1. GPCR/G Protein
  2. GnRH Receptor Neuropeptide FF Receptor
  3. 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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GUB08248

GUB08248 Chemical Structure

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Description

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[1][2].

IC50 & Target[1]

NPFF2-R

2.5 nM (EC50)

In Vitro

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.

In Vivo

GUB08248 (1250 nmol/kg; s.c.; twice daily) induces robust, sustained body weight loss of 13.5% relative to baseline and transient food intake suppression in diet-induced obese mice[1].

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

Animal Model: C57BL/6J (male, 5 weeks old at purchase, diet-induced obese)[1]
Dosage: 1250 nmol/kg
Administration: s.c.; twice daily
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.
Molecular Weight

1844.25

Formula

C85H150N24O21

Sequence

Ser-Arg-Gly-{Lys(AEEA-AEEA-γGlu-C18)}-Arg-Pro-Val-Gly-Arg-Phe-NH2

Sequence Shortening

SRG-Lys(AEEA-AEEA-γGlu-C18)-RPVGRF-NH2

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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  • 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.

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Product Name:
GUB08248
Cat. No.:
HY-P11810
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