SB 218795

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Cat.No. 1376 - SB 218795 | C25H20N2O3 | CAS No. 174635-53-1
Description: Potent, selective non-peptide NK3 antagonist
Chemical Name: (R)-[[2-Phenyl-4-quinolinyl)carbonyl]amino]-methyl ester benzeneacetic acid
Purity: ≥99% (HPLC)
Datasheet
Citations (4)
Reviews
Literature

Biological Activity

Potent, selective and competitive non-peptide NK3 receptor antagonist (Ki = 13 nM at hNK3). Displays 90-fold and 7000-fold selectivity over hNK2 and hNK1 receptors respectively. Active in vivo, inhibiting agonist-induced pupillary constriction.

Licensing Information

Sold under license

Compound Libraries

SB 218795 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 396.44
Formula C25H20N2O3
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 174635-53-1
PubChem ID 6604858
InChI Key IUMQXQJZIHWLIN-HSZRJFAPSA-N
Smiles COC(=O)[C@H](NC(=O)C1=C2C=CC=CC2=NC(=C1)C1=CC=CC=C1)C1=CC=CC=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

Solubility Soluble to 100 mM in DMSO and to 5 mM in ethanol

References

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

Giardina et al (1997) Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 1. Identification of the 4-quinolinecarboxamide framework. J.Med.Chem. 40 1794 PMID: 9191956

Medhurst et al (1997) In vitro and in vivo characterization of NK3 receptors in the rabbit eye by use of selective non-peptide NK3 receptor antagonists. Br.J.Pharmacol. 122 469 PMID: 9351503


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Keywords: SB 218795, SB 218795 supplier, Potent, selective, non-peptide, NK3, antagonists, Tachykinin, Receptors, Neurokinin, SB218795, Receptor, 1376, Tocris Bioscience

4 Citations for SB 218795

Citations are publications that use Tocris products. Selected citations for SB 218795 include:

Cunin et al (2011) The tachykinins substance P and hemokinin-1 favor the generation of human memory Th17 cells by inducing IL-1β, IL-23, and TNF-like 1A expression by monocytes. J Immunol 186 4175 PMID: 21368235

Wang et al (2014) Innervation of enteric mast cells by primary spinal afferents in guinea pig and human small intestine. Am J Physiol Gastrointest Liver Physiol 307 G719 PMID: 25147231

Liñán-Rico et al (2015) Neuropharmacology of purinergic receptors in human submucous plexus: Involvement of P2X?, P2X?, P2X? channels, P2Y and A? metabotropic receptors in neurotransmission. Neuropharmacology 95 83 PMID: 25724083

Valero et al (2011) Contractile effect of tachykinins on rabbit small intestine. Acta Pharmacol Sin 32 487 PMID: 21441943


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