ICA
Based on 1 publication(s) in Google Scholar
ICA (N-(pyridin-2-yl)-4-(pyridin-2-yl)thiazol-2-amine) is a SK channel inhibitor that has antileishmanial activity with an IC50 of 2.1 µM.
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- 純度: 99.92%
- CAS 番号: 3374-88-7
- 分子式: C13H10N4S
- 分子量:254.31
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
MedChemExpress(MCE)の使用を引用している文献 ICA
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生物活性
製品説明
IC50 & Target
IC50: 2.1 µM (Antileishmanial)[1]
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.025 μM
Compound: 1
|
Displacement of [125I]apamin from Kca2.3 channel expressed in HEK293 cells by scintillation proximity assay
Displacement of [125I]apamin from Kca2.3 channel expressed in HEK293 cells by scintillation proximity assay
|
[PMID: 18774291] |
| HEK293 | IC50 |
0.043 μM
Compound: 1
|
Inhibition of Kca2.1 channel expressed in HEK293 cells by thallium flux assay
Inhibition of Kca2.1 channel expressed in HEK293 cells by thallium flux assay
|
[PMID: 18774291] |
| HEK293 | IC50 |
0.123 μM
Compound: 1
|
Inhibition of Kca2.2 channel expressed in HEK293 cells by thallium flux assay
Inhibition of Kca2.2 channel expressed in HEK293 cells by thallium flux assay
|
[PMID: 18774291] |
| HEK293 | IC50 |
0.29 μM
Compound: 1
|
Inhibition of Kca2.3 channel expressed in HEK293 cells by electrophysiology assay
Inhibition of Kca2.3 channel expressed in HEK293 cells by electrophysiology assay
|
[PMID: 18774291] |
| HEK293 | IC50 |
0.543 μM
Compound: 1
|
Inhibition of Kca2.3 channel expressed in HEK293 cells by thallium flux assay
Inhibition of Kca2.3 channel expressed in HEK293 cells by thallium flux assay
|
[PMID: 18774291] |
| HEK293 | IC50 |
0.543 μM
Compound: 1
|
Displacement of [125I]apamin from Kca2.2 channel expressed in HEK293 cells
Displacement of [125I]apamin from Kca2.2 channel expressed in HEK293 cells
|
[PMID: 18774291] |
| Huh-7 | CC50 |
18.63 μM
Compound: GNF-Pf-4773
|
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
|
[PMID: 18579783] |
| J774.A1 | IC50 |
2.1 μM
Compound: 25
|
Antileishmanial activity against Leishmania donovani MHOM/IN/80/Dd8 expressing luciferase reporter gene infected in mouse J-774A1 cells assessed as inhibition of amastigote stage formation incubated for 72 hrs by luminometry
Antileishmanial activity against Leishmania donovani MHOM/IN/80/Dd8 expressing luciferase reporter gene infected in mouse J-774A1 cells assessed as inhibition of amastigote stage formation incubated for 72 hrs by luminometry
|
[PMID: 26318065] |
| KB | CC50 |
75.6 μM
Compound: 25
|
Cytotoxicity in human KB cells assessed as cell viability incubated for 72 hrs by MTT assay
Cytotoxicity in human KB cells assessed as cell viability incubated for 72 hrs by MTT assay
|
[PMID: 26318065] |
体外実験
The SK channel inhibitor ICA exhibits antiarrhythmic effects. ICA prevents electrically induced runs of atrial fibrillation in the isolated right atrium and induces atrial postrepolarization refractoriness and depolarizes resting membrane potential. ICA at 1 to 10 μM slows conduction velocity. At increased pacing frequencies, SK channel inhibition by ICA (10-30 μM) demonstrates prominent depression of other sodium channel-dependent parameters[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 3374-88-7
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性状 Solid
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分子量 254.31
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分子式 C13H10N4S
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Color Light brown to brown
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SMILES
C1(NC2=NC(C3=NC=CC=C3)=CS2)=NC=CC=C1
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別名
N-[4-(2-Pyridinyl)-2-thiazolyl]-2-pyridinamine
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Biomolecules
2025 Feb 1;15(2):202. PMID: 40001505
溶剤 & 溶解度
体外:
DMSO : ≥ 49.5 mg/mL (194.64 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Bhuniya D, et al. Aminothiazoles: Hit to lead development to identify antileishmanial agents. Eur J Med Chem. 2015 Sep 18;102:582-93. [Content Brief]
[2]. Skibsbye L, et al. Antiarrhythmic Mechanisms of SK Channel Inhibition in the Rat Atrium. J Cardiovasc Pharmacol. 2015 Aug;66(2):165-76. [Content Brief]
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 | 3.9322 mL | 19.6610 mL | 39.3221 mL | 98.3052 mL |
| 5 mM | 0.7864 mL | 3.9322 mL | 7.8644 mL | 19.6610 mL | |
| 10 mM | 0.3932 mL | 1.9661 mL | 3.9322 mL | 9.8305 mL | |
| 15 mM | 0.2621 mL | 1.3107 mL | 2.6215 mL | 6.5537 mL | |
| 20 mM | 0.1966 mL | 0.9831 mL | 1.9661 mL | 4.9153 mL | |
| 25 mM | 0.1573 mL | 0.7864 mL | 1.5729 mL | 3.9322 mL | |
| 30 mM | 0.1311 mL | 0.6554 mL | 1.3107 mL | 3.2768 mL | |
| 40 mM | 0.0983 mL | 0.4915 mL | 0.9831 mL | 2.4576 mL | |
| 50 mM | 0.0786 mL | 0.3932 mL | 0.7864 mL | 1.9661 mL | |
| 60 mM | 0.0655 mL | 0.3277 mL | 0.6554 mL | 1.6384 mL | |
| 80 mM | 0.0492 mL | 0.2458 mL | 0.4915 mL | 1.2288 mL | |
| 100 mM | 0.0393 mL | 0.1966 mL | 0.3932 mL | 0.9831 mL |