1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. SKA-121

SKA-121 

目录号: HY-107414 纯度: 99.47%
产品使用指南

SKA-121 是一种选择性的 KCa3.1 激活剂。SKA-121 作用于 KCa3.1KCa2.3EC50 分别为 109 nM 和 4.4 μM。

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SKA-121 Chemical Structure

SKA-121 Chemical Structure

CAS No. : 1820708-73-3

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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

SKA-121 is a selective KCa3.1 activator. SKA-121 exhibits EC50s of 109 nM and 4.4 μM for KCa3.1 and KCa2.3, respectively.

IC50 & Target

EC50: 109 nM (KCa3.1), 4.4 μM (KCa2.3)[1]

体外研究
(In Vitro)

SKA-121, a compound generated through an isosteric replacement approach. SKA-121 is a typical positive-gating modulator and shifts the calcium-concentration response curve of KCa3.1 to the left. SKA-121 displays 41-fold selectivity for KCa3.1 (EC50 109 nM±14 nM) over KCa2.3 (EC50 4.4 ± 1.6 μM). SKA-121 is 200- to 400-fold selective over representative KV (KV1.3, KV2.1, KV3.1, and KV11.1), NaV (NaV1.2, NaV1.4, NaV1.5, and NaV1.7), as well as CaV1.2 channels[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

In blood pressure telemetry experiments, SKA-121 (100 mg/kg i.p.) significantly lowers mean arterial blood pressure in normotensive and hypertensive wild-type but not in KCa3.1-/- mice. SKA-121 can be used as a new KCa3.1 selective pharmacological tool compound despite its relatively short half-life in mice. A lower dose of 30 mg/kg of SKA-121 does not produce significant alterations in MAP. The vehicle, peanut oil/DMSO (9:1 v/v, for SKA-121), does not cause significant alterations in MAP or HR. SKA-121 has a short half-life (~20 minutes), and plasma decay is extremely rapid (21.3±2.4 μM at 5 minutes; 483±231 nM at 1 hour and 53±44 nM at 4 hours). Since SKA-121 is relatively well soluble (logP=1.79) and can potentially be added to drinking water in animal experiments, it orally is also administered, and find that it has an oral availability of roughly 25%[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

198.22

Formula

C12H10N2O

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 42.86 mg/mL (216.22 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 5.0449 mL 25.2245 mL 50.4490 mL
5 mM 1.0090 mL 5.0449 mL 10.0898 mL
10 mM 0.5045 mL 2.5224 mL 5.0449 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;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
Kinase Assay
[1]

To fully evaluate the selectivity of the naphthooxazole SKA-121, seven-point concentration-response curves on KCa2.1, KCa2.2, KCa2.3 and KCa3.1 are determined with 250 nM free Ca2+ in the internal solution[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]
Twelve-week-old male C57Bl/6J mice are used. For i.v. application, SKA-121 is dissolved at 5 mg/mL in a mixture of 10% CremophorEL and 90% phosphate-buffered saline and then injected at 10  mg/kg into the tail vein (n=8 mice per compound). Another group of mice (n=8) receive SKA-121 orally. At various time points after the injection, blood is collected into EDTA blood sample collection tubes either from the saphenous vein or by cardiac puncture under deep isoflurane anesthesia. After the cardiac puncture, mice are sacrificed by cutting the heart, and then the brain is removed. Individual mice are typically used for three times points (two blood collections from the saphenous vein plus the terminal blood collection).

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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产品名称:
SKA-121
目录号:
HY-107414
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