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P2Y14R antagonist 1 (compound I-17)是一种选择性和高效的P2Y14R拮抗剂(IC50=0.6 nM),具有口服活性和良好生物利用度的优点,抑制单钠尿酸盐诱导的急性痛风性关节炎的炎症反应,通过NLRP3/GSDMD信号通路减少炎症因子释放和细胞焦亡。


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P2Y14R antagonist 1 (compound I-17)是一种选择性和高效的P2Y14R拮抗剂(IC50=0.6 nM),具有口服活性和良好生物利用度的优点,抑制单钠尿酸盐诱导的急性痛风性关节炎的炎症反应,通过NLRP3/GSDMD信号通路减少炎症因子释放和细胞焦亡。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 357 | In Stock | |
| 5 mg | ¥ 833 | In Stock | |
| 10 mg | ¥ 1,320 | In Stock | |
| 25 mg | ¥ 2,660 | In Stock | |
| 50 mg | ¥ 4,280 | In Stock | |
| 100 mg | ¥ 6,350 | In Stock |
P2Y14R antagonist 1 相关产品
| 产品描述 | P2Y14R antagonist 1 (compound I-17) is a selective and potent P2Y14R antagonist (IC50=0.6 nM) with oral activity and good bioavailability that inhibits monosodium urate-induced inflammatory response in acute gouty arthritis by reducing inflammatory factor release via the NLRP3/GSDMD signaling pathway and cellular pyroptosis. |
| 靶点活性 | P2Y14 receptor (HEK293 cells):0.11 nM (Kᴅ), P2Y14 receptor (HEK293 cells):0.60 nM |
| 体外活性 | P2Y14R antagonist 1(compound I-17)在 HEK293 稳转细胞中对 P2Y14R 的 IC₅₀ 为 0.60 nM,BLI 实验表明其与 P2Y14R 结合紧密(K_D = 0.11 nM),且对其他 P2Y 受体无明显抑制[1]。 |
| 体内活性 | SD大鼠口服 P2Y14R antagonist 1(compound I-17)(20 mg/kg),其口服生物利用度为 75%,T₁/₂ = 12.6 h。MSU 急性痛风小鼠模型中,P2Y14R antagonist 1 可显著缓解爪部肿胀、抑制 IL-1β、IL-6、IL-18 表达,减轻关节组织炎细胞浸润和病理损伤,并下调 NLRP3 水平[1]。 |
| 分子量 | 346.18 |
| 分子式 | C15H12BrN3O2 |
| CAS No. | 2728291-29-8 |
| Smiles | O=C(NC=1C=CC=2N=CNC2C1)COC3=CC=C(Br)C=C3 |
| 颜色 | White |
| 物理性状 | Solid |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 40 mg/mL (115.55 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
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