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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C85H150N24O21
- 分子量:1844.25
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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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.
化学情報
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分子量 1844.25
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分子式 C85H150N24O21
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配列
Ser-Arg-Gly-{Lys(AEEA-AEEA-γGlu-C18)}-Arg-Pro-Val-Gly-Arg-Phe-NH2
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シーケンスの短縮
SRG-Lys(AEEA-AEEA-γGlu-C18)-RPVGRF-NH2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
GUB08248 関連分類
HY-P11810 関連分類
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