2. GPCR/G Protein
  3. Bombesin Receptor
  4. MK-5046

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.

For research use only. We do not sell to patients.

MK-5046 Chemical Structure

MK-5046 Chemical Structure

CAS No. : 1022152-70-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 242 In-stock
Solution
10 mM * 1 mL in DMSO USD 242 In-stock
Solid
1 mg USD 100 In-stock
5 mg USD 220 In-stock
10 mg USD 350 In-stock
25 mg USD 690 In-stock
50 mg USD 1100 In-stock
100 mg USD 1650 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 2 publication(s) in Google Scholar

Other Forms of MK-5046:

MK-5046 Related Antibodies

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Description

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[1][2][3].

IC50 & Target

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]
In Vitro

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.

MK-5046 Related Antibodies
In Vivo

MK-5046 (3, 10 and 30 mg/kg; oral administration for once) inhibits food intake, and increases resting metabolic rate (MR) and body temperature in DIO mice[1].
MK-5046 (5, 25 and 50 mg/kg; s.c. once daily for 14 days) significantly reduces body weight and food intake in DIO mice[1].

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

Animal Model: Male C57BL/6N mice with high-fat diet for the diet-induced obese (DIO) model[1]
Dosage: 3, 10 and 30 mg/kg
Administration: Oral administration; 3, 10 and 30 mg/kg for once
Result: Dose-dependently inhibited food intake at 2 h and overnight in DIO mice. But showed no effect on Brs3 knockout mice.
Molecular Weight

444.37

Formula

C20H18F6N4O
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O[C@](CC1=NC(CC2(C(F)(F)F)CC2)=CN1)(C(F)(F)F)C3=CC=C(N4C=CC=N4)C=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2504 mL 11.2519 mL 22.5038 mL
5 mM 0.4501 mL 2.2504 mL 4.5008 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, 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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: ≥ 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.
  • Protocol 2

    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.
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.
Purity & Documentation

Purity: 99.67%

COA (252 KB) LCMS (107 KB)

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, 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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MK-5046 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:

MK-50461022152-70-0MK5046MK 5046Bombesin Receptorselectiveoralallosteric agonistDIObody weightfood intakeobesityInhibitorinhibitorinhibit

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