1. Metabolic Enzyme/Protease
  2. Aminotransferases (Transaminases)
  3. BCAT-IN-2

BCAT-IN-2 is a potent, selective and orally active inhibitor of mitochondrial branched-chain aminotransferase (BCATm), with a pIC50 of 7.3. BCAT-IN-2 shows selectivity for BCATm over BCATc (pIC50=6.6). BCAT-IN-2 can be used for the research of obesity and dislipidema.

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BCAT-IN-2

BCAT-IN-2 構造式

CAS 番号 : 1800024-45-6

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 385 在庫あり
Solution
10 mM * 1 mL in DMSO USD 385 在庫あり
Solid
5 mg $350 在庫あり
10 mg $550 在庫あり
25 mg $1150 在庫あり
50 mg $1800 在庫あり
100 mg $2900 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Aminotransferases (Transaminases) アイソフォーム固有の製品をすべて表示:

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

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製品説明

BCAT-IN-2 is a potent, selective and orally active inhibitor of mitochondrial branched-chain aminotransferase (BCATm), with a pIC50 of 7.3. BCAT-IN-2 shows selectivity for BCATm over BCATc (pIC50=6.6). BCAT-IN-2 can be used for the research of obesity and dislipidema[1].

IC50 & Target

pIC50: 7.3 (BCATm), 6.6 (BCATc)[1]

Cellular Effect
Cell Line Type Value Description References
MDA-MB-231 IC50
564 μM
Compound: Cpd A
Upregulation of BCAA expression in human MDA-MB-231 cells
Upregulation of BCAA expression in human MDA-MB-231 cells
[PMID: 36261130]
U-87MG ATCC IC50
5.3 μM
Compound: Cpd A
Upregulation of BCAA expression in human U-87 MG cells
Upregulation of BCAA expression in human U-87 MG cells
[PMID: 36261130]
体外実験

BCAT-IN-2 (compound 61) inhibits BCATm in differentiated primary human adipocyte, with pIC50 of 6.5[1].

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

体内実験

BCAT-IN-2 (compound 61) (10-100 mg/kg; p.o.) increases the level of leucine from 473 μM to 1.2 mM at the dose of 100 mg/kg in mice[1].
BCAT-IN-2 (5 mg/kg for p.o. and 1 mg/kg for i.v.) exhibits a high bioavailability (F=100%), long half-life (t1/2=9.2 h) and low clearance (Cl=0.3 mL/min/kg) in mice[1].

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

分子量

377.78

分子式

C17H14ClF2N5O

CAS 番号
Appearance

Solid

Color

White to yellow

SMILES

N#CC1=C2NC(CCC)=CC(N2N=C1NCC3=C(F)C=C(Cl)C=C3F)=O

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 : 50 mg/mL (132.35 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 2.6470 mL 13.2352 mL 26.4704 mL
5 mM 0.5294 mL 2.6470 mL 5.2941 mL
10 mM 0.2647 mL 1.3235 mL 2.6470 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)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始)

C1

×
体積 (開始)

V1

=
濃度 (終了)

C2

×
体積 (終了)

V2

体内:

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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.62 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.
純度とドキュメンテーション

純度: 99.07%

参考文献

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 2.6470 mL 13.2352 mL 26.4704 mL 66.1761 mL
5 mM 0.5294 mL 2.6470 mL 5.2941 mL 13.2352 mL
10 mM 0.2647 mL 1.3235 mL 2.6470 mL 6.6176 mL
15 mM 0.1765 mL 0.8823 mL 1.7647 mL 4.4117 mL
20 mM 0.1324 mL 0.6618 mL 1.3235 mL 3.3088 mL
25 mM 0.1059 mL 0.5294 mL 1.0588 mL 2.6470 mL
30 mM 0.0882 mL 0.4412 mL 0.8823 mL 2.2059 mL
40 mM 0.0662 mL 0.3309 mL 0.6618 mL 1.6544 mL
50 mM 0.0529 mL 0.2647 mL 0.5294 mL 1.3235 mL
60 mM 0.0441 mL 0.2206 mL 0.4412 mL 1.1029 mL
80 mM 0.0331 mL 0.1654 mL 0.3309 mL 0.8272 mL
100 mM 0.0265 mL 0.1324 mL 0.2647 mL 0.6618 mL
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  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます:C1V1 = C2V2

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

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備考

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Inquiry Information

製品名:
BCAT-IN-2
製品番号:
HY-141669
数量:
MCE 日本正規代理店: