Poterepatide
Based on 1 Customer Validation
Poterepatide (HDM1005) is a GLP-1R/GIPR dual agonist. Poterepatide preferentially reduces fat mass and improves hepatic steatosis in a dose-dependent manner, improving lipid metabolism and liver function. Poterepatide can be used in research on type 2 diabetes, obesity, and metabolic dysfunction-associated steatohepatitis.
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- Purity : 99.78%
- CAS No.: 3058127-20-8
- 화학식: C243H382N52O73
- 분자량:5199.94
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보관:
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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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
GLP-1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
0.0917 nM
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HDM1005-induced cAMP accumulation in HEK293/GIPR cells measured by TR-FRET after 30 mins stimulation and an additional 1 hr incubation.
HDM1005-induced cAMP accumulation in HEK293/GIPR cells measured by TR-FRET after 30 mins stimulation and an additional 1 hr incubation.
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42125916 |
In Vitro
Poterepatide (30 min) activates GLP-1R and GIPR with EC50 values of 0.0286 nM and 0.0917 nM, respectively, in HEK293 cAMP assays[1].
Poterepatide (0.1-10 μM; 0.5 h) is highly plasma protein bound across mouse, rat, monkey plasma, with ≥99.58% binding at 0.1-10 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | AUC0-96 | AUC0-∞ | AUC0-t | Cmax | CL_obs | T1/2 | Tmax | MRT0-t | Bioavailability |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 1.54 nmol/Kg | s.c. | 174 nM·h | 177 nM·h | 176 nM·h | 4.39 nM | 8.99 mL/h/kg | 13.3 h | 12.0 (12.0, 24.0) h | / | / |
| Rat[1] | 7.70 nmol/Kg | s.c. | 1206 nM·h | 1187 nM·h | 1206 nM·h | 27.3 nM | 6.98 mL/h/kg | 14.0 h | 24.0 (12.0, 24.0) h | 29.7 h | 39.3 % |
In Vivo
Poterepatide (3-30 nmol/kg; subcutaneous injection; repeated administration) improves glycemic control in db/db mice, with fasting blood glucose approaching normal at 30 nmol/kg[1].
Poterepatide (1-10 nmol/kg; subcutaneous injection; once every three days; 4 weeks) improves glycemic control in db/db mice, with a minimum effective dose of 1 nmol/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:db/db (male, 7-10 weeks old)[1]
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Dosage:1, 10, and 30 nmol/kg
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Administration:s.c.; single injection
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Result:Efficacy onset occurred at 1 nmol/kg.
Maximal glucose lowering was observed at 10 nmol/kg.
10 nmol/kg maintained glucose-lowering efficacy for 96 h.
30 nmol/kg maintained a glucose-lowering effect for 72 h.
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Animal Model:db/db (male, 7-10 weeks old)[1]
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Dosage:3, 10, and 30 nmol/kg
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Administration:s.c.; repeated dosing
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Result:Superior glycemic control was produced at 3 nmol/kg.
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Animal Model:db/db (male, 7-10 weeks old)[1]
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Dosage:1 and 10 nmol/kg
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Administration:s.c.; Q3D; 4 weeks
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Result:The minimum effective dose for HbA1c reduction was 1 nmol/kg.
10 nmol/kg produced HbA1c lowering equivalent to the 30 nmol/kg tirzepatide reference.
The OGTT minimum effective dose was 1 nmol/kg, with dose-dependent improvement in glucose tolerance.
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Animal Model:DIO (male, 26 weeks old)[1]
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Dosage:1 and 30 nmol/kg
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Administration:s.c.; Q3D; 28 days
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Result:The minimum effective dose was 1 nmol/kg.
Maximal body-weight reduction was 39.97% at 30 nmol/kg.
Reduced abdominal fat and cumulative food intake, lowered random and fasting glucose and insulin, improved lipid metabolism and liver function, and dose-dependently ameliorated hepatic steatosis.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 3058127-20-8
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Appearance Solid
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분자량 5199.94
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화학식 C243H382N52O73
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Color White to off-white
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Synonyms
HDM1005
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Sequence
Tyr-{Aib}-Glu-Gly-Thr-{Phe(αMe)}-Thr-Ser-Asp-Tyr-{Aib}-Ile-{Aib}-Leu-Asp-Lys-Gln-Ala-Gln-Ala-Glu-Phe-Val-{K(AEEA-AEEA-AEEA-{γGlu}-C22 diacid)}-Trp-Leu-Leu-Lys-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-Lys-NH2
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Sequence Shortening
Y-{Aib}-EGT-{Phe(αMe)}-TSDY-{Aib}-I-{Aib}-LDKQAQAEFV-{K(AEEA-AEEA-AEEA-{γGlu}-C22 diacid)}-WLLKGGPSSGAPPPSK-NH2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
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)
용액&용해도
In Vitro:
DMSO : 50 mg/mL (9.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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 (0.48 mM); 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 (0.48 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
In Vivo Dissolution Calculator
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.
순도&문서
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Data Sheet (301 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.1923 mL | 0.9615 mL | 1.9231 mL | 4.8077 mL |
| 5 mM | 0.0385 mL | 0.1923 mL | 0.3846 mL | 0.9615 mL |
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