GUB08248 acetate
Based on 1 Customer Validation
GUB08248 acetate is a full GPR10 agonist and a partial NPFF2R agonist, with EC50 values of 0.5 nM and 2.5 nM, respectively. GUB08248 acetate inhibits food intake and induces sustained weight loss. GUB08248 acetate can be used in obesity-related research.
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- Pureté: 98.86%
- Formule: C85H150N24O21·xC2H4O2
- Masse moléculaire:1844.25 (free base)
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Stockage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
GUB08248 (30 min) acetate 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) acetate 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.
Sustained body weight loss of 13.5% relative to baseline by day 13.
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.
Chemical Information
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Appearance Solid
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Masse moléculaire 1844.25 (free base)
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Formule C85H150N24O21·xC2H4O2
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Color White to off-white
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SMILES
CC(O)=O.O=C(N[C@@H](CCCNC(N)=N)C(NCC(N[C@@H](CCCCNC(COCCOCCNC(COCCOCCNC(CC[C@H](NC(CCCCCCCCCCCCCCCCC)=O)C(O)=O)=O)=O)=O)C(N[C@@H](CCCNC(N)=N)C(N1[C@@H](CCC1)C(N[C@@H](C(C)C)C(NCC(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC2=CC=CC=C2)C(N)=O)=O)=O)=O)=O)=O)=O)=O)=O)[C@H](CO)N.[x]
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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
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
DMSO : 33.33 mg/mL (Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL; Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL; Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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 acetate Related Classifications
HY-P11810A Related Classifications
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