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Glycine-β-muricholic Acid Sale

(Synonyms: Gly-MCA, GβMCA) 目录号 : GC40911

Glycine-β-muricholic Acid是一种有效的、稳定的、对精氨酸有选择性的口服生物活性FXR抑制剂,是鼠特异性初级胆汁酸β-鼠胆酸的甘氨酸结合形式。

Glycine-β-muricholic Acid Chemical Structure

Cas No.:66225-78-3

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥3,457.00
现货
5mg
¥3,375.00
现货
10mg
¥5,400.00
现货

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Sample solution is provided at 25 µL, 10mM.

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Description

Glycine-β-muricholic Acid is an effective, stable, and arginine-selective oral bioactive FXR inhibitor. It is the glycine-bound form of the murine primary bile acid β-muricholic acid. FXR is an important sensor and regulator of bile acid, lipid, and glucose metabolism [1]. Glycine-β-muricholic Acid can be used in studies of metabolic disorders [2].

In vivo, Glycine-β-muricholic Acid (10 and 50mg/kg; 5 weeks; oral) significantly reduced the absolute fat mass and fat-to-weight ratio of obese and insulin-resistant mice induced by HFD, as well as insulin resistance and hepatic steatosis, with a significant decrease in liver lipid droplets [1]. Glycine-β-muricholic Acid (10mg/kg/day; 23d once every 2 days; Gavage) treatment significantly reduced the protective effect of Lactobacillus reuteri on alcohol-induced lipid accumulation in the liver of mice. Lactobacillus reuteri and its metabolites may regulate liver inflammation through the FXR signaling regulatory axis [3].

References:
[1] Jiang, C., Xie, C., Lv, Y., et al. Intestine-selective farnesoid X receptor inhibition improves obesity-related metabolic dysfunction. Nat. Commun. 6, 10166 (2015).
[2] Hasan M N, Wang H, Luo W, et al. Gly-β-MCA is a potent anti-cholestasis agent against “human-like” hydrophobic bile acid-induced biliary injury in mice[J]. Journal of Lipid Research, 2024, 65(10). 
[3] Cheng Y, Xiang X, Liu C, et al. Transcriptomic analysis reveals Lactobacillus reuteri alleviating alcohol-induced liver injury in mice by enhancing the farnesoid X receptor signaling pathway[J]. Journal of agricultural and food chemistry, 2022, 70(39): 12550-12564.

Glycine-β-muricholic Acid是一种有效的、稳定的、对精氨酸有选择性的口服生物活性FXR抑制剂,是鼠特异性初级胆汁酸β-鼠胆酸的甘氨酸结合形式。FXR是胆汁酸、脂质和葡萄糖代谢的重要传感器和调节因子 [1]。Glycine-β-muricholic Acid可用于代谢障碍的研究 [2]

在体内,Glycine-β-muricholic Acid(10和50mg/kg; 5 weeks; oral)显著降低了HFD诱导的肥胖和胰岛素抵抗小鼠的绝对脂肪质量和脂肪/瘦体重比,以及胰岛素抵抗和肝脂肪变性,肝脏脂滴显著减少 [1]。Glycine-β-muricholic Acid(10mg/kg/day; 23d once every 2 days; gavage)显著降低了Lactobacillus reuteri对酒精诱导的小鼠肝脏脂质蓄积的保护作用,Lactobacillus reuteri及其代谢产物可能通过FXR信号调节轴调节肝脏炎症 [3]

实验参考方法

Animal experiment [1]:

Animal models

C57BL/6N mice

Preparation Method

For thermal neutral temperature exposure experiments, male 6-week-old C57BL/6N mice fed a HFD were orally administered with vehicle (control pills) or Glycine-β-muricholic Acid (0.25mg per pill per day, dose10mg kg−1) at 29.5°C for 2 weeks. For cold stimulation experiments, male 6-week-old C57BL/6N mice fed a HFD were orally administered with vehicle (control pills) or Glycine-β-muricholic Acid (0.25mg per pill per day, dose 10mg kg−1) at 22°C for 5 days and then acutely moved to 5°C for another 1 day. All mice were randomly assigned to experimental groups and the groups showed no difference in body weight gain before treatment.

Dosage form

10mg/kg/day for 5 days and two weeks; p.o.

Applications

A short-duration 5-day treatment with Glycine-β-muricholic Acid specifically increases beige fat thermogenesis and energy expenditure before body weight change.

References:
[1] Jiang, C., Xie, C., Lv, Y., et al. Intestine-selective farnesoid X receptor inhibition improves obesity-related metabolic dysfunction. Nat. Commun. 6, 10166 (2015).

化学性质

Cas No. 66225-78-3 SDF
别名 Gly-MCA, GβMCA
化学名 N-[(3α,5β,6β,7β)-3,6,7-trihydroxy-24-oxocholan-24-yl]-glycine
Canonical SMILES O[C@@H]1CC[C@@]2(C)[C@@]([C@H](O)[C@H](O)[C@]3([H])[C@]2([H])CC[C@@]4(C)[C@@]3([H])CC[C@]4([H])[C@H](C)CCC(NCC(O)=O)=O)([H])C1
分子式 C26H43NO6 分子量 465.6
溶解度 20mg/mL in ethanol, or in DMSO, 20mg/mL in DMF 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.1478 mL 10.7388 mL 21.4777 mL
5 mM 0.4296 mL 2.1478 mL 4.2955 mL
10 mM 0.2148 mL 1.0739 mL 2.1478 mL
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