SR 48692

Pricing Availability Delivery Time Qty
Cat.No. 3721 - SR 48692 | C32H31ClN4O5 | CAS No. 146362-70-1
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)
Datasheet
Citations (6)
Literature

Biological Activity

Neurotensin antagonist; selective for NTS1 over NTS2 (apparent affinity, Ke, 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.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 587.07. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.7 mL 8.52 mL 17.03 mL
5 mM 0.34 mL 1.7 mL 3.41 mL
10 mM 0.17 mL 0.85 mL 1.7 mL
50 mM 0.03 mL 0.17 mL 0.34 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Gully et al (1993) Biochemical and pharmacological profile of a potent and selective nonpeptide antagonist of the neurotensin receptor. Proc.Natl.Acad.Sci.USA 90 65 PMID: 8380498

Oury-Donat et al (1995) 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. 116 1899 PMID: 8528577

Thomas et al (2009) The identification of nonpeptide neurotensin receptor partial agonists from the potent antagonist SR48692 using a calcium mobilization assay. Bioorg.Med.Chem.Lett. 19 1438 PMID: 19195889


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Keywords: SR 48692, supplier, SR48692, neurotensin, nts1, selective, antagonists, Neurotensin, Receptors, Neurotensin, Receptors, Tocris Bioscience

6 Citations for SR 48692

Citations are publications that use Tocris products. Selected citations for SR 48692 include:

Rouibi et al (2016) Ventral Midbrain NTS1 Receptors Mediate Conditioned Reward Induced by the Neurotensin Analog, D-Tyr[11]neurotensin. PLoS One 9 470 PMID: 26733785

Piccart et al (2015) Neurotensin Induces Presynaptic Depression of D2 Dopamine Autoreceptor-Mediated Neurotransmission in Midbrain Dopaminergic Neurons. J Neurosci 35 11144 PMID: 26245975

Bakirtzi et al (2014) The neurotensin-HIF-1α-VEGFα axis orchestrates hypoxia, colonic inflammation, and intestinal angiogenesis. Am J Pathol 184 3405 PMID: 25307345

Toda et al (2014) Maternal separation enhances conditioned fear and decreases the mRNA levels of the neurotensin receptor 1 gene with hypermethylation of this gene in the rat amygdala. PLoS One 9 e97421 PMID: 24831231

Moody et al (2014) SR48692 inhibits non-small cell lung cancer proliferation in an EGF receptor-dependent manner. PLoS One 100 25 PMID: 24496038

Alysandratos et al (2012) Neurotensin and CRH interactions augment human mast cell activation. Life Sci 7 e48934 PMID: 23155429


Do you know of a great paper that uses SR 48692 from Tocris? If so please let us know.

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