2. GPCR/G Protein Neuronal Signaling
  3. Neurotensin Receptor
  4. SR 142948 dihydrochloride

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.

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SR 142948 dihydrochloride Chemical Structure

SR 142948 dihydrochloride Chemical Structure

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1 mg USD 160 In-stock
5 mg USD 544 In-stock
10 mg USD 870 In-stock
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Based on 1 publication(s) in Google Scholar

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SR 142948 dihydrochloride Related Antibodies

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Description

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[1][2].

In Vitro

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 dihydrochloride Related Antibodies
In Vivo

SR 142948 (2 µg/kg; p.o.; single) dihydrochloride inhibits the turning behavior induced by NT (10 pg/mouse)[2].
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.

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.
Molecular Weight

758.77

Formula

C39H53Cl2N5O6
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (65.90 mM; Need ultrasonic)

DMSO : 10 mg/mL (13.18 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3179 mL 6.5896 mL 13.1792 mL
5 mM 0.2636 mL 1.3179 mL 2.6358 mL
View the 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 98.6%

COA (249 KB) Elemental Analysis Report (107 KB)

Handling Instructions (2659 KB)
References

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 / H2O 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
H2O 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

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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SR 142948 dihydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SR 142948SR142948SR-142948Neurotensin ReceptorOrallyneurotensin receptorNTh-NTR1-CHOHT-29inositol monophosphatehypothermiaanalgesiasteeringblood-brain permeabilitypsychiatric disordersInhibitorinhibitorinhibit

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