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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.0%
- CAS. Nr.: 136381-85-6
- Formel: C20H14ClN3O3S
- Molecular Weight:411.86
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Chemical Information
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Biologische Aktivität
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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.
Chemical Information
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CAS. Nr. 136381-85-6
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Appearance Solid
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Molecular Weight 411.86
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Formel 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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Synonyms
SR 27897
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (277 KB)
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SDS (641 KB)
- English - EN (641 KB)
- Français - FR (641 KB)
- Deutsch - DE (641 KB)
- Norwegian - NO (641 KB)
- Español - ES (641 KB)
- Swedish - SV (641 KB)
- Italian - IT (641 KB)
- Korean - KR (641 KB)
- Portuguese - PT (641 KB)
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Handling Instructions (2659 KB)
Verweise
[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 Related Classifications
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