PG-901
Based on 1 Customer Validation
PG-901 is a selective MC5R agonist and also an MC3R/MC4R antagonist. PG-901 activates the MC5R‑cAMP‑PKA signaling axis in skeletal muscle, mediating increased skeletal muscle glucose uptake and enhanced glycolysis. PG-901 downregulates genes related to pro-hypertrophy, cardiac remodeling, inflammation, and fibrosis, including αSMA, αSKA, TGF-β, IL-6, NOS2, Col3A1, Nppb, and CTGF, and reduces JNK/ERK phosphorylation and cAMP levels. PG-901 synergizes with insulin to increase glucose uptake in myotubes, improves glucose tolerance in wild-type mice, and lowers fasting plasma glucose in MC4R-deficient mice. PG-901 can be used in research related to diseases such as cardiac hypertrophy, heart failure, and diabetes.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.35%
- CAS No.: 322639-20-3
- Formule: C53H71N13O9
- Masse moléculaire:1034.21
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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
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
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MC5R 0.072 nM (EC50) |
MC3R 1.0 nM (Kb) |
MC4R 0.53 nM (Kb) |
IL-6 |
JNK |
In Vitro
PG-901 (10-100 nM) increases glucose uptake in immortalized human LHCN-M2 myotubes in a dose-dependent manner, with 10 and 100 nM producing 2-DG uptake of 344.2 and 393.8 nmol/mg, respectively; at 100 nM, it increases glucose uptake in myotubes derived from primary human vastus lateralis muscle[5].
PG-901 (0.1 nM) prevents Ang II-induced leucine incorporation and attenuates the induction of Tgfb1/Ctgf in H9c2 cells; it inhibits JNK phosphorylation in NMCMs and prevents Ang II-induced leucine incorporation[3].
PG-901 has an EC50 = 0.072 nM for hMC5R; it is also a full antagonist of hMC3R and hMC4R (Kb = 1.0 nM and 0.53 nM, respectively)[7].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:hiPSC-CMs
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Concentration:0.1 nM, 10 nM, 1 μM
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Incubation Time:24 h
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Result:Reduced TGFB1, CTGF, and FN1 mRNA at 0.1 and 10 nM in hiPSC-CMs and downregulated ACTA1 at 1 μM under ET-1 stimulation.
In Vivo
PG-901 (1 µg/g body weight; intraperitoneal injection; single injection; 15 minutes before glucose bolus) improves glucose tolerance in healthy wild-type C57Bl6 mice and does not improve glucose tolerance in MC5R-deficient mice[5].
PG-901 (1 µg/g; intraperitoneal injection; two injections; six-hour interval) lowers fasting blood glucose in MC4R knockout mice and maintains this effect during the two injections spaced six hours apart[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6N (male, 8-week-old)[3]
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Dosage:0.005 mg/kg/day; 0.5 mg/kg/day
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Administration:i.p.; daily; starting 1 week after TAC until sacrifice at 5 weeks after TAC
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Result:Failed to significantly alter TAC-triggered rises in ventricular weight, left ventricular posterior wall thickness or left ventricular dilatation.
Significantly boosted left ventricular ejection fraction at 0.005 mg/kg/day versus vehicle-treated TAC mice.
Preserved mitral valve deceleration time from TAC-mediated decline.
Lessened the extent of left ventricular fibrosis.
Downregulated cardiac expression of Nppa, Mmp2, and Ctgf at 0.005 mg/kg/day.
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Animal Model:C57Bl6 (male, 8 weeks old, healthy or MC5R deficient)[5]
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Dosage:1 µg/g body weight
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Administration:i.p.; single injection; 15 minutes before glucose bolus
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Result:Showed improved glucose tolerance relative to vehicle-treated WT mice.
Reached a plasma glucose level of 22.0 mmol/l at 15 min post glucose bolus, compared with 27.0 mmol/l for vehicle-treated controls.
Reduced plasma glucose iAUC versus vehicle-treated WT mice.
Exhibited no difference in glucose tolerance relative to vehicle-treated MC5R deficient mice.
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Animal Model:loxTB Mc4r, C57BL/6J, Jax: 032518 (male)[5]
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Dosage:1 µg/g
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Administration:i.p.; first injection; second injection six hours later
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Result:Lowered fasting plasma glucose in MC4R knockout mice and maintains this effect over two injections six hours apart.
- Fibrosis/Collagen Morphometry
- Kinase activity and phosphorylation assays
- Collagen: Sirius Red Staining
- Western Blot
- Research Protocol for Endocrine Diseases
- Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
- Research Protocol for Cardiovascular Diseases
- Research Protocol for Inflammation-related Diseases
- Protocol for Kinase activity and phosphorylation assays
- Research Protocol for Metabolic Diseases
- Cardiac Morphometry
Chemical Information
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CAS No. 322639-20-3
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Appearance Solid
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Masse moléculaire 1034.21
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Formule C53H71N13O9
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Color White to off-white
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Sequence
Ac-{Nle}-cyclo(Asp-Pro-{d-Nal}-Arg-Trp-Lys)-NH2
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Sequence Shortening
Ac-{Nle}-cyclo(DP-{d-Nal}-RWK)-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
In Vitro:
DMSO : 100 mg/mL (96.69 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 (2.42 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 (2.42 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 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.
Pureté et documentation
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Fiche technique (299 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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Instruction de manipulation (2659 KB)
Références
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 |
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| DMSO | 1 mM | 0.9669 mL | 4.8346 mL | 9.6692 mL | 24.1730 mL |
| 5 mM | 0.1934 mL | 0.9669 mL | 1.9338 mL | 4.8346 mL | |
| 10 mM | 0.0967 mL | 0.4835 mL | 0.9669 mL | 2.4173 mL | |
| 15 mM | 0.0645 mL | 0.3223 mL | 0.6446 mL | 1.6115 mL | |
| 20 mM | 0.0483 mL | 0.2417 mL | 0.4835 mL | 1.2087 mL | |
| 25 mM | 0.0387 mL | 0.1934 mL | 0.3868 mL | 0.9669 mL | |
| 30 mM | 0.0322 mL | 0.1612 mL | 0.3223 mL | 0.8058 mL | |
| 40 mM | 0.0242 mL | 0.1209 mL | 0.2417 mL | 0.6043 mL | |
| 50 mM | 0.0193 mL | 0.0967 mL | 0.1934 mL | 0.4835 mL | |
| 60 mM | 0.0161 mL | 0.0806 mL | 0.1612 mL | 0.4029 mL | |
| 80 mM | 0.0121 mL | 0.0604 mL | 0.1209 mL | 0.3022 mL |
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