Chemical Properties | Back Directory | [Boiling point ]
648.941±55.00 °C(Press: 760.00 Torr)(predicted) | [density ]
1.366±0.10 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | [form ]
Solid | [pka]
5.581±0.10(predicted) | [color ]
Light yellow to yellow |
Hazard Information | Back Directory | [Uses]
Zharp2-1 is an oral effective RIPK2 inhibitor, highly associated with inflammatory bowel disease (IBD). Zharp2-1 blocker muramyl dipeptide (MDP) induces growth of mononuclear cells and induces inflammatory cell factor infection. Zharp2-1 attenuates MDP-induced small inguinal peritonitis, or ameliorates by DNBS-induced large inguinal conjunctivitis[1]. | [in vivo]
Zharp2-1 (15 mg/kg; gavage; once daily for 6 days) protects rats from DNBS-induced colon shortening and colon weight gain, protects rats against DNBS-induced diarrhea. Zharp2-1 significantly ameliorates colonic mucosal structural disruption, muscle thickening and inflammatory infiltration[1].
Pharmacokinetic Analysis[1]
| Route | Dose (mg/kg) | T1/2 (h) | Tmax (h) | Cmax (ng·h/mL) | AUC (ng·h/mL) | Vd (L/kg) | Cl (mL/kg/min) | F (%) | Mouse | iv | 2 | 1.2 | | | 2989 | 1.1 | 11.1 | | | po | 10 | | 0.5 | 9610 | 19,236 | | | 129 | Rat | iv | 2 | 1.7 | | | 7889 | 0.6 | 4.2 | | | po | 10 | | 3.3 | 3323 | 18,803 | | | 48 | Dog | iv | 1 | 2.1 | | | 1645 | 1.7 | 9.5 | | | po | 5 | | 0.7 | 2192 | 10,800 | | | 131 |
| [References]
[1] Lai Y, et al. Discovery of a novel RIPK2 inhibitor for the treatment of inflammatory bowel disease. Biochem Pharmacol. 2023 Aug;214:115647. DOI:10.1016/j.bcp.2023.115647 |
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