化學(xué)名

4-[2-[[7-amino-2-(furan-2-yl)-[1,2,4]triazolo[1,5-a][1,3,5]triazin-5-yl]amino]ethyl]phenol

簡(jiǎn)稱(chēng)

ZM241385

別名

ZM 241385, ZM-241385

中文名

N/A

化學(xué)式

C₁₆H₁₅N₇O₂

分子量

337.34

CAS號(hào)

139180-30-6

純度

98%

溶劑/溶解度

Water<1mg/ml; DMSO67mg/ml; Ethanol<1mg/ml

溶液配制

5mg加入1.48ml DMSO，或者每3.37mg加入1ml DMSO，配制成10mM溶液。SD2407-10mM用DMSO配制。

產(chǎn)品描述

ZM-241385 is a high affinity antagonist ligand selective for the adenosine A2A receptor.

信號(hào)通路

GPCR & G Protein

靶點(diǎn)

adenosine A2A receptor

－

－

－

－

IC50

－

－

－

－

－

體外研究

ZM 241385 has high affinity for A2a receptors. In rat phaeochromocytoma cell membranes, ZM 241385 displaces binding of tritiated 5'-N-ethylcarboxamidoadenosine (NECA) with a pIC50 of 9.52. ZM241385 delays the appearance of anoxic depolarization (AD), a phenomenon strictly related to cell damage and death, protect from the synaptic activity depression brought about by a severe (7 min) OGD period, and protect CA1 neuron and astrocyte from injury.

體內(nèi)研究

ZM-241385 significantly blunts the hypotensive effects of CCPA and NECA without altering the bradycardia induced by these agonists. It blocks the infarct size-reducing effects(cardioprotective effects) of this two distinct adenosine receptor agonists.

臨床實(shí)驗(yàn)

N/A

特征

N/A

酶活性檢測(cè)實(shí)驗(yàn)

方法

N/A

細(xì)胞實(shí)驗(yàn)

細(xì)胞系

PC12 cells

濃度

1μM

處理時(shí)間

24h

方法

Nitric oxide (NO) production is assessed by measuring the amount of nitrite, a stable metabolic product of NO that provides an indirect measurement of NO, by using the Griess diazotization reaction. Briefly, 24h after incubation with 1.0μM CG21680 or 1.0μM ZM241385 or exposure to SMF, samples of medium (150μl) are collected from cells and mixed with 130μl dH₂O and with 20μl Griess reagent using instruction supplied by the manufacturer. After a 30 min incubation period at room temperature, the samples are evaluated spectrophotometrically at 548nM and OD values-in comparison with a standard curve is determined in culture medium by using serial dilutions of sodium nitrite-represented total stable metabolites of NO.

動(dòng)物實(shí)驗(yàn)

動(dòng)物模型

Adult Sprague-Dawley rats

配制

10% DMSO in 1ml normal saline

劑量

1.5mg/kg

給藥方式

i.v.

產(chǎn)品編號(hào)

產(chǎn)品名稱(chēng)

包裝

SD2407-10mM

ZM241385 (Adenosine Receptor抑制劑)

10mM×0.2ml

SD2407-5mg

ZM241385 (Adenosine Receptor抑制劑)

5mg

SD2407-25mg

ZM241385 (Adenosine Receptor抑制劑)

25mg

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說(shuō)明書(shū)

1份