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BAY-1797 99%+

货号:A1364936 Ambeed 开学季,买赠积分,赢豪礼

BAY-1797 化学结构 CAS号:2055602-83-8
BAY-1797 化学结构
CAS号:2055602-83-8
BAY-1797 3D分子结构
CAS号:2055602-83-8
BAY-1797 化学结构 CAS号:2055602-83-8
BAY-1797 3D分子结构 CAS号:2055602-83-8
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BAY-1797 纯度/质量文件 产品仅供科研

货号:A1364936 标准纯度: 99%+
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BAY-1797 生物活性

描述 BAY-1797 is a potent, orally bioavailable, and selective antagonist of P2X4, exhibiting an IC50 of 211 nM against human P2X4. It has little to no activity on other P2X ion channels. BAY-1797 demonstrates anti-nociceptive and anti-inflammatory properties[1].
体内研究

BAY-1797 (12.5-50 mg/kg; pO.) significantly increases PGE2 levels in the inflamed paw within the mouse Complete Freund’s Adjuvant (CFA) inflammatory pain model[1].

BAY-1797 (50 mg/kg; once daily for multiple pO. administrations) significantly lowers the load on the ipsilateral paw 24 and 48 hours post Complete Freund’s Adjuvant (CFA) injection[1].

Under BAY-1797 treatment, the normalized area under the curve (AUCnorm), steady-state volume of distribution (Vss), and half-life (t1/2) are reported as 1.06 kg h/L, 3.67 L/kg, and 2.64 hours, respectively[1].

体外研究

BAY-1797 blocks P2X4 in 1321N1 cells across human, mouse, and rat species, showing IC50 values of 108 nM, 112 nM, and 233 nM, respectively[1].

BAY-1797 shows no significant activity against hERG and carbonic anhydrase II (both IC50 >10 μM). Additionally, when assessed against a variety of non-target entities such as G-protein coupled receptors (GPCRs), ion channels, kinases, and transporters at 10 μM, the only observed inhibitory effect was on the dopamine transporter (DAT, with an IC50 of 2.17 μM)[1].

BAY-1797 参考文献

[1]Werner S, et al. Discovery and Characterization of the Potent and Selective P2X4 Inhibitor N-[4-(3-Chlorophenoxy)-3-sulfamoylphenyl]-2-phenylacetamide (BAY-1797) and Structure-Guided Amelioration of Its CYP3A4 Induction Profile. J Med Chem. 2019 Dec 26;62

BAY-1797 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.40mL

0.48mL

0.24mL

11.99mL

2.40mL

1.20mL

23.99mL

4.80mL

2.40mL

BAY-1797 技术信息

CAS号2055602-83-8
分子式C20H17ClN2O4S
分子量 416.878
别名
运输蓝冰
存储条件

粉末 Keep in dark place,Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 250 mg/mL(599.7 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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