2. GPCR/G Protein Neuronal Signaling
  3. Melanocortin Receptor
  4. PF-07258669

PF-07258669 is an orally active melanocortin-4 receptor (MC4R) antagonist that antagonizes MC4R with an IC50 of 13 nM (Ki=0.46 nM). PF-07258669 can be used for the research of cachexia, anorexia, or anorexia nervosa.

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PF-07258669

PF-07258669 Chemische Struktur

CAS. Nr. : 2755890-53-8

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Based on 1 publication(s) in Google Scholar

Other Forms of PF-07258669:

PF-07258669 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE PF-07258669

Alle Melanocortin Receptor Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen
MC1R MC3R MC2R MC4R MC5R

  • Biologische Aktivität

  • Reinheit & Dokumentation

  • Verweise

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Beschreibung

PF-07258669 is an orally active melanocortin-4 receptor (MC4R) antagonist that antagonizes MC4R with an IC50 of 13 nM (Ki=0.46 nM). PF-07258669 can be used for the research of cachexia, anorexia, or anorexia nervosa[1].

IC50 & Target

MC4R

13 nM (IC50)

MC4R

0.46 nM (Ki)

In Vivo

PF-07258669 (0.3-10 mg/kg, po, twice a day for 22 days) regulates appetite and food intake, increases body weight in aged rats models[2].
PF-07258669 exhibits good pharmacokinetic properties in rats and dogs with an oral bioavailability of 93% in dogs[2].
Pharmacokinetic Analysis of PF-07258669[1]

species Dose (mg/kg) route CLp (mL/min/kg) Vss (L/kg) T1/2 (h) Tmax (h) Cmax (ng/mL) AUCinf (ng·h/mL) AUClast (ng·h/mL)) F (%)
rat 1 iv 21 0.95 1.0 - - 785 780 -
rat 5 oral - - 0.98 0.5 600 1120 1110 28
dog 1 iv 11 1.3 2.3 - - 1660 1640 -
dog 5 oral - - 3.6 0.38 1470 4610 4580 93

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Aged rats models[2]
Dosage: 0.3-10 mg/kg
Administration: po, twice a day for 22 days
Result: Increased daily food intake and body weight.
Klinische Studie
Molekulargewicht

462.52

Formel

C25H27FN6O2
CAS. Nr.
Appearance

Solid

Color

White to off-white

SMILES

CC(N=C(N1)C(CC[C@]21CCN(C([C@H](C)C3=C(C=NC(OC)=C3)F)=O)C2)=C4)=C4C5=NC=CC=N5
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 100 mg/mL (216.21 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 2.1621 mL 10.8103 mL 21.6207 mL
5 mM 0.4324 mL 2.1621 mL 4.3241 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. 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 (5.41 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 (5.41 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).
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. 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 2.1621 mL 10.8103 mL 21.6207 mL 54.0517 mL
5 mM 0.4324 mL 2.1621 mL 4.3241 mL 10.8103 mL
10 mM 0.2162 mL 1.0810 mL 2.1621 mL 5.4052 mL
15 mM 0.1441 mL 0.7207 mL 1.4414 mL 3.6034 mL
20 mM 0.1081 mL 0.5405 mL 1.0810 mL 2.7026 mL
25 mM 0.0865 mL 0.4324 mL 0.8648 mL 2.1621 mL
30 mM 0.0721 mL 0.3603 mL 0.7207 mL 1.8017 mL
40 mM 0.0541 mL 0.2703 mL 0.5405 mL 1.3513 mL
50 mM 0.0432 mL 0.2162 mL 0.4324 mL 1.0810 mL
60 mM 0.0360 mL 0.1802 mL 0.3603 mL 0.9009 mL
80 mM 0.0270 mL 0.1351 mL 0.2703 mL 0.6756 mL
100 mM 0.0216 mL 0.1081 mL 0.2162 mL 0.5405 mL
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PF-07258669 Related Classifications

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.

Keywords:

PF-072586692755890-53-8PF07258669PF 07258669Melanocortin ReceptorMC Receptormelanocortin-4 receptor (MC4)cachexiaanorexiaanorexia nervosaCHOInhibitorinhibitorinhibit

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