| Field | Specification |
|---|---|
| Applications | |
| Molecular weight | |
| Molecular formula | C39H53Cl2N5O6 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
SR 142948 dihydrochloride is an orally active, selective, non-peptide antagonist of the neurotensin receptor (NT), with IC50 values of 1.19 nM, 0.32 nM and 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively, and it antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. It blocks NT-induced hypothermia, analgesia and steering behavior in vivo, shows blood-brain permeability, and can be used to study psychiatric disorders[1][2]. It is supplied as a white to off-white solid (C39H53Cl2N5O6, MW 758.77) at 99.07% purity.
Physical & Chemical Properties
| Molecular Formula | C39H53Cl2N5O6 |
|---|---|
| Molecular Weight | 758.77 g/mol |
| Purity | 99.07% |
| Appearance | Solid |
| Color | White to off-white |
| 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 |
| Signaling Pathway | GPCR/G Protein; Neuronal Signaling |
| Solubility | In Vitro: 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. |
| Storage | 4°C, sealed storage, away from moisture. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | ≥ 100 mg/mL (131.79 mM) | use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); sealed storage, away from moisture; avoid repeated freeze-thaw cycles.
Data provided by the manufacturer.
In Vitro
SR 142948 dihydrochloride (1 μM; 90 min) inhibits c-fos and krox24 expression in CHO-hNT1-R cells[1]. SR 142948 dihydrochloride (0-1 μM; 1 h) shows good antagonistic activity, inhibiting binding of [125I-Tyr3]NT to membranes from h-NTR1-CHO (IC50 1.19 nM) and HT 29 (IC50 0.32 nM) cells[2]. SR 142948 dihydrochloride (0-1 μM; 30 min) antagonizes NT-stimulated IP1 production in both h-NTR1-CHO and HT 29 cells in a concentration-dependent manner[2]. SR 142948 dihydrochloride (1, 10 nM; 60-80 s) antagonizes NT-stimulated intracellular calcium mobilization in h-NTR1-CHO cells[2].
In Vivo
SR 142948 dihydrochloride (2 μg/kg; p.o.; single) inhibits NT (10 pg/mouse)-induced turning behavior[2]. SR 142948 dihydrochloride (0.01, 0.03, 0.3 mg/kg; i.p.; single) dose-dependently prevents the increase in ACh release produced by NT (100 nM)[2]. NT-induced hypothermia is partially but significantly blocked by SR 142948 dihydrochloride (0-10 mg/kg; p.o.; single) (in rats, 53% at 2 mg/kg; in mice, 54% at 4 mg/kg)[2].
| Animal Model | Female Swiss albino CD1 mice (25-30 g; intrastriatal injection of 10 pg/mouse NT)[2] |
|---|---|
| Dosage | 2 μg/kg |
| Administration | Oral administration; single |
| Result | Inhibited the turning behavior with maximal and significant antagonism between 1-2 h after administration. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Res Sq. 2026 Jun 2.
