产品
编 号：F741537
分子式：C16H16Cl2N4O2
分子量：367.23
分子式：C16H16Cl2N4O2
分子量：367.23
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CAS No: 2387510-88-3
产品详情
生物活性：
OD36hydrochloride is a RIPK2 inhibitor with an IC50 of 5.3 nM. OD36 hydrochloride is a macrocyclic inhibitor with potent binding to the ALK2 kinase ATP pocket. OD36 hydrochloride shows ALK2-directed activity with KDs of 37 nM.
体内研究：
OD36 (6.25 mg/kg; i.p.; once) alleviates inflammation in an acute peritonitis mice model.Animal Model:C57BL/6 mice, muramyl dipeptide (MDP)-induced model of peritonitis
Dosage:6.25 mg/kg
Administration:Intraperitoneal injection, 30 min prior to MDP
Result:Inhibited the recruitment of inflammatory cells to the peritoneum, specifically that of neutrophils, and, to a lesser extent, lymphocytes. Decreased RIPK2-specific genes as well as inflammatory cytokine and chemokine gene expression.
体外研究：
OD36 also inhibits ALK2 and ALK2 R206H with IC50s of 47 and 22 nM, respevtively.OD36 shows activity against ALK1 with a KD of 90 nM.OD36 potently antagonize mutant ALK2 signaling and osteogenic differentiation.OD36 (0.1-1 μM; 24 h) efficiently inhibits BMP-6 (50 ng/mL)-induced p-Smad1/5 in KS483 cells.Preincubation of fibrodysplasia ossificans progressiva (FOP) endothelial colony-forming cells (ECFCs) with OD36 (0.5 μM) completely prevents the activation of Smad1/5 and gene targets ID-1 and ID-3 in response to activin A.
OD36hydrochloride is a RIPK2 inhibitor with an IC50 of 5.3 nM. OD36 hydrochloride is a macrocyclic inhibitor with potent binding to the ALK2 kinase ATP pocket. OD36 hydrochloride shows ALK2-directed activity with KDs of 37 nM.
体内研究：
OD36 (6.25 mg/kg; i.p.; once) alleviates inflammation in an acute peritonitis mice model.Animal Model:C57BL/6 mice, muramyl dipeptide (MDP)-induced model of peritonitis
Dosage:6.25 mg/kg
Administration:Intraperitoneal injection, 30 min prior to MDP
Result:Inhibited the recruitment of inflammatory cells to the peritoneum, specifically that of neutrophils, and, to a lesser extent, lymphocytes. Decreased RIPK2-specific genes as well as inflammatory cytokine and chemokine gene expression.
体外研究：
OD36 also inhibits ALK2 and ALK2 R206H with IC50s of 47 and 22 nM, respevtively.OD36 shows activity against ALK1 with a KD of 90 nM.OD36 potently antagonize mutant ALK2 signaling and osteogenic differentiation.OD36 (0.1-1 μM; 24 h) efficiently inhibits BMP-6 (50 ng/mL)-induced p-Smad1/5 in KS483 cells.Preincubation of fibrodysplasia ossificans progressiva (FOP) endothelial colony-forming cells (ECFCs) with OD36 (0.5 μM) completely prevents the activation of Smad1/5 and gene targets ID-1 and ID-3 in response to activin A.
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