BayCysLT2
Based on 1 Customer Validation
BayCysLT2, an isophthalic acid derivative, is a selective and potent cysteinyl leukotriene 2 (CysLT2) receptor antagonist with an IC50 value of 53 nM. BayCysLT2 inhibits calcium mobilization induced by leukotriene D4 in HEK293 cells expressing human CysLT2 receptors. BayCysLT2 reverses LTC4-induced increases in coronary artery perfusion pressure and decreases in contractility in isolated perfused guinea pig hearts.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 712313-33-2
- 分子式: C34H39NO8
- 分子量:589.68
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Leukotriene Receptor アイソフォーム固有の製品をすべて表示
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生物活性
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
>2.5 μM
Compound: BayCysLT2
|
Antagonist activity at human CysLT1 receptor expressed in CHO cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
Antagonist activity at human CysLT1 receptor expressed in CHO cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
|
[PMID: 25408836] |
| HEK293 | IC50 |
>2.5 μM
Compound: BayCyLT2
|
Antagonist activity against CysLT1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
Antagonist activity against CysLT1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
|
[PMID: 26985325] |
| HEK293 | IC50 |
0.053 μM
Compound: BayCyLT2
|
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
|
[PMID: 26985325] |
| HEK293 | IC50 |
0.053 μM
Compound: BayCysLT2
|
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
|
[PMID: 25408836] |
化学情報
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CAS 番号 712313-33-2
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性状 Solid
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分子量 589.68
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分子式 C34H39NO8
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Color White to off-white
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SMILES
OC(C1=CC=C(OCCCC2=CC=C(C=C2)OCCCCOC3=CC=CC=C3)C(C(NC4CC(C(O)=O)CCC4)=O)=C1)=O
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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 In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 20 mg/mL (33.92 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (269 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Michael Harter, et al. Isophtalic acid derivatives. US20060154912A1. 2009 March 03.
[2]. Ni NC, et al. A selective cysteinyl leukotriene receptor 2 antagonist blocks myocardial ischemia/reperfusion injury and vascular permeability in mice. J Pharmacol Exp Ther. 2011 Dec;339(3):768-78. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6958 mL | 8.4792 mL | 16.9584 mL | 42.3959 mL |
| 5 mM | 0.3392 mL | 1.6958 mL | 3.3917 mL | 8.4792 mL | |
| 10 mM | 0.1696 mL | 0.8479 mL | 1.6958 mL | 4.2396 mL | |
| 15 mM | 0.1131 mL | 0.5653 mL | 1.1306 mL | 2.8264 mL | |
| 20 mM | 0.0848 mL | 0.4240 mL | 0.8479 mL | 2.1198 mL | |
| 25 mM | 0.0678 mL | 0.3392 mL | 0.6783 mL | 1.6958 mL | |
| 30 mM | 0.0565 mL | 0.2826 mL | 0.5653 mL | 1.4132 mL |