2. GPCR/G Protein Neuronal Signaling
  3. GPR119
  4. 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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YH18968

YH18968 Chemical Structure

CAS No. : 1632498-56-6

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YH18968 Related Antibodies

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Description

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[1].

In Vitro

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.

YH18968 Related Antibodies

ELISA Assay[1]

Cell Line: HIT-T15 hamster insulinoma cells
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)
Incubation Time: 60 min
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.

ELISA Assay[1]

Cell Line: GLUTag murine intestinal L cells
Concentration: 0.03, 0.1, 0.3, 1, 3, 10, 30, 100, 300, and 1,000 nM
Incubation Time: 120 min
Result: Enhanced GLP-1 secretion in a dose-dependent manner with an EC50 of 0.1 nM.
Parmacokinetics
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 %
In Vivo

YH18968 (0.1-10 mg/kg; p.o.; single dose) dose-dependently improves glucose tolerance in normal C57BL/6J mice[1].
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.

Animal Model: C57BL/6J (8-week-old, male)[1]
Dosage: 0.1 mg/kg; 1 mg/kg; 10 mg/kg; 10 mg/kg + 1 mg/kg linagliptin
Administration: p.o.; single dose
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.
Animal Model: diet-induced obese (DIO) (17-week-old, male, Type 2 diabetes model)[1]
Dosage: 0.1 mg/kg; 1 mg/kg; 10 mg/kg
Administration: p.o.; single dose
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.
Animal Model: diet-induced obese (DIO) (17-week-old, male, Type 2 diabetes model)[1]
Dosage: 1 mg/kg; 1 mg/kg + 1 mg/kg linagliptin
Administration: p.o.; once daily; 28 days
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.
Molecular Weight

545.58

Formula

C27H28FN9O3
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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YH18968 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

YH189681632498-56-6YH 18968YH-18968GPR119G Protein-Coupled Receptor 119pancreatic beta cellsintestinal L cellsdipeptidyl peptidase 4 inhibitorglucagon-like peptide-1type 2 diabetes mellitusCHO-K1 cellsnormal micediet-induced obese miceintracellular cyclic adenosine monophosphateInhibitorinhibitorinhibit

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