2. GPCR/G Protein
  3. Free Fatty Acid Receptor
  4. MK-2305

MK-2305 is an orally active GPR40 partial agonist with an EC50 of 6 nM in rats. MK-2305 mediates glucose-stimulated insulin secretion and inhibits endogenous glucose production by reducing gluconeogenesis from tricarboxylic acid (TCA) cycle substrates. MK-2305 increases plasma insulin levels under hyperglycemic and glucose-stimulated conditions, reduces fasting blood glucose, and improves glucose homeostasis. MK-2305 can be used in studies related to type 2 diabetes.

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MK-2305

MK-2305 Chemical Structure

CAS No. : 2101206-49-7

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MK-2305 Related Antibodies

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Description

MK-2305 is an orally active GPR40 partial agonist with an EC50 of 6 nM in rats. MK-2305 mediates glucose-stimulated insulin secretion and inhibits endogenous glucose production by reducing gluconeogenesis from tricarboxylic acid (TCA) cycle substrates. MK-2305 increases plasma insulin levels under hyperglycemic and glucose-stimulated conditions, reduces fasting blood glucose, and improves glucose homeostasis. MK-2305 can be used in studies related to type 2 diabetes[1][2].

IC50 & Target[2]

GPR40

6 nM (EC50)

In Vitro

MK-2305 (60 min) potently and selectively activates rat GPR40 in CHO cells with an EC50 of 6 nM and 166% partial activation, while showing minimal activity against other metabolic receptors[1].

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

MK-2305 Related Antibodies
In Vivo

MK-2305 (0.3-10 mg/kg; p.o.; single dose) acutely improves glucose tolerance and stimulates glucose-dependent insulin secretion in male GK rats, with a maximally efficacious dose of 3 mg/kg that reduces glucose AUC0-t by 40%[1].
MK-2305 (10-30 mg/kg/day; p.o.; daily via diet; 20 days) reduces both fed and fasting blood glucose, lowers HbA1c, and enhances glucose-stimulated insulin secretion in male GK rats, with a 30 mg/kg/day dose producing a 30% reduction in fasting glucose on day 14[1].
MK-2305 (10 mg/kg; p.o.; single dose; 10 mg/kg/day; p.o.; daily) reduces endogenous glucose production in male GK rats, primarily through suppression of gluconeogenesis, with acute treatment lowering total EGP by 36.7%[1].
MK-2305 (10 mg/kg; p.o.; single dose) does not enhance glucose uptake in skeletal muscle or liver of male GK rats, instead reducing hepatic glucose disposal into glycogen and glycolytic products[1].

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

Animal Model: Goto Kakizaki (GK) (male, 8 weeks of age)[1]
Dosage: 0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: p.o.; single dose
Result: Reduced glucose AUC during OGTT by 18% at 0.3 mg/kg, 40% at 3 mg/kg, and 54% at 10 mg/kg.
Increased insulin AUC by 59% at 1 mg/kg, 83% at 3 mg/kg, and 124% at 10 mg/kg.
Identified maximally efficacious dose (MED) as 3 mg/kg.
Animal Model: Goto Kakizaki (GK) (male, 8 weeks of age)[1]
Dosage: 10 mg/kg/day; 30 mg/kg/day
Administration: p.o.; daily via diet; 20 days
Result: Reduced fed blood glucose by 22% at 10 mg/kg and 27% at 30 mg/kg on day 3, with effects maintained through day 20.
Reduced fasting blood glucose by 19% at both doses on day 7, and by 26% at 10 mg/kg and 30% at 30 mg/kg on day 14.
Reduced HbA1c levels at both doses.
Increased plasma insulin levels during OGTT on day 13 compared to vehicle controls.
Reduced food intake through day 14 at 30 mg/kg, with no sustained effect on body weight; 10 mg/kg dose had no effect on food intake or body weight.
Caused no significant changes in fasting plasma insulin, plasma non-esterified fatty acids, or liver triglycerides.
Animal Model: Goto Kakizaki (GK) (male, 8 weeks of age)[1]
Dosage: 10 mg/kg; 10 mg/kg/day
Administration: p.o.; single dose; p.o.; daily
Result: Acutely reduced total endogenous glucose production (EGP) to 32.9 μmol/kg/min, a 36.7% reduction.
Acutely reduced EGP from gluconeogenic substrates entering at the TCA cycle to 26.0 μmol/kg/min.
Acutely reduced EGP from gluconeogenic substrates entering as triose phosphates to 6.90 μmol/kg/min.
Chronically reduced total EGP and EGP from TCA cycle substrates at 10 mg/kg/day.
Caused no effect on EGP derived from glycogenolysis.
Animal Model: Goto Kakizaki (GK) (male, 8 weeks of age)[1]
Dosage: 10 mg/kg
Administration: p.o.; single dose
Result: Produced no significant effect on the disposal of 13C-glucose into metabolites in skeletal muscle.
Significantly reduced the disposal of 13C-glucose into 13C-glucose-6-phosphate, 13C-glycogen, 13C-lactate, and 13C-alanine in the liver.
Molecular Weight

443.82

Formula

C19H13ClF3NO4S
CAS No.
SMILES

O=C1SC(C(=O)N1)C2C3=CC=C(OC4=CC=C(C=C4Cl)C(F)(F)F)C=C3OCC2
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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
References
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MK-2305 Related Classifications

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  • 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:

MK-23052101206-49-7MK2305MK 2305Free Fatty Acid ReceptorFFARHbA1cGPR40glucose homeostasisGoto Kakizaki ratstype 2 diabetesplasma insulinTCA cycleCHO cellsgluconeogenesispancreatic β-cellsInhibitorinhibitorinhibit

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