Cat. No.: HY-153660

Bivamelagon

(Synonyms: MC-4R Agonist 2)

Customer Review

Based on 1 Customer Validation

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 K_i 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.

Purity: 99.19%
CAS No.: 2641595-54-0
Formula: C₃₅H₅₃ClN₄O₄
Molecular Weight:629.27

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Bivamelagon Chemical Structure

CAS No.: 2641595-54-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

MC4R

65 nM (Ki)

All Melanocortin Receptor Isoforms :

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.

In Vivo

Pharmacokinetic Analysis in C57BL6^[1]

	Route	Dose (mg/kg)	C_max (ng/mL)	AUC_inf (ng·hr/mL)	t_1/2 (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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 2641595-54-0
Appearance Solid
Molecular Weight 629.27
Formula C₃₅H₅₃ClN₄O₄
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
Synonyms

MC-4R Agonist 2
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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.5891 mL

7.9457 mL

15.8914 mL

5 mM

0.3178 mL

1.5891 mL

3.1783 mL

10 mM

0.1589 mL

0.7946 mL

1.5891 mL

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (7.95 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Seung Wan Kang, et al. Melanocortin-4 receptor agonists. Patent WO2021091283A1. 2021-05-14.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

All Melanocortin Receptor Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Bivamelagon

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

All Melanocortin Receptor Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Bivamelagon Related Classifications

HY-153660 Related Classifications