| Bioactivity | HDL-16 is a potent P2Y14R antagonist with an IC50 of 0.3095 nM. HDL-16 ameliorates DSS (HY-116282C)-induced colitis through suppressing necroptosis of intestinal epithelium cells (IECs) and protecting mucosal barrier function[1]. |
| Invitro | HDL-16 的苯并恶唑环上的 N 原子与 Tyr102 残基形成氢键，胺基也与 P2Y14R 的结合口袋中的 His184 残基形成氢键相互作用[1]。HDL-16 在 10 μM 浓度下对 HT-29 细胞几乎无细胞毒性[1]。HDL-16 可以抑制 HT-29 细胞的坏死性凋亡 (20 ng/mL TNF-α 加 20 μM z-VAD-fmk (HY-16658B) 和 Smac 模拟物 (BV6，2 μM)；作用 8 小时)[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> HDL-16 相关抗体: |
| In Vivo | HDL-16 (10 μM 或 20 μM；100 μL；直肠给药；每天；6 天) 高剂量的可显着抑制小鼠结肠炎症状，并维持小鼠肠道屏障的完整性[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| CAS | 2373280-36-3 |
| Formula | C14H11BrN2O |
| Molar Mass | 303.15 |
| 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]. Chunxiao Liu, et al. Targeting P2Y14R protects against necroptosis of intestinal epithelial cells through PKA/CREB/RIPK1 axis in ulcerative colitis. Nat Commun. 2024 Mar 7;15(1):2083. |