1. Membrane Transporter/Ion Channel
  2. Calcium Channel

ACT-709478 

目录号: HY-112723 纯度: 99.68%
产品使用指南

ACT-709478 是一种有效、选择性、可口服、可透过血脑屏障的 T 型电压门控钙通道 (T-type calcium channel) 阻滞剂,对 Cav3.1,Cav3.2,Cav3.3,Cav1.2 的 IC50 值分别为 6.4,18,7.5 和 2410 nM。ACT-709478 对大鼠、小鼠、狗和猕猴的 T-type calcium channel 都有作用,物种差异不大。ACT-709478 可用于全身性癫痫的研究。

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ACT-709478 Chemical Structure

ACT-709478 Chemical Structure

CAS No. : 1838651-58-3

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Size Price Stock Quantity
10 mM * 1 mL in DMSO ¥6050 In-stock
5 mg ¥5500 In-stock
10 mg ¥8500 In-stock
50 mg ¥27500 In-stock
100 mg ¥39500 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Description

ACT-709478 is a potent, selective, orally active, and brain penetrating T-type calcium channel blocker, with IC50s of 6.4, 18, 7.5 and 2410 nM for Cav3.1, Cav3.2, Cav3.3, Cav1.2, respectively. ACT-709478 is effective on rat and mice, dog, and cynomolgus T-type calcium channel, with no significant species differences. ACT-709478 is used in the research of generalized epilepsies[1].

IC50 & Target[1]

Cav3.1

6.4 nM (IC50)

Cav3.2

18 nM (IC50)

Cav3.3

7.5 nM (IC50)

Cav1.2

2410 nM (IC50)

In Vitro

ACT-709478 (Compound 66b) blocks currents through hKv11.1-hERG channels with an IC50 of 5.5 μM[1].
ACT-709478 shows weak inhibition on P450, with IC50s of 52, 14, 22, 25, 15, and 51 μM for P4502A6, 2B6, 2C8, 2C9, 2C19, 2D6 and 3A4, respectively[1].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 125 mg/mL (293.83 mM)

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3507 mL 11.7534 mL 23.5067 mL
5 mM 0.4701 mL 2.3507 mL 4.7013 mL
10 mM 0.2351 mL 1.1753 mL 2.3507 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: ≥ 2.08 mg/mL (4.89 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (4.89 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.89 mM); Clear solution

References
Molecular Weight

425.41

Formula

C₂₂H₁₈F₃N₅O

CAS No.

1838651-58-3

SMILES

O=C(NC1=NN(CC2=NC=C(C#N)C=C2)C=C1)CC3=CC=C(C4(C(F)(F)F)CC4)C=C3

Storage

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

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:
ACT-709478
目录号:
HY-112723
需求量:

ACT-709478

Cat. No.: HY-112723