LY-311727
Based on 1 Customer Validation
LY-311727 is a potent secretory non-pancreatic phospholipase A2 (sPLA2) inhibitor (IC50 <1 μM for group IIA sPLA2). sPLA2 is an important proinflammatory enzyme.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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。
- 純度: 99.73%
- CAS 番号: 164083-84-5
- 分子式: C22H27N2O5P
- 分子量:430.43
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Phospholipase 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
sPLA2[1]
LY-311727 (0.1-10 μM) suppresses the contractile responses induced by human non-pancreatic secretory phospholipase A2 (hnps-PLA2), in a concentration related manner[1].
LY-311727 nearly abolishes the hnps-PLA2 responses at 1 μM, while it failed to suppress porcine pancreatic PLA2 concentration response curves at the same concentration[1].
LY-311727 displays 1,500-fold selectivity when assayed against porcine pancreatic s-PLA2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice, Mt-sPLA2 transgenic mice model[2]
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Dosage:3 mg/kg, 10 mg/kg, 30 mg/kg
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Administration:Intravenous injection
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Result:Significantly and dose dependently suppressed the PLA2 activity in the serum.
化学情報
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CAS 番号 164083-84-5
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性状 Solid
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分子量 430.43
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分子式 C22H27N2O5P
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Color White to off-white
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SMILES
NC(CC1=C(CC)N(CC2=CC=CC=C2)C3=C1C=C(OCCCP(O)(O)=O)C=C3)=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 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : ≥ 30 mg/mL (69.70 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, 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 (273 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]. R W Schevitz, et al. Structure-based design of the first potent and selective inhibitor of human non-pancreatic secretory phospholipase A2. Nat Struct Biol. 1995 Jun;2(6):458-65. [Content Brief]
[2]. N Fox, et al. Transgenic model for the discovery of novel human secretory non-pancreatic phospholipase A2 inhibitors. Eur J Pharmacol. 1996 Jul 18;308(2):195-203. [Content Brief]
[3]. M Murakami, et al. The functions of five distinct mammalian phospholipase A2S in regulating arachidonic acid release. Type IIa and type V secretory phospholipase A2S are functionally redundant and act in concert with cytosolic phospholipase A2. J Biol Chem. 1998 Jun 5;273(23):14411-23. [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 | 2.3233 mL | 11.6163 mL | 23.2326 mL | 58.0815 mL |
| 5 mM | 0.4647 mL | 2.3233 mL | 4.6465 mL | 11.6163 mL | |
| 10 mM | 0.2323 mL | 1.1616 mL | 2.3233 mL | 5.8081 mL | |
| 15 mM | 0.1549 mL | 0.7744 mL | 1.5488 mL | 3.8721 mL | |
| 20 mM | 0.1162 mL | 0.5808 mL | 1.1616 mL | 2.9041 mL | |
| 25 mM | 0.0929 mL | 0.4647 mL | 0.9293 mL | 2.3233 mL | |
| 30 mM | 0.0774 mL | 0.3872 mL | 0.7744 mL | 1.9360 mL | |
| 40 mM | 0.0581 mL | 0.2904 mL | 0.5808 mL | 1.4520 mL | |
| 50 mM | 0.0465 mL | 0.2323 mL | 0.4647 mL | 1.1616 mL | |
| 60 mM | 0.0387 mL | 0.1936 mL | 0.3872 mL | 0.9680 mL |