2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. Calcium Channel
  4. ABT-639

ABT-639 is a novel, peripherally acting, selective T-type Ca2+ channel blocker.

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ABT-639

ABT-639 構造式

CAS 番号 : 1235560-28-7

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 60 在庫あり
Solution
10 mM * 1 mL in DMSO USD 60 在庫あり
Solid
5 mg $55 在庫あり
10 mg $90 在庫あり
25 mg $210 在庫あり
50 mg $360 在庫あり
100 mg $610 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

This product is a controlled substance and not for sale in your territory.

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Based on 3 publication(s) in Google Scholar

Other Forms of ABT-639:

ABT-639 関連抗体

Top Publications Citing Use of Products

Calcium Channel アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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製品説明

ABT-639 is a novel, peripherally acting, selective T-type Ca2+ channel blocker.

IC50 & Target

T-type calcium channel

 

体内実験

ABT-639 blocks recombinant human T-type (Cav3.2) Ca2+ channels in a voltage-dependent fashion (IC50=2 μM) and attenuates low voltage-activated (LVA) currents in rat DRG neurons (IC50=8 μM). ABT-639 is significantly less active at other Ca2+ channels (e.g. Cav1.2 and Cav2.2) (IC50>30 mM). ABT-639 has high oral bioavailability (%F=73), low protein binding (88.9%) and a low brain:plasma ratio (0.05:1) in rodents. Following oral administration ABT-639 produces dose-dependent antinociception in a rat model of knee joint pain (ED50=2 mg/kg, p.o.). ABT-639 (10-100 mg/kg, p.o.) also increases tactile allodynia thresholds in multiple models of neuropathic pain (e.g. spinal nerve ligation, CCI, and vincristine-induced, and capsaicin secondary hypersensitivity). ABT-639 does not attenuate hyperalgesia in inflammatory pain models induced by complete Freund’s adjuvant or carrageenan. At higher doses (e.g. 100-300 mg/kg) ABT-639 does not significantly alter hemodynamic or psychomotor function. The antinociceptive profile of ABT-639 provides novel insights into the role of peripheral T-type (Cav3.2) channels in chronic pain states[1].

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

455.91

分子式

C20H20ClF2N3O3S
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=CC(C(N2C[C@](CCC3)([H])N3CC2)=O)=C(Cl)C=C1F)(NC4=CC=CC=C4F)=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 : 10 mg/mL (21.93 mM; Need ultrasonic and warming; 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 2.1934 mL 10.9671 mL 21.9342 mL
5 mM 0.4387 mL 2.1934 mL 4.3868 mL
10 mM 0.2193 mL 1.0967 mL 2.1934 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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一般には略語で表示されます：C1V1 = C2V2

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In Vivo Dissolution Calculator
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純度とドキュメンテーション
参考文献
動物実験
[1]

Rats[1]
The pharmacokinetic properties are determined in Sprague Dawley rats dosed intravenously with 5 μmol/kg ABT-639 prepared in 10% DMSO/90% poly ethylene glycol 400 (PEG400). The plasma levels of ABT-639 are determined using HPLC and mass spectrometry. Following oral administration (p.o.) of the ABT-639 (3, 10 and 30 mg/kg) prepared in 10% PEG400/10% Cremophor EL/80% Oleic Acid the levels of ABT-639 in plasma and brain are determined. Briefly, the brains are immediately removed and freed from blood vessels as much as possible. The resulting brain tissues are frozen at -20°C, followed by weighing and homogenization before analysis. The heparinized blood samples are also frozen (-20°C) until analysis. ABT-639 is separated from the blood and brain samples using protein precipitation with acetonitrile followed by quantification with liquid chromatography/mass spectroscopy. Plasma samples for concentration determinations from in vivo efficacy experiments are collected from each animal within 15 min following behavioral testing.

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1934 mL 10.9671 mL 21.9342 mL 54.8354 mL
5 mM 0.4387 mL 2.1934 mL 4.3868 mL 10.9671 mL
10 mM 0.2193 mL 1.0967 mL 2.1934 mL 5.4835 mL
15 mM 0.1462 mL 0.7311 mL 1.4623 mL 3.6557 mL
20 mM 0.1097 mL 0.5484 mL 1.0967 mL 2.7418 mL
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ABT-639 Related Classifications

  • 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.

Keywords:

ABT-6391235560-28-7ABT639ABT 639Calcium ChannelCa2+ channelsCa channelsInhibitorinhibitorinhibit

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製品名:
ABT-639
製品番号:
HY-19721
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