SZM679
Based on 1 Customer Validation
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).
For research use only. We do not sell to patients.
- Purity: 99.59%
- CAS No.: 3027645-52-6
- Formula: C27H18F5N3O5S
- Molecular Weight:591.51
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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RIPK1 8.6 nM (Kd) |
RIPK3 >5000 nM (Kd) |
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[1].
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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Necrotic HT-29 cells
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Concentration:1 μM
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Incubation Time:6 hours
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Result:Inhibited the phosphorylation of RIPK1 at 1 μM, resulting in the inhibition of the downstream phosphorylation of RIPK3 and MLKL.
SZM679 (1 mg/kg; administered intragastrically; once daily for 7 days) improves cognitive function in STZ-induced AD mice[1].
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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 J mice with TNF-induced SIRS models[1]
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Dosage:10, 20, and 40 mg/kg
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Administration:Intraperitoneal injection
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Result:Protected mice in a dose-dependent manner from hypothermia and death.
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Animal Model:Male C57BL/6 J mice with AD models[1]
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Dosage:1 mg/kg
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Administration:Administered intragastrically; once daily for 7 days
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Result:Improved the anxiety, behavior, and exploratory ability of AD mice.
Improved the learning and memory ability of AD mice.
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Animal Model:Male C57BL/6 J mice with AD models[1]
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Dosage:1 mg/kg
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Administration:Administered intragastrically; once daily for 7 days
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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.
Chemical Information
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CAS No. 3027645-52-6
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Appearance Solid
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Molecular Weight 591.51
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Formula C27H18F5N3O5S
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Color Off-white to light yellow
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SMILES
O=C(C1CC(C1)=O)NC2=NC3=CC(F)=C(OC4=CC=C(F)C(NC(CC5=CC=CC(OC(F)(F)F)=C5)=O)=C4)C=C3S2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 125 mg/mL (211.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.6906 mL | 8.4529 mL | 16.9059 mL | 42.2647 mL |
| 5 mM | 0.3381 mL | 1.6906 mL | 3.3812 mL | 8.4529 mL | |
| 10 mM | 0.1691 mL | 0.8453 mL | 1.6906 mL | 4.2265 mL | |
| 15 mM | 0.1127 mL | 0.5635 mL | 1.1271 mL | 2.8176 mL | |
| 20 mM | 0.0845 mL | 0.4226 mL | 0.8453 mL | 2.1132 mL | |
| 25 mM | 0.0676 mL | 0.3381 mL | 0.6762 mL | 1.6906 mL | |
| 30 mM | 0.0564 mL | 0.2818 mL | 0.5635 mL | 1.4088 mL | |
| 40 mM | 0.0423 mL | 0.2113 mL | 0.4226 mL | 1.0566 mL | |
| 50 mM | 0.0338 mL | 0.1691 mL | 0.3381 mL | 0.8453 mL | |
| 60 mM | 0.0282 mL | 0.1409 mL | 0.2818 mL | 0.7044 mL | |
| 80 mM | 0.0211 mL | 0.1057 mL | 0.2113 mL | 0.5283 mL | |
| 100 mM | 0.0169 mL | 0.0845 mL | 0.1691 mL | 0.4226 mL |
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