1. Metabolic Enzyme/Protease
  2. Cytochrome P450

DMU2139 

目录号: HY-101285
产品使用指南

DMU2139 是有效的特异性细胞色素 cP4501B1 (CYP1B1) 的抑制剂,其对 CYP1B1 和 CYP1A1 的 IC50 值分别为 9,795 nM。

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DMU2139 Chemical Structure

DMU2139 Chemical Structure

CAS No. : 1821143-80-9

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Size Price Stock Quantity
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥1650 In-stock
5 mg ¥1500 In-stock
10 mg ¥2400 In-stock
50 mg ¥7500 In-stock
100 mg ¥12000 In-stock
200 mg   Get quote  
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Description

DMU2139 is a potent and specific CYP1B1 inhibitor, with IC50s of 9, 795 nM for CYP1B1 and CYP1A1, respectively.

IC50 & Target

IC50: 9 nM (CYP1B1), 795 nM (CYP1A1)[1].

In Vitro

DMU2139 (6j) shows 88 and 133-fold selectivity for CYP1B1 over CYP1A1 and CYP1A2. In the presence of DMU2139, the EC50 is reversed back to 8.3 μM from 61 μM (seen in CYP1B1-expressing cells without any inhibitor). The EC50 value, in the presence of DMU2139, resembles the EC50 of cisplatin, 8.7μM, in cells transfected with the empty plasmid which has no CYP1B1 gene and therefore cannot express CYP1B1 protein[1].

Solvent & Solubility
In Vitro: 

DMSO : 77.5 mg/mL (267.86 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4563 mL 17.2813 mL 34.5626 mL
5 mM 0.6913 mL 3.4563 mL 6.9125 mL
10 mM 0.3456 mL 1.7281 mL 3.4563 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.58 mg/mL (8.92 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.58 mg/mL (8.92 mM); Clear solution

References
Molecular Weight

289.33

Formula

C₁₉H₁₅NO₂

CAS No.

1821143-80-9

SMILES

O=C(C1=CC=C2C=C(OC)C=CC2=C1)/C=C/C3=CC=CN=C3

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

Room temperature in continental US; may vary elsewhere

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The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

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

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产品名称:
DMU2139
目录号:
HY-101285
需求量:

DMU2139

Cat. No.: HY-101285