| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
HDL-16 (10?μM or 20?μM; 100?μL; Rectally administered; daily; 6 days) with high-dose significantly suppresses colitis symptoms and leads to maintained gut barrier integrity in the mice[1].
| Animal Model: | Male, 7-8-week-old, P2Y14Rfl/fl Vil-cre (P2Y14R?IEC), P2Y14Rfl/fl Lyz2-cre and WT mice with C57BL/6?J background[1] | | Dosage: | 10?μM or 20?μM; 100?μL | | Administration: | Rectally administered; daily; 6 days | | Result: | With high-dose showed dramatically less body weight loss and lower Disease Activity Index (DAI) than Dextran sodium sulfate (DSS; 36-50?kDa; 3% w/v; drinking water for 7 days)-exposed mice.
With high-dose improved DSS-induced inflammatory infiltration and tissue damage.
With high-dose resulted in a prominently suppression in necroptosis of the IECs in DSS-treated mice.
|
| [IC 50]
P2Y14 Receptor: 0.3095 nM (IC50) | [References]
[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. DOI:10.1038/s41467-024-46365-x |
|
|