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WAY-100635 maleate

WAY-100635 maleate

产品编号 T3453   CAS 634908-75-1

WAY-100635 is a specific and effective 5-HT receptor antagonist (IC50=0.95 nM).

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WAY-100635 maleate Chemical Structure
WAY-100635 maleate, CAS 634908-75-1
规格 价格/CNY 货期 数量
2 mg ¥ 315 现货
5 mg ¥ 483 现货
10 mg ¥ 693 现货
25 mg ¥ 1,130 现货
50 mg ¥ 1,660 现货
100 mg ¥ 2,460 现货
500 mg ¥ 5,930 现货
1 mL * 10 mM (in DMSO) ¥ 625 现货
其他形式的 WAY-100635 maleate:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: WAY-100635 maleate (T3453)
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生物活性
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存储 & 溶解度
参考文献
产品描述 WAY-100635 is a specific and effective 5-HT receptor antagonist (IC50=0.95 nM).
体外活性 在小鼠中,通过静脉给药WAY 100635后,能够选择性结合到脑5-HT1A受体.在小鼠和大鼠体内,WAY 100635(ID50=0.01 mg/kg. s.c)能够阻断8-OH-DPAT诱导的低体温症.
体内活性 WAY 100635所产生的拮抗作用通过增加5-HT的浓度至300 μM,IC50为0.95 nM。
激酶实验 Enzyme activity assay: To determine the IC50 values of HM781-36B for kinase inhibition, enzymes of EGFR, HER2, and HER4 are expressed as recombinant proteins in Sf9 insect cells. Enzyme selectivity screening is then performed using a tyrosine kinase assay kit. Briefly, the reactions are performed in 96 well polystyrene round-bottomed plates containing kinase buffer composed of 100 mM HEPES (pH 7.4), 25 mM MgCl2, 10 mM MnCl2 and 250 μM Na3VO4. The reactions are initiated by the addition of 100 ng/assay enzyme, 100 μM ATP, and 10 ng/mL poly(Glu, Tyr). After 1 h of incubation at room temperature, the reactions are terminated by adding 6 mM EDTA solution and then anti-phosphotyrosine antibody, PTK Green Tracer, and FP dilution buffer mixtures. The fluorescence polarization values are then measured after 30 min at room temperature using a Victor3 microplate reader. Finally, the IC50 values were calculated using the following equation: Y = bottom + (top–bottom)/(1 + 10(X-logIC50)).
细胞实验 Extracellular recordings are made with glass microelectrodes filled with 2 M NaC1 (12 MΩ-15 MΩ). Cells are identified as 5-HT neurons according to the following criteria: biphasic action potentials of 2 msec to 3 msec in duration, slow (0.5 Hz - 2.0 Hz) and regular pattern of discharge. Firing is evoked in the otherwise silent neurons by adding the alpha-l adrenergic agonist phenylephrine (3 μM) to the superfusing ACSF. Baseline activity is recorded for at least 10 minutes before application of the different drugs. The electric signals are fed into a high-input impedance amplifier, an oscilloscope and an electronic ratemeter triggered by individual action potentials connected to an A/D converter and a personal computer. Using dedicated software, the integrated firing rate is recorded, computed and displayed on a chart recorder as consecutive 10-sec samples. The effects of agonists are evaluated by comparing the mean discharge frequency recorded during the 2 minutes that preceded WAY 100635 application with that recorded at the peak of WAY 100635 action (usually 2-5 minutes after the beginning of application). When the agonists are applied in the presence of the antagonist, the effect of the agonist is compared to baseline firing rate and to the frequency recorded during superfusion of the antagonist alone. The antagonist is left to equilibrate for 10 minutes to 25 minutes before retesting of the action of agonists. (Only for Reference)
分子量 N/A
分子式 C25H34N4O2.xC4H4O4
CAS No. 634908-75-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 79 mg/mL (146.7 mM)

DMSO: 79 mg/mL (146.7 mM)

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TargetMol Library Books参考文献

1. Corradetti R, et al. J Pharmacol Exp Ther. 1996, 278(2), 679-688.
Nexopamil racemate Phenylbiguanide Sulamserod Lurasidone Eltoprazine hydrochloride Pancopride Thioridazine hydrochloride Spiroxatrine

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母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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Keywords

WAY-100635 maleate 634908-75-1 GPCR/G Protein Neuroscience 5-HT Receptor WAY 100635 maleate WAY-100635 Maleate WAY 100635 Maleate WAY100635 Maleate WAY100635 maleate Inhibitor inhibitor inhibit

 

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