EMPA

Cat. No. 4558 4 篇引用文献提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Highly potent and selective OX₂ antagonist; brain penetrant

化学名： N-Ethyl-2-[(6-methoxy-3-pyridinyl)[(2-methylphenyl)sulfonyl]amino]-N-(3-pyridinylmethyl)-acetamide

纯度： ≥98% (HPLC)

引用文献 (4)

文献 (1)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 for EMPA

EMPA is a highly potent, selective OX₂ receptor antagonist (IC₅₀ values are 2.3 nM and 1900 nM for OX₂ and OX₁ respectively). Displays negligible or no inhibition of a panel of 80 receptors. Blocks orexin-B- and orexin-A-invoked calcium mobilization in hOX₂-expressing CHO cells (IC₅₀ values are 7.9 nM and 8.8 nM respectively); reverses orexin-B-induced hyperlocomotion in mice. Brain penetrant.

技术数据 for EMPA

分子量	454.54
公式	C₂₃H₂₆N₄O₄S
储存	Store at -20°C
纯度	≥98% (HPLC)
CAS Number	680590-49-2
PubChem ID	9981404
InChI Key	KJPHTXTWFHVJIG-UHFFFAOYSA-N
Smiles	O=C(CN(C2=CN=C(OC)C=C2)S(C3=C(C)C=CC=C3)(=O)=O)N(CC)CC1=CN=CC=C1

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

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

溶解性数据 for EMPA

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
	DMSO	45.45	100
	ethanol	22.73	50

制备储备液 for EMPA

以下数据基于产品分子量 454.54。 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.

浓度/溶剂体积/质量	1 mg	5 mg	10 mg
1 mM	2.2 mL	11 mL	22 mL
5 mM	0.44 mL	2.2 mL	4.4 mL
10 mM	0.22 mL	1.1 mL	2.2 mL
50 mM	0.04 mL	0.22 mL	0.44 mL

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产品说明书 for EMPA

分析证书/产品说明书

化学品安全技术说明书

参考文献 for EMPA

参考文献是支持产品生物活性的出版物。

Malherbe et al (2009) Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX₂ receptor. Br.J.Pharmacol. 156 1326 PMID: 19751316

Mochizuki et al (2011) Orexin receptor 2 expression in the posterior hypothalamus rescues sleepiness in narcoleptic mice. Proc.Natl.Acad.Sci.U.S.A 108 4471 PMID: 21368172

Malherbe et al (2010) Mapping the binding pocket of dual antagonist almorexant to human orexin 1 and orexin 2 receptors: comparison with the selective OX1 antagonist SB-674042 and the selective OX2 antagonist N-ethyl-2-[(6-methoxy-pyridin-3-yl)-(toluene- Mol.Pharmacol. 78 81 PMID: 20404073

If you know of a relevant reference for EMPA, please let us know.

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关键词: EMPA, EMPA supplier, supplier, orexin, 2, receptor, OX2, antagonists, inhibits, potent, selective, hyperlocomotion, brain, penetrant, Receptor, 4558, Tocris Bioscience

4 篇 EMPA 的引用文献

引用文献是使用了 Tocris 产品的出版物。 EMPA 的部分引用包括：

Ralph J et al (2020) Orexin signaling in GABAergic lateral habenula neurons modulates aggressive behavior in male mice. Nat Neurosci 23 638-650 PMID: 32284606

Beig et al (2015) Both Ox1R and Ox2R orexin receptors contribute to the cardiorespiratory response evoked from the perifornical hypothalamus. Clin.Exp.Pharmacol.Physiol. 42 1059 PMID: 26174505

Jennifer J et al (2021) Orexin receptor antagonists reverse aberrant dopamine neuron activity and related behaviors in a rodent model of stress-induced psychosis. Transl Psychiatry 11 114 PMID: 33558469

Guerreiro et al (2015) The sleep-modulating peptide orexin-B protects midbrain DA neurons from degeneration, alone or in cooperation with nicotine. Mol.Pharmacol. 87 525 PMID: 25552485

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