GUB08248
GUB08248 is a full GPR10 agonist and a partial NPFF2R agonist, with EC50 values of 0.5 nM and 2.5 nM, respectively. GUB08248 inhibits food intake and induces sustained weight loss. GUB08248 can be used in obesity-related research.
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- Formule: C85H150N24O21
- Masse moléculaire:1844.25
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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NPFF2-R 2.5 nM (EC50) |
GUB08248 (30 min) acts as a potent dual full agonist of GPR10 and partial agonist of NPFF2R in Chem-1 cells expressing GPR10 and CHO-K1 cells expressing NPFF2R, with EC50 values of 0.5 nM and 2.5 nM, respectively[1].
GUB08248 (1 h) potently activates wild-type NPFF2R in HEK293T cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 5 weeks old at purchase, diet-induced obese)[1]
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Dosage:1250 nmol/kg
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Administration:s.c.; twice daily
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Result:Induced significant body weight loss of 10.9% relative to baseline by day 7 (p < 0.001).
Sustained body weight loss of 13.5% relative to baseline by day 13 (p < 0.001).
Significantly suppressed total food intake during the 7-day treatment phase relative to vehicle controls.
Restored food intake to vehicle levels during the wash-out phase.
Was detected in plasma samples collected 4 hours after last dosing on treatment day 6, and was further N-terminally degraded to GUB08251 in vivo.
Chemical Information
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Masse moléculaire 1844.25
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Formule C85H150N24O21
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Sequence
Ser-Arg-Gly-{Lys(AEEA-AEEA-γGlu-C18)}-Arg-Pro-Val-Gly-Arg-Phe-NH2
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Sequence Shortening
SRG-Lys(AEEA-AEEA-γGlu-C18)-RPVGRF-NH2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Alexopoulou F, et al. Lipidated PrRP31 metabolites are long acting dual GPR10 and NPFF2 receptor agonists with potent body weight lowering effect. Sci Rep. 2022;12(1):1696. Published 2022 Feb 1. [Content Brief]
[2]. Li X, et al. Molecular basis for cross-activation of NPFF2R by a short PrRP-related peptide. Acta Pharmacol Sin. Published online February 4, 2026. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GUB08248 Related Classifications
HY-P11810 Related Classifications
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