OD36 是一种RIPK2抑制剂，IC50为 5.3 nM。OD36 是一种大环抑制剂，可与ALK2激酶 ATP 口袋有效结合。OD36 靶向作用于 ALK2，KD为 37 nM。
| 生物活性 | OD36 is aRIPK2inhibitor with anIC50of 5.3 nM. OD36 is a macrocyclic inhibitor with potent binding to theALK2kinase ATP pocket. OD36 shows ALK2-directed activity withKDs of 37 nM[1][2]. |
| IC50& Target[1][2] | RIPK2 5.3 nM (IC50) | ACVR1 37 nM (Kd) | ACVR1 47 nM (IC50) | ALK2 R206H 22 nM (IC50) |
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体外研究
(In Vitro) | OD36 also inhibits ALK2 and ALK2 R206H with IC50s of 47 and 22 nM, respevtively[1].
OD36 shows activity against ALK1 with a KDof 90 nM[2].
OD36 potently antagonize mutant ALK2 signaling and osteogenic differentiation[2].
OD36 (0.1-1 μM; 24 h) efficiently inhibits BMP-6 (50 ng/mL)-induced p-Smad1/5 in KS483 cells[2].
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[2].
Western Blot Analysis[2] | Cell Line: | KS483 cells | | Concentration: | 0.1, 0.2, and 1 μM | | Incubation Time: | | | Result: | Inhibited BMP-6 induced p-Smad1/5. |
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体内研究
(In Vivo) | OD36 (6.25 mg/kg; i.p.; once) alleviates inflammation in an acute peritonitis mice model[3].
| Animal Model: | C57BL/6 mice, muramyl dipeptide (MDP)-induced model of peritonitis[3] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 33.33 mg/mL(100.76 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 3.0232 mL | 15.1162 mL | 30.2325 mL | | 5 mM | 0.6046 mL | 3.0232 mL | 6.0465 mL | | 10 mM | 0.3023 mL | 1.5116 mL | 3.0232 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
