SR 142948 dihydrochloride
Based on 1 publication(s) in Google Scholar
SR 142948 dihydrochloride is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 dihydrochloride antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 dihydrochloride blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 dihydrochloride shows blood-brain permeability and can be used in study of psychiatric disorders.
For research use only. We do not sell to patients.
- Purity: 99.07%
- Formula: C39H53Cl2N5O6
- Molecular Weight:758.77
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) SR 142948 dihydrochloride
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Biological Activity
SR 142948 (1 µM; 90 min) dihydrochloride inhibits expression of c-fos and krox24 in CHO-hNT1-R cells[1].
SR 142948 (0-1 µM; 1 h) dihydrochloride exhibits good antagonistic activity by inhibiting [125I-Tyr3]NT binds to h-NTR1-CHO and HT 29 cell membranes, with IC50s of 1.19 and 0.32 nM, respectively[2].
SR 142948 (0-1 µM; 30 min) dihydrochloride antagonizes production of IP1 stimulated by NT both in h-NTR1-CHO and HT 29 cells, in a concentration-dependent manner[2].
SR 142948 (1, 10 nM; 60-80 s) dihydrochloride antagonizes intracellular calcium mobilization stimulated by NT in h-NTR1-CHO cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
SR 142948 (0.01, 0.03, 0.3 mg/kg; i.p.; single) dihydrochloride prevents the enhancement of ACh release produced by NT (100 nM), in a dose-dependent manner[2].
SR 142948 (0-10 mg/kg; p.o.; single) dihydrochloride partially but significantly blocks NT-induced hypothermia (53% at 2 mg/kg in rats and 54% at 4 mg/kg in mice)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Swiss albino CD1 mice (25-30 g; intrastriatal injection of 10 pg/mouse NT)[2]
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Dosage:2 µg/kg
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Administration:Oral administration; single
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Result:Inhibited the turning behavior with maximal and significant antagonism between 1-2 h after administration.
Chemical Information
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Appearance Solid
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Molecular Weight 758.77
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Formula C39H53Cl2N5O6
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Color White to off-white
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SMILES
O=C(C1=NN(C2=C(C=C(C(N(C)CCCN(C)C)=O)C=C2)C(C)C)C(C3=C(C=CC=C3OC)OC)=C1)NC4([C@H]5C[C@H](C6)C[C@@H]4C[C@H]6C5)C(O)=O.[H]Cl.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
DMSO : ≥ 100 mg/mL (131.79 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (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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Handling Instructions (2659 KB)
References
[1]. M Portier, et al. neurotensin antagonists SR Neurotensin type 1 receptor-mediated activation of krox24, c-fos and Elk-1: preventing effect of the 48692 and SR 142948. FEBS Lett. 1998 Jul 31;432(1-2):88-93. [Content Brief]
[2]. D Gully, et al. Biochemical and pharmacological activities of SR 142948A, a new potent neurotensin receptor antagonist. J Pharmacol Exp Ther. 1997 Feb;280(2):802-12. [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 (sealed storage, away from moisture). 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 | 1.3179 mL | 6.5896 mL | 13.1792 mL | 32.9481 mL |
| 5 mM | 0.2636 mL | 1.3179 mL | 2.6358 mL | 6.5896 mL | |
| 10 mM | 0.1318 mL | 0.6590 mL | 1.3179 mL | 3.2948 mL | |
| 15 mM | 0.0879 mL | 0.4393 mL | 0.8786 mL | 2.1965 mL | |
| 20 mM | 0.0659 mL | 0.3295 mL | 0.6590 mL | 1.6474 mL | |
| 25 mM | 0.0527 mL | 0.2636 mL | 0.5272 mL | 1.3179 mL | |
| 30 mM | 0.0439 mL | 0.2197 mL | 0.4393 mL | 1.0983 mL | |
| 40 mM | 0.0329 mL | 0.1647 mL | 0.3295 mL | 0.8237 mL | |
| 50 mM | 0.0264 mL | 0.1318 mL | 0.2636 mL | 0.6590 mL | |
| 60 mM | 0.0220 mL | 0.1098 mL | 0.2197 mL | 0.5491 mL | |
| 80 mM | 0.0165 mL | 0.0824 mL | 0.1647 mL | 0.4119 mL | |
| 100 mM | 0.0132 mL | 0.0659 mL | 0.1318 mL | 0.3295 mL |
SR 142948 dihydrochloride Related Classifications
HY-107664A Related Classifications
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