SR 142948 dihydrochloride

Name: SR 142948 dihydrochloride
Brand: MedChemExpress
SKU: HY-107664A
Rating: 4.5 (1 reviews)

Cat. No.: HY-107664A Purity: ≥98.0%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

SR 142948 dihydrochloride Chemical Structure

Size	Price	Stock	Quantity
1 mg	USD 160	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 544	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 870	Get quote	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Based on 1 publication(s) in Google Scholar

Other Forms of SR 142948 dihydrochloride:

SR 142948 Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

Description

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.

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
10 mM	0.1318 mL	0.6590 mL	1.3179 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.

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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μL

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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: ≥98.0%

Select Batch:

Data Sheet (274 KB) SDS (251 KB)

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

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

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.