製品番号: HY-153660

Bivamelagon

Name: Bivamelagon
Brand: MedChemExpress
SKU: HY-153660
Price: 320.00 USD
Availability: InStock
Rating: 5 (1 reviews)

(別名: MC-4R Agonist 2)

カスタマーレビュー

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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度 : 99.19%
CAS 番号: 2641595-54-0
分子式: C₃₅H₅₃ClN₄O₄
分子量:629.27

保管条件:

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

Bivamelagon 構造式

CAS 番号: 2641595-54-0

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
- 臨床実験
化学情報
溶剤 & 溶解度
- 体外
- 体内
プロトコル (1)
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

^[1]

MC4R

65 nM (Ki)

Melanocortin Receptor アイソフォーム固有の製品をすべて表示 :

体外実験

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. Further protocols information, click here.

体内実験

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.

臨床実験

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

化学情報

CAS 番号 2641595-54-0
性状 Solid
分子量 629.27
分子式 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
別名

MC-4R Agonist 2
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

溶剤 & 溶解度

体外:

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.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

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

プロトコル

All Signal Pathway Related

Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (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)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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

Melanocortin Receptor アイソフォーム固有の製品をすべて表示

生物活性

製品説明

IC₅₀ & Target

体外実験

体内実験

臨床実験

化学情報

溶剤 & 溶解度

体外:

体内:

In Vivo Dissolution Calculator

プロトコル

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Bioz

Keywords

最近チェックした製品

Bivamelagon

Melanocortin Receptor アイソフォーム固有の製品をすべて表示

生物活性

製品説明

IC50 & Target

体外実験

体内実験

臨床実験

化学情報

溶剤 & 溶解度

体外:

体内:

In Vivo Dissolution Calculator

プロトコル

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Bivamelagon 関連分類

HY-153660 関連分類

Bioz

Keywords

最近チェックした製品

IC₅₀ & Target