Art. -Nr.: HY-151873

SZM679

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SZM679 is a potent, orally active and selective RIPK1 inhibitor with K_d 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).

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Reinheit: 99.59%
CAS. Nr.: 3027645-52-6
Formel: C₂₇H₁₈F₅N₃O₅S
Molecular Weight:591.51

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

SZM679 Chemical Structure

CAS. Nr.: 3027645-52-6

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Preis

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

RIPK1

8.6 nM (Kd)

RIPK3

>5000 nM (Kd)

Alle RIP kinase Isoform-spezifische Produkte anzeigen :

In Vitro

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.

Western Blot Analysis^[1]

Cell Line:

Necrotic HT-29 cells
Concentration:

1 μM
Incubation Time:

6 hours
Result:

Inhibited the phosphorylation of RIPK1 at 1 μM, resulting in the inhibition of the downstream phosphorylation of RIPK3 and MLKL.

In Vivo

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^[1].
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.

Animal Model:

Male C57BL/6 J mice with TNF-induced SIRS models^[1]
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^[1]
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^[1]
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.

Chemical Information

CAS. Nr. 3027645-52-6
Appearance Solid
Molecular Weight 591.51
Formel C₂₇H₁₈F₅N₃O₅S
Color Off-white to light yellow
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.6906 mL

8.4529 mL

16.9059 mL

5 mM

0.3381 mL

1.6906 mL

3.3812 mL

10 mM

0.1691 mL

0.8453 mL

1.6906 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
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)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Sun Y, et, al. Discovery of a Trifluoromethoxy Cyclopentanone Benzothiazole Receptor-Interacting Protein Kinase 1 Inhibitor as the Treatment for Alzheimer's Disease. J Med Chem. 2022 Nov 10;65(21):14957-14969. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
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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SZM679

Orally Active Compound Library

Anti-Alzheimer's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Multi-Target Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

NF-κB Signaling Compound Library

Anti-Cancer Compound Library

Alle RIP kinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SZM679

Orally Active Compound Library

Anti-Alzheimer's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Multi-Target Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

NF-κB Signaling Compound Library

Anti-Cancer Compound Library

Alle RIP kinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SZM679 Related Classifications

HY-151873 Related Classifications