RIPK1-IN-33
RIPK1-IN-33 is a blood-brain barrier-permeable and orally active RIPK1 inhibitor, with an IC50 of 0.115 μM. RIPK1-IN-33 demonstrates remarkable anti-ferroptosis activity, radical scavenging capacity (IC50 = 123.3 μM), and anti-lipid peroxidation effects (IC50 = 9.72 μM). RIPK1-IN-33 markedly reduces cerebral infarction volume and improves neurological function scores in transient middle cerebral artery occlusion (tMCAO) model. RIPK1-IN-33 can be used for the study of ischemic stroke.
For research use only. We do not sell to patients.
- Formula: C26H27F2N5O2
- Molecular Weight:479.52
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
RIPK1-IN-33 (Compound 23a) (30-60 min) demonstrates remarkable radical scavenging DAPH capacity (IC50 = 123.3 μM), and antioxidant MDA effects (IC50 = 9.72 μM)[1]. RIPK1-IN-33 (0.0076-50 μM, 17 h) dose-dependently reduces the mRNA expression level of PTGS2 (IC50 = 0.156 μM) in HT-1080 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT-1080 cells
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Concentration:0.0076, 0.0227, 0.0686, 0.206, 0.617, 1.9, 5.6, 16.7, 50 μM
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Incubation Time:17 h
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Result:Reduced the mRNA expression level of PTGS2 (IC50 = 0.156 μM) in HT-1080 cells.
Displayed markedly superior anti-ferroptotic activity compared to Edaravone (HY-B0099) (IC50 = 4.92 μM).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male Sprague-Dawley rats (200-230 g) subjected to transient middle cerebral artery occlusion (tMCAO)[1]
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Dosage:33 mg/kg (68.8 μmol/kg)
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Administration:i.v. for twice doses and the second dose was administered 6 h later
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Result:Reduced infarct volume in tMCAO rats compared to the vehicle control.
Improved neurological function in tMCAO rats.
Downregulated MDA level.
Reduced the protein expression of necroptosis-associated caspase-3 in the ischemic penumbra.
Downregulated the protein expression of cyclooxygenase-2 (COX-2, encoded by PTGS2).
Upregulated glutathione peroxidase 4 (GPX4) within the ferroptosis pathway.
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Animal Model:Adult male Sprague-Dawley rats (200-230 g) subjected to transient middle cerebral artery occlusion (tMCAO)[1]
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Dosage:100, 200 mg/kg
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Administration:i.v. for a single dose or i.v. once daily for 7 days
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Result:Showed no abnormalities in body weight, food consumption, organ-to-body weight ratios, blood biochemical parameters, or gross necropsy findings.
Chemical Information
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Molecular Weight 479.52
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Formula C26H27F2N5O2
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SMILES
FC1=CC([C@@H]2CC=NN2C(C3CCN(CC4=CC=CC(N5C(CC(C)=N5)=O)=C4)CC3)=O)=CC(F)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RIPK1-IN-33 Related Classifications
HY-175027 Related Classifications
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