GPR109 receptor agonist-3
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.
For research use only. We do not sell to patients.
- CAS No.: 944559-31-3
- Formula: C16H23N3O2S2
- Molecular Weight:353.50
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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.
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.
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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]
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Dosage:60 mg/kg
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Administration:p.o. daily for 4 weeks
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Result:Decreased total cholesterol (TC), triglyceride (TG), and low-density lipoprotein cholesterol (LDL-C) levels.
Increased high-density lipoprotein cholesterol (HDL-C) level.
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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]
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Dosage:0.03% and 0.1% in diet
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Administration:p.o. for 9 weeks
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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.
Chemical Information
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CAS No. 944559-31-3
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Molecular Weight 353.50
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Formula C16H23N3O2S2
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SMILES
O=C(C1=CC=CN=C1)NCCNC(CCCCC2SSCC2)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GPR109 receptor agonist-3 Related Classifications
HY-176817 Related Classifications
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