GPR109 receptor agonist-3

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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.

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GPR109 receptor agonist-3 Chemical Structure

CAS No. : 944559-31-3

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Description

In Vitro

GPR109 receptor agonist-3 (Compound N2L) (10-100 μM, 30 min pretreatment) significantly attenuates L-glutamate-induced toxicity in HT22 cells and effectively reduces H2O2-induced toxicity in HUVECs, improving cell viability^[1].

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

In Vivo

GPR109 receptor agonist-3 (Compound N2L) (60 mg/kg, p.o., daily, 4 weeks) 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^[1].
GPR109 receptor agonist-3 (0.03%-0.1% in diet, p.o., 9 weeks) reduces aortic plaque area, decreases serum TC, TG, LDL-C, increases HDL-C, attenuates vascular superoxide production and hepatic MDA levels, and inhibits weight gain in ApoE null mice^[1].

MedChemExpress (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.

Molecular Weight

353.50

Formula

C₁₆H₂₃N₃O₂S₂

CAS No.

944559-31-3

SMILES

O=C(C1=CC=CN=C1)NCCNC(CCCCC2SSCC2)=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Jiang Y, et al. Discovery of a novel niacin-lipoic acid dimer N2L attenuating atherosclerosis and dyslipidemia with non-flushing effects. Eur J Pharmacol. 2020 Feb 5;868:172871. [Content Brief]