Bivamelagon hydrochloride (Synonyms: MC-4R Agonist 2 hydrochloride)

Cat. No.: HY-153660A: Data Sheet Handling Instructions
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Bivamelagon (MC-4R Agonist 2) hydrochloride is an orally active and BBB-penetrable 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 hydrochloride can be used for the research of diseases such as obesity and diabetes.

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

Bivamelagon hydrochloride Chemical Structure

CAS No. : 2641595-55-1

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Other In-stock Forms of Bivamelagon hydrochloride:

Bivamelagon

Other Forms of Bivamelagon hydrochloride:

Bivamelagon In-stock

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target^[1]

MC4R

65 nM (Ki)

In Vitro

Bivamelagon (Example 1) (90 min) hydrochloride 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) hydrochloride 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.

Molecular Weight

665.73

Formula

C₃₅H₅₄Cl₂N₄O₄

CAS No.

2641595-55-1

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.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

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

Bivamelagon hydrochloride Related Classifications

Metabolic Disease

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The molarity calculator equation

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

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The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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:

Bivamelagon2641595-55-1MC-4R Agonist 2Melanocortin ReceptorMC Receptorobesity modelU2OS cellsInhibitorinhibitorinhibit

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