1. GPCR/G Protein
    Neuronal Signaling
  2. Dopamine Receptor
  3. A-381393

A-381393 

目录号: HY-116941 纯度: 99.96%
产品使用指南

A-381393 是一种有效、选择性、可透过血脑屏障的 dopamine D4 receptor 拮抗剂,对人 dopamine D4.4,D4.2 和 D4.7 受体的 Ki 值分别为 1.5,1.9 和 1.6 nM,选择性是对 D1,D2,D3,D5 多巴胺受体的 2700 多倍。A-381393 对 5-HT2A 的选择性适中,Ki 值为 370 nM。

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A-381393 Chemical Structure

A-381393 Chemical Structure

CAS No. : 726174-00-1

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Size Price Stock Quantity
10 mM * 1 mL in DMSO ¥209 In-stock
5 mg ¥1900 In-stock
10 mg ¥2900 In-stock
25 mg ¥5900 In-stock
50 mg ¥9900 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Description

A-381393 is a potent, selective, brain penetrate dopamine D4 receptor antagonist, with Kis of 1.5, 1.9 and 1.6 nM for human dopamine D4.4, D4.2, and D4.7 receptor, respectively, >2700-fold selectivity over D1, D2, D3 and D5 dopamine receptors. A-381393 shows moderate affinity for 5-HT2A (Ki, 370 nM)[1].

IC50 & Target

Ki: 1.5 nM (D4.4 receptor), 1.9 nM (D4.2 receptor), 1.6 nM (D4.7 receptor)[1]

In Vitro

A-381393 exhibits weak affinity at 5-HT1A, Sigma 2, Adenoceptor α1A, Adenoceptor α2C, Histamine H1, with Kis of 1365, 8600, 2044, 1912 and 2962 nM, respectively[1].

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 : 51.67 mg/mL (161.25 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1208 mL 15.6040 mL 31.2081 mL
5 mM 0.6242 mL 3.1208 mL 6.2416 mL
10 mM 0.3121 mL 1.5604 mL 3.1208 mL
*请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液。
In Vivo:
  • 1.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.58 mg/mL (8.05 mM); Clear solution

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.58 mg/mL (8.05 mM); Clear solution

  • 3.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.58 mg/mL (8.05 mM); Clear solution

*以上所有助溶剂都可在 MCE 网站选购。
References
Molecular Weight

320.43

Formula

C₂₀H₂₄N₄

CAS No.

726174-00-1

SMILES

CC1=CC=C(C=C1C)N2CCN(CC2)CC3=NC4=CC=CC=C4N3

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)

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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

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产品名称:
A-381393
目录号:
HY-116941
需求量:

A-381393

Cat. No.: HY-116941