AZ 10606120 dihydrochloride

Cat. No. 3323 15 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： Potent P2X₇ antagonist

化学名： N-[2-[[2-[(2-Hydroxyethyl)amino]ethyl]amino]-5-quinolinyl]-2-tricyclo[3.3.1.13,7]dec-1-ylacetamide dihydrochloride

纯度： ≥98% (HPLC)

引用文献 (15)

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 AZ 10606120 dihydrochloride

AZ 10606120 dihydrochloride is a potent P2X₇ receptor antagonist (K_D values are 1.4 and 19 nM at human and rat P2X₇ receptors respectively). Binds in a positive cooperative manner to sites distinct from, but coupled to, the ATP binding site and acts as a negative allosteric modulator. Inhibits tumor growth and displays antiangiogenic effects in mice.

许可信息

Sold for research purposes under agreement from AstraZeneca

化合物库 for AZ 10606120 dihydrochloride

AZ 10606120 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。

技术数据 for AZ 10606120 dihydrochloride

分子量	495.48
公式	C₂₅H₃₄N₄O₂.2HCl
储存	Desiccate at RT
纯度	≥98% (HPLC)
CAS Number	607378-18-7
PubChem ID	56972227
InChI Key	BVFONFUUWORSPO-UHFFFAOYSA-N
Smiles	O=C(NC4=C(C=CC(NCCNCCO)=N5)C5=CC=C4)CC1(C3)CC2CC(CC3C2)C1.Cl.Cl

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 AZ 10606120 dihydrochloride

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
	water	12.39	25
	DMSO	49.55	100

制备储备液 for AZ 10606120 dihydrochloride

以下数据基于产品分子量 495.48。 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	2.02 mL	10.09 mL	20.18 mL
5 mM	0.4 mL	2.02 mL	4.04 mL
10 mM	0.2 mL	1.01 mL	2.02 mL
50 mM	0.04 mL	0.2 mL	0.4 mL

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产品说明书 for AZ 10606120 dihydrochloride

分析证书/产品说明书

化学品安全技术说明书

参考文献 for AZ 10606120 dihydrochloride

参考文献是支持产品生物活性的出版物。

Michel et al (2007) Direct labelling of the human P2X₇ receptor and identification of positive and negative cooperativity of binding. Br.J.Pharmacol. 151 103 PMID: 17339830

Michel and Fonfria (2007) Agonist potency at P2X₇ receptors is modulated by structurally diverse lipids. Br.J.Pharmacol. 152 523 PMID: 17700717

Michel et al (2008) Negative and positive allosteric modulators of the P2X₇ receptor. Br.J.Pharmacol. 153 737 PMID: 18071294

Adinolfi et al (2012) Expression of P2X7 receptor increases in vivo tumor growth. Cancer Res. 72 2957 PMID: 22505653

If you know of a relevant reference for AZ 10606120 dihydrochloride, please let us know.

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Purinergic (P2X) Receptors

关键词: AZ 10606120 dihydrochloride, AZ 10606120 dihydrochloride supplier, Potent, P2X7, receptor, antagonists, Receptors, Purinergic, purinoceptors, AZ10606120, dihydrochloride, AstraZeneca, P2X, 3323, Tocris Bioscience

15 篇 AZ 10606120 dihydrochloride 的引用文献

引用文献是使用了 Tocris 产品的出版物。 AZ 10606120 dihydrochloride 的部分引用包括：

Palygin et al (2018) Characterization of purinergic receptor expression in ARPKD cystic epithelia. Purinergic Signal 14 485 PMID: 30417216

Kaiser et al (2014) Tanshinone II A sulfonate, but not tanshinone II A, acts as potent negative allosteric modulator of the human purinergic receptor P2X7. J Pharmacol Exp Ther 350 531 PMID: 24970925

Bhaskaracharya et al (2014) Probenecid blocks human P2X7 receptor-induced dye uptake via a pannexin-1 independent mechanism. PLoS One 9 e93058 PMID: 24671093

Gadeock et al (2012) P2X7 receptor activation mediates organic cation uptake into human myeloid leukaemic KG-1 cells. Mol Biol Cell 8 669 PMID: 22661222

Kowal et al (2015) Bile acid effects are mediated by ATP release and purinergic signalling in exocrine pancreatic cells. Mol Cancer 13 28 PMID: 26050734

Giannuzzo et al (2015) The P2X7 receptor regulates cell survival, migration and invasion of pancreatic ductal adenocarcinoma cells. Purinergic Signal 14 203 PMID: 26607222

Martin et al (2014) IKKα negatively regulates ASC-dependent inflammasome activation. Nat Commun 5 4977 PMID: 25266676

Karmakar et al (2016) Neutrophil P2X₇ receptors mediate NLRP3 inflammasome-dependent IL-1β secretion in response to ATP. Nat.Commun. 7 10555 PMID: 26877061

Russo et al (2016) Active Caspase-1 Induces Plasma Membrane Pores That Precede Pyroptotic Lysis and Are Blocked by Lanthanides The Journal of Immunology 197 1353 PMID: 27385778

Hracskó et al (2011) Lack of neuroprotection in the absence of P2X7 receptors in toxin-induced animal models of Parkinson's disease. Mol Neurodegener 6 28 PMID: 21542899

Allsopp (2017) Unique residues in the ATP gated human P2X7 receptor define a novel allosteric binding pocket for the selective antagonist AZ10606120 Sci Rep 7 PMID: 28389651

Helliwell et al (2015) Selected ginsenosides of the protopanaxdiol series are novel positive allosteric modulators of P2X7 receptors. Br J Pharmacol 172 3326 PMID: 25752193

Fischer et al (2013) Natural compounds with P2X7 receptor-modulating properties. Purinergic Signal 10 313 PMID: 24163006

Nörenberg et al (2012) Positive allosteric modulation by iverm. of human but not murine P2X7 receptors. Br J Pharmacol 167 48 PMID: 22506590

Heinrich et al (2012) K+ depolarization evokes ATP, adenosine and glutamate release from glia in rat hippocampus: a microelectrode biosensor study. Br J Pharmacol 167 1003 PMID: 22394324

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