2. GPCR/G Protein Neuronal Signaling
  3. Melanocortin Receptor
  4. Bivamelagon

Bivamelagon  (Synonyms: MC-4R Agonist 2)

Cat. No.: HY-153660 Purity: 99.19%
COA
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Handling Instructions Technical Support

Bivamelagon (MC-4R Agonist 2) is an orally active MC4R agonist with EC50 values of 0.562 nM (Luci assay) and 36.5 nM (cAMP assay), and a Ki of 65 nM. Bivamelagon can be used for the research of diseases such as obesity and diabetes.

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

Bivamelagon

Bivamelagon Chemical Structure

CAS No. : 2641595-54-0

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Based on 1 publication(s) in Google Scholar

Other Forms of Bivamelagon:

Bivamelagon Related Antibodies

Top Publications Citing Use of Products

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MC1R MC3R MC2R MC4R MC5R

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Description

Bivamelagon (MC-4R Agonist 2) is an orally active MC4R agonist with EC50 values of 0.562 nM (Luci assay) and 36.5 nM (cAMP assay), and a Ki of 65 nM. Bivamelagon can be used for the research of diseases such as obesity and diabetes[1].

IC50 & Target[1]

MC4R

65 nM (Ki)

In Vitro

Bivamelagon (Example 1) (90 min) exhibits β-arrestin recruitment activity in U2OS cells expressing MC4R and β-arrestin, with an EC50 value of 4.6 nM[1].

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

Bivamelagon Related Antibodies
In Vivo

Pharmacokinetic Analysis in C57BL6[1]

Route Dose (mg/kg) Cmax (ng/mL) AUCinf (ng·hr/mL) t1/2 (hr)
Plasma p.o. 10 232.3 2067.0 3.9
Brain p.o. 10 49.1 1495.3 19.0

Bivamelagon (10-30 mg/kg; oral administration; 16 days) exhibits weight-loss activity in a mouse obesity model[1].

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

Animal Model: C57BL/6 male mice (5 weeks old) treated fat diet[1]
Dosage: 10 and 30 mg/kg
Administration: Oral administration; 16 days
Result: Caused a 9.4% inhibition of weight gain compared to the vehicle control group at 10 mg/kg.
Caused a 15.1% inhibition of weight gain compared to the vehicle control group at 30 mg/kg.
Clinical Trial
Molecular Weight

629.27

Formula

C35H53ClN4O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@H]1[C@H](C2=CC=C(C=C2)Cl)CN(C1)C(C)(C)C)N3[C@@H](C[C@@H](C3)N([C@@H]4CC[C@@H](CC4)C)C(C(C)C)=O)C(N5CCOCC5)=O
Shipping

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

DMSO : 100 mg/mL (158.91 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 1.5891 mL 7.9457 mL 15.8914 mL
5 mM 0.3178 mL 1.5891 mL 3.1783 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.

  • Molarity Calculator

  • Dilution Calculator

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: ≥ 5 mg/mL (7.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (7.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Purity & Documentation

Purity: 99.50%

SDS (252 KB)

COA (260 KB) HNMR (276 KB) LCMS (87 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, 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 1.5891 mL 7.9457 mL 15.8914 mL 39.7286 mL
5 mM 0.3178 mL 1.5891 mL 3.1783 mL 7.9457 mL
10 mM 0.1589 mL 0.7946 mL 1.5891 mL 3.9729 mL
15 mM 0.1059 mL 0.5297 mL 1.0594 mL 2.6486 mL
20 mM 0.0795 mL 0.3973 mL 0.7946 mL 1.9864 mL
25 mM 0.0636 mL 0.3178 mL 0.6357 mL 1.5891 mL
30 mM 0.0530 mL 0.2649 mL 0.5297 mL 1.3243 mL
40 mM 0.0397 mL 0.1986 mL 0.3973 mL 0.9932 mL
50 mM 0.0318 mL 0.1589 mL 0.3178 mL 0.7946 mL
60 mM 0.0265 mL 0.1324 mL 0.2649 mL 0.6621 mL
80 mM 0.0199 mL 0.0993 mL 0.1986 mL 0.4966 mL
100 mM 0.0159 mL 0.0795 mL 0.1589 mL 0.3973 mL
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Bivamelagon 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:

Bivamelagon2641595-54-0MC-4R Agonist 2Melanocortin ReceptorMC Receptorobesity modelU2OS cellsInhibitorinhibitorinhibit

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