This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
SZM679
Catalog No. T73511 CAS
T73511
SZM679 is an orally active, selective RIPK1 inhibitor displaying potent affinity with a dissociation constant (Kd) of 8.6 nM for RIPK1, while exhibiting minimal activity towards RIPK3, with a Kd of <5000 nM. It effectively counteracts tumor necrosis factor-induced systemic inflammation, reduces Tau hyperphosphorylation, diminishes neuroinflammation, and lowers RIPK1 phosphorylation in the hippocampus and cortex. SZM679 is utilized in Alzheimer’s disease (AD) research [1].
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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
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Biological Description
Chemical Properties
Storage
& Solubility Information
Description
SZM679 is an orally active, selective RIPK1 inhibitor displaying potent affinity with a dissociation constant (Kd) of 8.6 nM for RIPK1, while exhibiting minimal activity towards RIPK3, with a Kd of >5000 nM. It effectively counteracts tumor necrosis factor-induced systemic inflammation, reduces Tau hyperphosphorylation, diminishes neuroinflammation, and lowers RIPK1 phosphorylation in the hippocampus and cortex. SZM679 is utilized in Alzheimer’s disease (AD) research [1].
Targets&IC50
RIPK1:8.6 nM (Kd), RIPK3:>5000 nM (Kd)
In vitro
SZM679 exhibits anti-necrosis activity in necrotic L929 and HT-29 cells by inhibiting the RIPK1 pathway, with an EC50 value of 2 nM after exposure at concentrations of 0-10 μM for 24 hours. Additionally, SZM679 confers protection against necroptosis prompted by TNF-α, cycloheximide, and z-VAD-fmk (TCZ), demonstrating dose-dependent efficacy. In necrotic HT-29 cells, a 1 μM dose of SZM679 administered for 6 hours selectively suppresses RIPK1 expression without affecting RIPK3 or MLKL levels, and impedes necrosome assembly by blocking TSZ-triggered phosphorylation of RIPK1 [1].
In vivo
SZM679 (10-40 mg/kg; i.p.; male C57BL/6 J mice with TNF-induced SIRS models) confers in vivo protection against necroptosis-specific, TNF-induced systemic inflammatory response syndrome (SIRS) [1]. Moreover, at a dosage of 1 mg/kg delivered intragastrically once daily for a week, SZM679 enhances cognitive function in STZ-induced Alzheimer's disease (AD) mice, mitigates brain structure damage, reduces AD biomarkers, and suppresses inflammatory cytokine expression, along with inhibiting RIPK1 phosphorylation in brain tissue, all without apparent toxicity [1].
Molecular Weight
591.51
Formula
C27H18F5N3O5S
CAS No.
T73511
Storage
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Method for preparing DMSO master liquid: mg
drug pre-dissolved in μL DMSO (Master liquid concentration
mg/mL),
Method for preparing in vivo formulation:Take μL
DMSO master liquid, next add μL PEG300, mix and clarify, next add μL
Tween 80,mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation:Take μL
DMSO master liquid, next add μL Corn oil,mix and clarify.
Note:
Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.