SR 48692

Name: SR 48692
Brand: Tocris Bioscience
SKU: 3721

Tocris Bioscience, part of Bio-Techne | Catalog # 3721

Citations (22)

COA / SDS

Selective non-peptide NTS1 antagonist

Key Product Details

Description:	Selective non-peptide NTS₁ antagonist
Chemical Name:	2-[[[1-(7-Chloro-4-quinolinyl)-5-(2,6-dimethoxyphenyl)-1H-pyrazol-3-yl]carbonyl]amino]-tricyclo[3.3.1.13,7]decane-2-carboxylic acid
Purity:	≥98% (HPLC)
Molecular Weight:	587.07

View Full Technical Details for SR 48692

Technical Data
Citations

Biological Activity for SR 48692

SR 48692 is a neurotensin antagonist; selective for NTS₁ over NTS₂ (apparent affinity, K_e, is 36 nM for NTS₁). Competitively inhibits binding of [¹²⁵I]-neurotensin to HT29 and N1E115 cell membranes (IC₅₀ values are 15.3 and 20.4 nM respectively). Orally bioavailable.

Compound Libraries for SR 48692

SR 48692 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for SR 48692

M. Wt	587.07
Formula	C₃₂H₃₁ClN₄O₅
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	146362-70-1
PubChem ID	119192
InChi Key	DYLJVOXRWLXDIG-UHFFFAOYSA-N
Smiles	O=C(NC5(C(O)=O)C4CC(CC5C6)CC6C4)C2=NN(C(C3=C(OC)C=CC=C3OC)=C2)C1=C(C=CC(Cl)=C7)C7=NC=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for SR 48692

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	11.74	20

Preparing Stock Solutions for SR 48692

The following data is based on the product molecular weight 587.07.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.2 mM	8.52 mL	42.58 mL	85.17 mL
1 mM	1.70 mL	8.52 mL	17.03 mL
2 mM	0.85 mL	4.26 mL	8.52 mL
10 mM	0.17 mL	0.85 mL	1.70 mL

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References for SR 48692

References are publications that support the biological activity of the product.

Oury-Donat Characterization of the effect of SR48692 on inositol monophosphate, cyclic GMP and cyclic AMP responses linked to neurotensin receptor activation in neuronal and non-neuronal cells. Br.J.Pharmacol. 1995 PMID: 8528577
Thomas The identification of nonpeptide neurotensin receptor partial agonists from the potent antagonist SR48692 using a calcium mobilization assay. Bioorg.Med.Chem.Lett. 2009 PMID: 19195889
Gully Biochemical and pharmacological profile of a potent and selective nonpeptide antagonist of the neurotensin receptor. Proc.Natl.Acad.Sci.USA 1993 PMID: 8380498