Lintitript
Based on 1 Customer Validation
Lintitript (SR 27897) is a highly potent, selective, orally active, competitive and non-peptide cholecystokinin (CCK1) receptor antagonist with an EC50 of 6 nM and a Ki of 0.2 nM. Lintitript displays > 33-fold selectivity more selective for CCK1 than CCK2 receptors (EC50 value of 200 nM). Lintitript increases plasma concentration of leptin and food intake as well as plasma concentration of insulin.
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: 99.0%
- CAS 番号: 136381-85-6
- 分子式: C20H14ClN3O3S
- 分子量:411.86
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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
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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CCKAR |
In vitro, Lintitript (SR 27897) is a competitive antagonist of cholecystokinin (CCK)-stimulated amylase release in isolated rat pancreatic acini (pA2 = 7.50) and of CCK-induced guinea pig gall bladder contractions (pA2 = 9.57)[1].
Lintitript produces concentration dependent inhibition of [125I]CCK binding to CCK1 receptor sites in the rat pancreas (IC50 value of 0.58 nM) and also to CCK 2 sites in the guinea pig cortex (IC2 value of 479 nM). Lintitript inhibits [125I]gastrin binding to gastrin receptors. Lintitript (0.5 nM) increases the dissociation constant of CCK for the CCK A receptor (Kd = 1.8 to 7.2 nM) without modifying the maximum number of receptors (Bmax = 1800 to 1770 fmol/mg)[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.
化学情報
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CAS 番号 136381-85-6
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性状 Solid
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分子量 411.86
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分子式 C20H14ClN3O3S
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Color White to off-white
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SMILES
O=C(O)CN1C(C(NC2=NC(C3=CC=CC=C3Cl)=CS2)=O)=CC4=C1C=CC=C4
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別名
SR 27897
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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 : 100 mg/mL (242.80 mM; Need ultrasonic; 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 (277 KB)
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SDS (641 KB)
- English - EN (641 KB)
- Français - FR (641 KB)
- Deutsch - DE (641 KB)
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- Español - ES (641 KB)
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- Korean - KR (641 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Gully D, et al. Peripheral biological activity of SR 27897: a new potent non-peptide antagonist of CCKA receptors. Eur J Pharmacol. 1993 Feb 23;232(1):13-9. [Content Brief]
[2]. Gouldson P, et al. Contrasting roles of leu(356) in the human CCK(1) receptor for antagonist SR 27897 and agonist SR 146131 binding. Eur J Pharmacol. 1999 Nov 3;383(3):339-46. [Content Brief]
[3]. Cano V, et al. Regulation of leptin distribution between plasma and cerebrospinal fluid by cholecystokinin receptors. Br J Pharmacol. 2003 Oct;140(4):647-52. [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 | 2.4280 mL | 12.1400 mL | 24.2801 mL | 60.7002 mL |
| 5 mM | 0.4856 mL | 2.4280 mL | 4.8560 mL | 12.1400 mL | |
| 10 mM | 0.2428 mL | 1.2140 mL | 2.4280 mL | 6.0700 mL | |
| 15 mM | 0.1619 mL | 0.8093 mL | 1.6187 mL | 4.0467 mL | |
| 20 mM | 0.1214 mL | 0.6070 mL | 1.2140 mL | 3.0350 mL | |
| 25 mM | 0.0971 mL | 0.4856 mL | 0.9712 mL | 2.4280 mL | |
| 30 mM | 0.0809 mL | 0.4047 mL | 0.8093 mL | 2.0233 mL | |
| 40 mM | 0.0607 mL | 0.3035 mL | 0.6070 mL | 1.5175 mL | |
| 50 mM | 0.0486 mL | 0.2428 mL | 0.4856 mL | 1.2140 mL | |
| 60 mM | 0.0405 mL | 0.2023 mL | 0.4047 mL | 1.0117 mL | |
| 80 mM | 0.0304 mL | 0.1518 mL | 0.3035 mL | 0.7588 mL | |
| 100 mM | 0.0243 mL | 0.1214 mL | 0.2428 mL | 0.6070 mL |
Lintitript 関連分類
HY-101764 関連分類
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