2. GPCR/G Protein
  3. GPR109A
  4. GPR109 receptor agonist-3

GPR109 receptor agonist-3 是一种具有口服活性的 GPR109 受体激动剂，IC50 为 310 nM。GPR109 receptor agonist-3 保留了硫辛酸 (HY-18733) 的抗氧化和细胞保护作用。GPR109 receptor agonist-3 在高脂饮食喂养的大鼠中降低总胆固醇 (TC)、甘油三酯 (TG)、低密度脂蛋白胆固醇 (LDL-C)，并增加高密度脂蛋白胆固醇 (HDL-C)。GPR109 receptor agonist-3 可用于动脉粥样硬化研究。

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GPR109 receptor agonist-3

GPR109 receptor agonist-3 Chemical Structure

CAS No. : 944559-31-3

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GPR109 receptor agonist-3 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GPR109 receptor agonist-3 is an orally active GPR109 receptor agonist, with an IC50 of 310 nM. GPR109 receptor agonist-3 retains the antioxidation and cytoprotection of Lipoic acid (HY-18733). GPR109 receptor agonist-3 reduces total cholesterol (TC), triglyceride (TG), low-density lipoprotein cholesterol (LDL-C) and increases high-density lipoprotein cholesterol (HDL-C) in high-fat diet-fed rats. GPR109 receptor agonist-3 can be used for the study of atherosclerosis[1].

体外研究
(In Vitro)

GPR109 receptor agonist-3 (Compound N2L) (10-100 μM，预处理 30 分钟) 显著减弱 HT22 细胞中 L-谷氨酸诱导的毒性，并有效降低 HUVECs 中 H2O2 诱导的毒性，改善细胞存活率[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

GPR109 receptor agonist-3 相关抗体:
体内研究
(In Vivo)

GPR109 receptor agonist-3 (Compound N2L) (60 mg/kg，口服，每日一次，4 周) 在高脂饮食喂养的大鼠中降低总胆固醇 (TC)、甘油三酯 (TG)、低密度脂蛋白胆固醇 (LDL-C)，并增加高密度脂蛋白胆固醇 (HDL-C)[1]。
GPR109 receptor agonist-3 (饮食中 0.03%-0.1%，口服，9 周) 在 ApoE 敲除小鼠中减少主动脉斑块面积，降低血清 TC、TG、LDL-C，增加 HDL-C，减弱血管超氧化物产生和肝脏 MDA 水平，并抑制体重增加[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: High-fat diet-fed rats: Female Sprague-Dawley rats were fed a high-fat diet (5% lard oil, 10% sugar and 1% cholesterol) for 8 weeks to establish hyperlipidemia model[1]
Dosage: 60 mg/kg
Administration: p.o. daily for 4 weeks
Result: Decreased total cholesterol (TC), triglyceride (TG), and low-density lipoprotein cholesterol (LDL-C) levels.
Increased high-density lipoprotein cholesterol (HDL-C) level.
Animal Model: ApoE null mice: Homozygous male apolipoprotein E (ApoE) null mice (10 weeks old) on C57BL/6 background were fed a Western-type diet containing 0.15% (w/w) cholesterol and 21% (w/w) fat for 1 week to obtain similar total cholesterol levels, then used to establish atherosclerosis model[1]
Dosage: 0.03% and 0.1% in diet
Administration: p.o. for 9 weeks
Result: Reduced aortic plaque area. Decreased serum total cholesterol (TC) triglyceride (TG) and low-density lipoprotein cholesterol (LDL-C).
Increased high-density lipoprotein cholesterol (HDL-C) by 128% at 0.1% dose.
Attenuated vascular superoxide production in innominate arteries.
Decreased hepatic malondialdehyde (MDA) level to 36% at 0.1% dose.
Inhibited body weight gain compared to control.
Exhibited higher food intake but lower body weight.
Showed no significant liver or kidney toxicity, with hepatic protection against diet-induced damage.
分子量

353.50

Formula

C16H23N3O2S2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

GPR109 receptor agonist-3 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

GPR109 receptor agonist-3944559-31-3GPR109AHM74APUMA-GHCA2HCAR2 GPR109 receptoratherosclerosistotal cholesterol (TC)triglyceride (TG)low-density lipoprotein cholesterol (LDL-C)high-density lipoprotein cholesterol (HDL-C)Inhibitorinhibitorinhibit

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