1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  2. Melanocortin Receptor Interleukin Related
  3. PG-901

PG-901 is a full, selective MC5R agonist (EC50 = 0.072 nM for hMC5R). PG-901 is also a full antagonist at the hMC3R and the hMC4R (Kb: 1.0 nM and 0.53 nM, respectively). PG-901 significantly diminishes Cytokines (IL-1α, IL-1β, IL-6). PG-901 increases glucose tolerance, reduces blood glucose, decreases retinal damage.

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Kundenspezifische Peptidsynthese

PG-901

PG-901 Chemische Struktur

CAS. Nr. : 322639-20-3

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Beschreibung

PG-901 is a full, selective MC5R agonist (EC50 = 0.072 nM for hMC5R). PG-901 is also a full antagonist at the hMC3R and the hMC4R (Kb: 1.0 nM and 0.53 nM, respectively). PG-901 significantly diminishes Cytokines (IL-1α, IL-1β, IL-6). PG-901 increases glucose tolerance, reduces blood glucose, decreases retinal damage[1][2][3].

IC50 & Target[1][2][3]

MC5R

0.072 nM (EC50)

MC3R

1.0 nM (Kb)

MC4R

0.53 nM (Kb)

IL-1β

 

IL-1α

 

IL-6

 

Molekulargewicht

1034.21

Formel

C53H71N13O9

CAS. Nr.
Appearance

Solid

Color

White to off-white

Sequence

Ac-{Nle}-cyclo(Asp-Pro-{d-Nal}-Arg-Trp-Lys)-NH2

Sequence Shortening

Ac-{Nle}-cyclo(DP-{d-Nal}-RWK)-NH2

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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)

Lösungsmittel & Löslichkeit
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9669 mL 4.8346 mL 9.6692 mL
5 mM 0.1934 mL 0.9669 mL 1.9338 mL
View the 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.

  • Molaritätsrechner

  • Verdünnungsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Reinheit & Dokumentation
Verweise

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 0.9669 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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Help & FAQs
  • 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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