MK-5046
Based on 2 publication(s) in Google Scholar
MK-5046 is a potent, selective and orally active Bombesin receptor subtype-3 (BRS-3) allosteric agonist with an IC50 and an EC50 value of 27 and 25 nM for hBRS-3, respectively. MK-5046 inhibits food intake and reduces body weight of diet-induced obese (DIO) mouse models. MK-5046 can be used for the research of obesity.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.75%
- CAS. Nr.: 1022152-70-0
- Formel: C20H18F6N4O
- Molecular Weight:444.37
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) MK-5046
More
Biologische Aktivität
IC50: 28 nM (human BRS3), 5.4 nM (mouse BRS3), 1.2 nM (rat BRS3), 6.5 nM (dog BRS3), 50 nM (rhesus BRS3)[2]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | EC50 |
14 nM
Compound: 1a
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Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
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[PMID: 25497965] |
| CHO-K1 | EC50 |
21 nM
Compound: 1a
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Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
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[PMID: 25497965] |
MK-5046 shows IC50 values of 28, 5.4, 1.2, 6.5 and 50 nM for BRS3 of human, mouse, rat, dog and rhesus, respectively[2]. MK-5046 exhibits Ki values of 3.4, 1.6, 0.6, 9.9 and 2.4 nM for BRS3 of human, mouse, rat, dog and rhesus, respectively[2]. MK-5046 shows EC50 values of 14, 21, 2.2, 1.6 and 6.9 nM for BRS3 of human, mouse, rat, dog and rhesus, respectively[2]. MK-5046 inhibits diltiazem (DLZ) site of the rabbit calcium ion channel with an IC50 value of 1.9 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6N mice with high-fat diet for the diet-induced obese (DIO) model[1]
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Dosage:3, 10 and 30 mg/kg
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Administration:Oral administration; 3, 10 and 30 mg/kg for once
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Result:Dose-dependently inhibited food intake at 2 h and overnight in DIO mice. But showed no effect on Brs3 knockout mice.
Chemical Information
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CAS. Nr. 1022152-70-0
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Appearance Solid
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Molecular Weight 444.37
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Formel C20H18F6N4O
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Color White to light yellow
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SMILES
O[C@](CC1=NC(CC2(C(F)(F)F)CC2)=CN1)(C(F)(F)F)C3=CC=C(N4C=CC=N4)C=C3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Cell Metab
2021 Jul 6;33(7):1389-1403.e6. PMID: 34038711 -
Cell Rep
Structural insights into ligand recognition, selectivity, and activation of bombesin receptor subtype-3. [Abstract]2024 Jul 17;43(8):114511. PMID: 39024101
Lösungsmittel & Löslichkeit
DMSO : 14.29 mg/mL (32.16 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 1.43 mg/mL (3.22 mM); Clear solution
This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 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: ≥ 1.43 mg/mL (3.22 mM); Clear solution
This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 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.
Reinheit & Dokumentation
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Data Sheet (278 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)
Verweise
[1]. Guan XM, et al. Antiobesity effect of MK-5046, a novel bombesin receptor subtype-3 agonist. J Pharmacol Exp Ther. 2011 Feb;336(2):356-364. [Content Brief]
[2]. Sebhat IK, et al. Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity. ACS Med Chem Lett. 2010 Oct 18;2(1):43-47. [Content Brief]
[3]. Ramos-Alvarez I, et al. The Nonpeptide Agonist MK-5046 Functions As an Allosteric Agonist for the Bombesin Receptor Subtype-3. J Pharmacol Exp Ther. 2022 Aug;382(2):66-78. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2504 mL | 11.2519 mL | 22.5038 mL | 56.2594 mL |
| 5 mM | 0.4501 mL | 2.2504 mL | 4.5008 mL | 11.2519 mL | |
| 10 mM | 0.2250 mL | 1.1252 mL | 2.2504 mL | 5.6259 mL | |
| 15 mM | 0.1500 mL | 0.7501 mL | 1.5003 mL | 3.7506 mL | |
| 20 mM | 0.1125 mL | 0.5626 mL | 1.1252 mL | 2.8130 mL | |
| 25 mM | 0.0900 mL | 0.4501 mL | 0.9002 mL | 2.2504 mL | |
| 30 mM | 0.0750 mL | 0.3751 mL | 0.7501 mL | 1.8753 mL |
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