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Chemical Structure| 4311-88-0 Chemical Structure| 4311-88-0

Structure of Necrostatin-1
CAS No.: 4311-88-0

Chemical Structure| 4311-88-0

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CAS No.: 4311-88-0

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Necrostatin-1 is an inhibitor of RIP1 and can decrease TNF-α-induced necroptosis with EC50 of 490 nM.

Synonyms: Nec-1

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Product Details of Necrostatin-1

CAS No. :4311-88-0
Formula : C13H13N3OS
M.W : 259.33
SMILES Code : CN1C(NC(CC2=CNC3=C2C=CC=C3)C1=O)=S
Synonyms :
Nec-1
MDL No. :MFCD00056916
InChI Key :TXUWMXQFNYDOEZ-UHFFFAOYSA-N
Pubchem ID :2828334

Safety of Necrostatin-1

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H317
Precautionary Statements:P280

Related Pathways of Necrostatin-1

pyroptosis

Isoform Comparison

Biological Activity

Target
  • TNF-α

    RIP1, EC50:490 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
BMDMs 50 μM 3 h Inhibition of necroptosis, reducing hypoxia-induced cell death PMC8329871
THP-1 cells 30 μM 1 h To evaluate the inhibitory effect of Necrostatin-1 on necroptosis in THP-1 cells. The results showed that Necrostatin-1 completely inhibited HMGB1 release, supporting the major contribution of necrotic cell death in VEXAS. PMC10828464
Astrocytes 30 μM 4 h To evaluate the effect of RIPK1 kinase activity on inflammatory gene expression in astrocytes. Results showed that Nec-1s inhibited RIPK1 kinase activity and reduced inflammatory gene expression. PMC8917516
Microglia 30 μM 2 h To evaluate the effect of RIPK1 kinase activity on inflammation and cell death in microglia. Results showed that Nec-1s inhibited RIPK1 kinase activity and reduced cell death. PMC8917516

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats Middle cerebral artery occlusion (MCAO) model Intracerebroventricular injection 20 mM Single injection, observed for 72 hours Nec-1 treatment significantly reduced ischemia-induced brain damage and neurological deficits, inhibited RIPK1 phosphorylation and its downstream signaling pathways. PMC6675533
Mice CD11c-Flip-KO mouse model In vitro differentiation medium 30 μM 3 or 6 days To evaluate the effect of Necrostatin-1 on DC differentiation, results showed that Necrostatin-1 slightly increased the viability of control cells but did not significantly enhance DC differentiation. PMC4429912
Mice Experimental autoimmune encephalomyelitis (EAE) model Oral 30 mg/kg and 60 mg/kg Twice daily, continuous treatment To evaluate the therapeutic effect of RIPK1 kinase inhibitor in the EAE model. Results showed that RIPK1 kinase inhibitor significantly alleviated disease symptoms. PMC8917516
Mice Myocardial infarction model Subcutaneous injection 5 mg/kg Once daily, continued until the end of the experiment Inhibition of necroptosis, improving survival and cardiac function after myocardial infarction PMC8329871

Protocol

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Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.86mL

0.77mL

0.39mL

19.28mL

3.86mL

1.93mL

38.56mL

7.71mL

3.86mL

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