| Bioactivity | P2Y14R antagonist 1 (compound I-17) is a selective P2Y14R antagonist with an IC50 of 0.6 nM. It exhibits potent P2Y14R antagonistic activity, both in vitro and in vivo efficacy, and favorable pharmacokinetic profiles. P2Y14R antagonist 1 reduces the release of inflammatory factors and cell pyroptosis through the NOD-like receptor family pyrin domain-containing 3 (NLRP3)/gasdermin D (GSDMD) signaling pathway. P2Y14R antagonist 1 holds promise for research in the field of acute gouty arthritis[1]. |
| Invitro | 低于 256 μM 浓度的 P2Y14R antagonist 1 (compound I-17) (2-256 μM, 24小时) 在 RAW264.7 细胞中未显示出显著的细胞毒性[1]。P2Y14R antagonist 1 (10-40 μM, 1 小时) 可以对抗 MSU 和 LPS 的作用，具有抑制痛风性炎症的特性[1]。P2Y14R antagonist 1 (10-40 μM, 1 小时) 作用于 NLRP3 炎症小体组装的上游，抑制了后续的 caspase-1 激活和巨噬细胞焦亡[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> P2Y14R antagonist 1 相关抗体: Cell Viability Assay[1] Cell Line: |
| In Vivo | P2Y14R antagonist 1 (compound I-17) (5-20 mg/mL，腹腔注射，1 小时)能够在 MSU 诱导的小鼠痛风模型中促进由 MSU 晶体注射引起的急性痛风性关节炎的炎症[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| CAS | 2728291-29-8 |
| Formula | C15H12BrN3O2 |
| Molar Mass | 346.18 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Liu W, et al. Discovery of N-Substituted Acetamide Derivatives as Promising P2Y14R Antagonists Using Molecular Hybridization Based on Crystallographic Overlay. J Med Chem. 2024 Jun 27;67(12):10233-10247. |
P2Y14R antagonist 1
CAS: 2728291-29-8 F: C15H12BrN3O2 W: 346.18
P2Y14R antagonist 1 (compound I-17) is a selective P2Y14R antagonist with an IC50 of 0.6 nM. It exhibits potent P2Y14R a
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