BAY-1797是一种高效、口服活性的选择性 P2X4 拮抗剂,对人 P2X4 的 IC50 为 211 nM。BAY-1797 在其他 P2X 离子通道上没有或表现出极弱的活性,具有抗伤害和抗炎作用。
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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]. |
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 |
CAS号 | 2055602-83-8 |
分子式 | C20H17ClN2O4S |
分子量 | 416.878 |
别名 | |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place,Sealed in dry,Room Temperature |
溶解方案 |
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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |