产品
编 号：F762897
分子式：C27H18F5N3O5S
分子量：591.51
分子式：C27H18F5N3O5S
分子量：591.51
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 3027645-52-6
产品详情
生物活性：
SZM679 is a potent, orally active and selective RIPK1 inhibitor with Kd values of 8.6 nM and >5000 nM for RIPK1 and RIPK3, respectively. SZM679 reverses the tumor necrosis factor-induced systemic inflammatory response. SZM679 decreases the Tau hyperphosphorylation, neuroinflammation, and the RIPK1 phosphorylation level in the hippocampus and cortex. SZM679 can be used in research of Alzheimer's disease (AD).
体内研究：
SZM679 (10-40 mg/kg; i.p.; male C57BL/6 J mice with TNF-induced SIRS models) protects against necroptosis-specific TNF-induced systemic inflammatory response syndrome (SIRS) in vivo.SZM679 (1 mg/kg; administered intragastrically; once daily for 7 days) improves cognitive function in STZ-induced AD mice.SZM679 (1 mg/kg; administered intragastrically; once daily for 7 days) rescues brain structure damage with no obvious toxicity and decreases AD biomarkers and decreases the expression levels of inflammatory cytokines and inhibits RIPK1 phosphorylation in the brain tissues of AD mice.Animal Model:Male C57BL/6 J mice with TNF-induced SIRS models
Dosage:10, 20, and 40 mg/kg
Administration:Intraperitoneal injection
Result:Protected mice in a dose-dependent manner from hypothermia and death.
Animal Model:Male C57BL/6 J mice with AD models
Dosage:1 mg/kg
Administration:Administered intragastrically; once daily for 7 days
Result:Improved the anxiety, behavior, and exploratory ability of AD mice.Improved the learning and memory ability of AD mice.
Animal Model:Male C57BL/6 J mice with AD models
Dosage:1 mg/kg
Administration:Administered intragastrically; once daily for 7 days
Result:Rescued the damaged hippocampal structure of AD mice and restored the cell number and morphology.Down-regulated the expression of the inflammatory cytokines, the IL-1β and TNF-α levels.
体外研究：
SZM679 (0-10 μM; 24 h; necrotic L929 and HT-29 cells) has an anti-necrosis activity by Inhibiting the RIPK1 pathway with an EC50 value of 2 nM. SZM679 also protects against TNF-α, cycloheximide, and z-VAD-fmk (TCZ)-induced necroptosis. SZM679 protects against necroptosis induced by TZ in a dose dependent manner.SZM679 (1 μM; 6 h; necrotic HT-29 cells) selectively inhibits the expression of RIPK1 but not RIPK3 or MLKL. SZM679 blocks necrosome formation by inhibiting TSZ-induced phosphorylation of RIPK1.
SZM679 is a potent, orally active and selective RIPK1 inhibitor with Kd values of 8.6 nM and >5000 nM for RIPK1 and RIPK3, respectively. SZM679 reverses the tumor necrosis factor-induced systemic inflammatory response. SZM679 decreases the Tau hyperphosphorylation, neuroinflammation, and the RIPK1 phosphorylation level in the hippocampus and cortex. SZM679 can be used in research of Alzheimer's disease (AD).
体内研究：
SZM679 (10-40 mg/kg; i.p.; male C57BL/6 J mice with TNF-induced SIRS models) protects against necroptosis-specific TNF-induced systemic inflammatory response syndrome (SIRS) in vivo.SZM679 (1 mg/kg; administered intragastrically; once daily for 7 days) improves cognitive function in STZ-induced AD mice.SZM679 (1 mg/kg; administered intragastrically; once daily for 7 days) rescues brain structure damage with no obvious toxicity and decreases AD biomarkers and decreases the expression levels of inflammatory cytokines and inhibits RIPK1 phosphorylation in the brain tissues of AD mice.Animal Model:Male C57BL/6 J mice with TNF-induced SIRS models
Dosage:10, 20, and 40 mg/kg
Administration:Intraperitoneal injection
Result:Protected mice in a dose-dependent manner from hypothermia and death.
Animal Model:Male C57BL/6 J mice with AD models
Dosage:1 mg/kg
Administration:Administered intragastrically; once daily for 7 days
Result:Improved the anxiety, behavior, and exploratory ability of AD mice.Improved the learning and memory ability of AD mice.
Animal Model:Male C57BL/6 J mice with AD models
Dosage:1 mg/kg
Administration:Administered intragastrically; once daily for 7 days
Result:Rescued the damaged hippocampal structure of AD mice and restored the cell number and morphology.Down-regulated the expression of the inflammatory cytokines, the IL-1β and TNF-α levels.
体外研究：
SZM679 (0-10 μM; 24 h; necrotic L929 and HT-29 cells) has an anti-necrosis activity by Inhibiting the RIPK1 pathway with an EC50 value of 2 nM. SZM679 also protects against TNF-α, cycloheximide, and z-VAD-fmk (TCZ)-induced necroptosis. SZM679 protects against necroptosis induced by TZ in a dose dependent manner.SZM679 (1 μM; 6 h; necrotic HT-29 cells) selectively inhibits the expression of RIPK1 but not RIPK3 or MLKL. SZM679 blocks necrosome formation by inhibiting TSZ-induced phosphorylation of RIPK1.
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