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Synonyms: SR 48692


| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 1 mg | $113 | In Stock | In Stock | |
| 2 mg | $198 | In Stock | In Stock | |
| 5 mg | $430 | In Stock | In Stock | |
| 10 mg | $833 | In Stock | In Stock | |
| 25 mg | $923 | In Stock | In Stock |
| Description | Meclinertant (SR 48692) is a small-molecule compound and a neurotensin receptor-1 (NTSR1) antagonist with good selectivity and cell permeability. This compound can be used to study neurotensin signaling pathways and related neurological diseases, and serves as a potential diagnostic and therapeutic probe targeting NTSR1-positive tumors. |
| Targets & IC50 | NTS2:20.4 nM, NTS1:5.6 nM |
| In vitro | Methods: Using extracellular recording techniques on rat dorsal raphe nucleus brain slices, the samples were pretreated with Meclinertant (SR 48692) (100 nM–1 μM) for 20 minutes to 2 hours. Results: Meclinertant (SR 48692) caused a concentration-dependent rightward shift in the concentration-response curve for NT, selectively blocking the excitation of serotonergic neurons induced by NT (1 μM) without affecting the response to phenylephrine. [1] |
| In vivo | Methods: In a mouse turning model induced by unilateral striatal injection of neurotensin (10 pg), Meclinertant (SR 48692) (80 μg/kg, oral, Tween 80 solvent) was pretreated for 30 min; in a rat hyperlocomotion model induced by amphetamine with neurotensin injection into the nucleus accumbens, Meclinertant (SR 48692) (0.1–1 mg/kg, oral) was pretreated. Results: Meclinertant (SR 48692) significantly antagonized turning behavior in mice, and dose-dependently reversed the inhibitory effect of neurotensin on amphetamine-induced hyperlocomotion.[2] |
| Synonyms | SR 48692 |
| Molecular Weight | 587.07 |
| Formula | C32H31ClN4O5 |
| Cas No. | 146362-70-1 |
| Smiles | O=C(O)C1(NC(=O)C2=NN(C=3C=CN=C4C=C(Cl)C=CC43)C(=C2)C=5C(OC)=CC=CC5OC)C6CC7CC(C6)CC1C7 |
| Relative Density. | 1.50 g/cm3 |
| Storage | Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 20 mg/mL (34.07 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 µL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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