YH18968
YH18968 is an orally active GPR119 agonist with an EC50 of 2.8 nM for inducing cAMP accumulation. YH18968 activates GPR119, elevates intracellular cyclic adenosine monophosphate levels, stimulates glucagon-like peptide-1 secretion from intestinal L cells, and triggers glucose-dependent insulin secretion from pancreatic β cells. YH18968 improves glucose tolerance in normal mice and diet-induced obese mice. YH18968 can be used for the research of type 2 diabetes.
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- CAS No.: 1632498-56-6
- 화학식: C27H28FN9O3
- 분자량:545.58
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보관:
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
- 순도&문서
- References
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Help & FAQs
Biological Activity
YH18968 (0.03-1000 nM; 60 min) stimulates insulin secretion in HIT-T15 cells in a dose-dependent manner, with an EC50 of 3.5 nM[1].
YH18968 (0.03-1000 nM; 120 min) stimulates GLP-1 secretion from GLUTag cells in a dose-dependent manner, with an EC50 of 0.1 nM[1].
YH18968 (0.1-100 μM; 48 h) exhibits extremely low cytotoxicity in HIT-T15, GLUTag and HepG2 cells, with an LC50 greater than 100 μM in all three cell lines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HIT-T15 hamster insulinoma cells
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Concentration:0.03, 0.1, 0.3, 1, 3, 10, 30, 100, 300, and 1,000 nM nM (15 mM glucose condition); 100 nM (0, 3, or 15 mM glucose conditions)
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Incubation Time:60 min
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Result:Elicited dose-dependent increases in insulin release with an EC50 of 3.5 nM.
Enhanced insulin release in a glucose-dependent manner at 100 nM, with a significant increase observed at 15 mM glucose (2.19-fold vs control) and no effect in the absence of glucose.
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Cell Line:GLUTag murine intestinal L cells
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Concentration:0.03, 0.1, 0.3, 1, 3, 10, 30, 100, 300, and 1,000 nM
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Incubation Time:120 min
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Result:Enhanced GLP-1 secretion in a dose-dependent manner with an EC50 of 0.1 nM.
| Species | Dose | Route | AUClast | AUC0-inf | CL | Vss | MRT | Cmax | Tmax | T1/2 | F |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 1 mg/kg | i.v. | 1375.1 ng·h/mL | 1619.9 ng·h/mL | 617.3 mL/h/kg | 2112.2 mL/kg | 3.4 h | / | / | / | / |
| Mice[1] | 1 mg/kg | p.o. | 549.7 ng·h/mL | 719.8 ng·h/mL | / | / | / | 168.6 ng/mL | 0.5 h | 3.1 h | 40.0 % |
| Mice[1] | 10 mg/kg | p.o. | 2471.7 ng·h/mL | 2958.2 ng·h/mL | / | / | / | 759.7 ng/mL | 0.5 h | 2.6 h | 18.0 % |
| Mice[1] | 100 mg/kg | p.o. | 6538.0 ng·h/mL | 15773.9 ng·h/mL | / | / | / | 1472.2 ng/mL | 0.5 h | 9.2 h | 4.8 % |
YH18968 (0.1-10 mg/kg; p.o.; single dose) significantly improves glucose tolerance in DIO mice, with its efficacy reaching saturation at 1 mg/kg[1].
YH18968 (1 mg/kg; p.o.; once daily; for 28 consecutive days) for 4 consecutive weeks sustains improved glucose tolerance in DIO mice without rapid desensitization, and produces a synergistic effect when combined with Linagliptin (HY-10284)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (8-week-old, male)[1]
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Dosage:0.1 mg/kg; 1 mg/kg; 10 mg/kg; 10 mg/kg + 1 mg/kg linagliptin
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Administration:p.o.; single dose
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Result:Significantly lowered the 2-hour area under the curve (AUC) for blood glucose in a dose-dependent manner compared to vehicle control.
Produced a significant additive glucose-lowering effect when co-administered with 1 mg/kg linagliptin.
Increased active plasma GLP-1 levels by 2.7-fold compared to vehicle control at 30 minutes post-administration at 10 mg/kg dose.
Co-administration with linagliptin significantly increased active GLP-1 levels compared to either agent alone.
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Animal Model:diet-induced obese (DIO) (17-week-old, male, Type 2 diabetes model)[1]
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Dosage:0.1 mg/kg; 1 mg/kg; 10 mg/kg
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Administration:p.o.; single dose
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Result:Significantly lowered the 2-hour AUC for blood glucose compared to vehicle control at 1 and 10 mg/kg doses, with a dose-dependent effect observed.
Produced similar levels of glucose lowering at 1 and 10 mg/kg doses, indicating a saturated effect.
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Animal Model:diet-induced obese (DIO) (17-week-old, male, Type 2 diabetes model)[1]
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Dosage:1 mg/kg; 1 mg/kg + 1 mg/kg linagliptin
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Administration:p.o.; once daily; 28 days
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Result:Significantly lowered the 2-hour AUC for blood glucose compared to vehicle control on day 1, with a more potent effect than 10 mg/kg MBX2982 (HY-15291).
Produced an additive glucose-lowering effect when co-administered with 1 mg/kg linagliptin compared to either agent alone on day 1.
Continued to effectively lower the 2-hour AUC for blood glucose on day 29, maintaining glucose tolerance improvement equivalent to day 1 efficacy when used alone or in combination with Linagliptin.
Chemical Information
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CAS No. 1632498-56-6
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분자량 545.58
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화학식 C27H28FN9O3
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SMILES
O=C1N(C=NN1[C@H]2CCOC2)C3=C(F)C=C(C=C3)C=4C=C(C#N)C(=NC4)N5CCN(CC5)C=6N=C(C(C)C)ON6
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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