| Bioactivity | SZM-1209 is an orally active, potent and specific RIPK1 inhibitor, with a Kd of 85 nM. SZM-1209 exhibits high anti-necroptotic activity (EC50=22.4 ± 8.1 nM). SZM-1209 shows anti-SIRS (systemic inflammatory response syndrome), and anti-ALI (acute lung injury) effects[1]. |
| Invitro | SZM-1209 以剂量依赖的方式阻断坏死性凋亡[1]。SZM-1209 (0-1 μM, 6 h) 特异性抑制 RIPK1-RIPK3-MLKL 坏死性凋亡信号的磷酸化[1]。 Western Blot Analysis[1] Cell Line: |
| In Vivo | SZM-1209 (25-100 mg/kg, 灌胃) 在 mTNF-α 诱导的全身炎症反应综合征 (SIRS) 模型中具有显著的抗炎作用，可以逆转小鼠死亡[1]。SZM-1209 (25-100 mg/kg, 腹腔注射) 通过减少肺水肿和病理损伤显着减轻 ALI (急性肺损伤)[1]。 Animal Model: |
| Name | SZM-1209 |
| Formula | C31H29F5N4O5S2 |
| Molar Mass | 696.71 |
| 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]. Zhang X, et al. Targeting Receptor-Interacting Protein Kinase 1 by Novel Benzothiazole Derivatives: Treatment of Acute Lung Injury through the Necroptosis Pathway. J Med Chem. 2023 Apr 13;66(7):5261-5278. |