产品
编 号：F756855
分子式：C31H29F5N4O5S2
分子量：696.71
分子式：C31H29F5N4O5S2
分子量：696.71
产品类型
规格
价格
是否有货
结构图
CAS No: 2919801-86-6
产品详情
生物活性：
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.
体内研究：
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。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)。Animal Model:C57BL/6J mice (female, 6-8 weeks old, mTNF-α (intravenous injection)-induced SIRS model)
Dosage:25, 50, and 100 mg/kg
Administration:Intragastric administration
Result:Dose-dependently improved survival rates of the SIRS mice to 30, 90, and 100%. Could effectively protect against mTNFα-induced SIRS in vivo. Serum levels of IL-6 and IL-1β were significantly decreased.
Animal Model:C57BL/6J mice (female, 6-8 weeks old, NNK (HY-126477) (65 mg/kg) short-term intratracheal exposure-induced ALI model)
Dosage:25, 50, and 100 mg/kg
Administration:IP
Result:Exhibited lower levels of IL-6 and TNF-α in BALF than those of model mice. Inhibited the expression of inflammatory genes of IL-6 and TNF-α in lung tissues of mice at a mRNA level. Significant reduced phosphorylation of RIPK1, and also completely blocked at a high dose of 100 mg/kg in lung tissue of ALI model mice.
体外研究：
SZM-1209 以剂量依赖的方式阻断坏死性凋亡。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。
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.
体内研究：
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。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)。Animal Model:C57BL/6J mice (female, 6-8 weeks old, mTNF-α (intravenous injection)-induced SIRS model)
Dosage:25, 50, and 100 mg/kg
Administration:Intragastric administration
Result:Dose-dependently improved survival rates of the SIRS mice to 30, 90, and 100%. Could effectively protect against mTNFα-induced SIRS in vivo. Serum levels of IL-6 and IL-1β were significantly decreased.
Animal Model:C57BL/6J mice (female, 6-8 weeks old, NNK (HY-126477) (65 mg/kg) short-term intratracheal exposure-induced ALI model)
Dosage:25, 50, and 100 mg/kg
Administration:IP
Result:Exhibited lower levels of IL-6 and TNF-α in BALF than those of model mice. Inhibited the expression of inflammatory genes of IL-6 and TNF-α in lung tissues of mice at a mRNA level. Significant reduced phosphorylation of RIPK1, and also completely blocked at a high dose of 100 mg/kg in lung tissue of ALI model mice.
体外研究：
SZM-1209 以剂量依赖的方式阻断坏死性凋亡。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。
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备