potential impact in diabetes. J Med Chem. 2010 Jan 14;53(1):178-90. [Content Brief]
[3]. Ackerman HD, et al. Bile Acids Induce Neurite Outgrowth in Nsc-34 Cells via TGR5 and a Distinct Transcriptional Profile. Pharmaceuticals (Basel). 2023 Jan 24;16(2):174. [Content Brief]
[4]. Romero-Ramírez L, et al. Bile acids attenuate PKM2 pathway activation in proinflammatory microglia. Sci Rep. 2022 Jan 27;12(1):1459. [Content Brief]
[5]. Fujisaka S, et al. Antibiotic effects on gut microbiota and metabolism are host dependent. J Clin Invest. 2016 Dec 1;126(12):4430-4443. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
RG-239 関連分類
HY-177050 関連分類
Powered by Bioz