PF-07258669
Based on 1 publication(s) in Google Scholar
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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- Purity: 98.44%
- CAS No.: 2755890-53-8
- 화학식: C25H27FN6O2
- 분자량:462.52
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) PF-07258669
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Biological Activity
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MC4R 13 nM (IC50) |
MC4R 0.46 nM (Ki) |
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.
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Animal Model:Aged rats models[2]
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Dosage:0.3-10 mg/kg
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Administration:po, twice a day for 22 days
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Result:Increased daily food intake and body weight.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2755890-53-8
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Appearance Solid
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분자량 462.52
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화학식 C25H27FN6O2
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Color White to off-white
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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
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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J Neuroinflammation
A microglial LCN2-MC4R signaling axis drives silica-induced neuronal damage via C1q release. [Abstract]2026 Jan 23;23(1):70. PMID: 41578331
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (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.
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.
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.
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 (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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. 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 | 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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