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S8817

Sigma-Aldrich

SB 218795

>98% (HPLC)

Sinónimos:

(−)-(R)-N-(α-Methoxycarbonylbenzyl)-2-phenylquinoline-4-carboxamide

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About This Item

Fórmula empírica (notación de Hill):
C25H20N2O3
Peso molecular:
396.44
MDL number:
MFCD00951240
UNSPSC Code:
12352200
PubChem Substance ID:
24278467

assay

>98% (HPLC)

form

solid

color

white

solubility

DMSO: soluble 40 mg/mL
H2O: insoluble

storage temp.

2-8°C

SMILES string

COC(=O)[C@H](NC(=O)c1cc(nc2ccccc12)-c3ccccc3)c4ccccc4

Gene Information

human ... TACR2(6865) , TACR3(6870)

Application

The pharmacodynamics profile of SB 218795 enables its use as a tool to study physiological and pathophysiological roles of NK-3 receptor in CNS-modulated behaviors.

Biochem/physiol Actions

SB 218795 is a 2-phenyl-4-quinolinecarboxamides and a selective, reversible and competitive antagonist of human NK-3 receptor that effectively crosses the blood-brain barrier. It inhibits the NK-3 receptor-induced miosis or pupil constriction in conscious rabbits.1,2
Non-peptide NK3 tachykinin receptor antagonist.

Legal Information

Sold for research purposes under agreement from Glaxo­Smith­Kline

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)

Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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A D Medhurst et al.
British journal of pharmacology, 122(3), 469-476 (1997-11-14)
1. Inhibition of NK3 receptor agonist-induced contraction in the rabbit isolated iris sphincter muscle was used to assess the in vitro functional activity of three 2-phenyl-4-quinolinecarboxamides, members of a novel class of potent and selective non-peptide NK3 receptor antagonists. In
H M Sarau et al.
The Journal of pharmacology and experimental therapeutics, 295(1), 373-381 (2000-09-19)
The pharmacological and pharmacokinetic profile of SB-222200 [(S)-(-)-N-(alpha-ethylbenzyl)-3-methyl-2-phenylquinoline-4-car boxami de], a human NK-3 receptor (hNK-3R) antagonist, was determined. SB-222200 inhibited (125)I-[MePhe(7)]neurokinin B (NKB) binding to Chinese hamster ovary (CHO) cell membranes stably expressing the hNK-3 receptor (CHO-hNK-3R) with a K(i)
Jin Zhu et al.
Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology, 34(3), 768-780 (2014-08-30)
Activated microglia perform many of the immune effector functions typically associated with macrophages. However, the regulators involved in microglial activation are not well defined. Because microglia play a pivotal role in immune surveillance of the CNS, we studied the effect

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