1. Membrane Transporter/Ion Channel
  2. Calcium Channel
  3. ACT-709478

ACT-709478 

目录号: HY-112723 纯度: 99.68%
产品使用指南

ACT-709478 是一种口服有效的,可透过血脑屏障的选择性 T 型电压门控钙通道 (T-type calcium channel) 阻滞剂,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. ACT-709478 is used in the research of generalized epilepsies[1].

IC50 & Target

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 Cav3.1, Cav3.2, Cav3.3, Cav1.2 with IC50s of 6.4, 18, 7.5 and 2410 nM, respectively. ACT-709478 blocks recombinant channel hCav3.3 potently with marked voltage-dependency (Kr≈1500 nM and Ki≈20 nM). ACT-709478 blocks currents through hKv11.1-hERG channels with an IC50 of 5.5 μM[1].
ACT-709478 also inhibits P450 enzymes with IC50s of 14, 15, 22, 25, 51 and 52 μM for CYP2C8,CYP2D6 CYP2C9, CYP2C19, CYP3A4, and CYP2B6, respectively[1].

In Vivo

ACT-709478 (Compound 66b, 100, 300 mg/kg, p.o., 12 hours) potently decreases the cumulative duration of absence-like seizures in mice[1].

Animal Model: Male juvenile DBA/2J mice (22-24 days old)[1]
Dosage: 100, 300 mg/kg, 1 hour or 3 hours before exposure to the stimulus.
Administration: P.O., for 12 hours
Result: Decreased the cumulative duration of absence-like seizures over the next 12 h period by 93%.
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 : ≥ 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
*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    40% PEG300    5% Tween-80    45% saline

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

  • 2.

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

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

  • 3.

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

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

*以上所有助溶剂都可在 MCE 网站选购。
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

Shipping

Room temperature in continental US; may vary elsewhere

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
C1   V1   C2   V2

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Inquiry Information

产品名称:
ACT-709478
目录号:
HY-112723
需求量:

ACT-709478

Cat. No.: HY-112723