RIPK1-IN-11
RIPK1-IN-11 is a potent and orally active RIPK1 inhibitor (Kd=9.2 nM; IC50=67 nM). RIPK1-IN-11 inhibits necroptosis in both human and mouse cells (EC50=17-30 nM). Anti-inflammatory activity.
For research use only. We do not sell to patients.
- CAS No.: 2173557-02-1
- Formula: C23H24N4O4S
- Molecular Weight:452.53
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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
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RIPK1 |
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Cell Line
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Type | Value | Description | References |
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| HT-29 | EC50 |
17 nM
Compound: 70
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Anti-necroptic activity in human HT-29 cells assessed as TNFalpha/Z-VAD (TSZ) induced necroptosis by measuring cell viability preincubated for 1 hr followed by TSZ addition ans measured after 24 hrs by celltiter-glo luminescent cell viability assay
Anti-necroptic activity in human HT-29 cells assessed as TNFalpha/Z-VAD (TSZ) induced necroptosis by measuring cell viability preincubated for 1 hr followed by TSZ addition ans measured after 24 hrs by celltiter-glo luminescent cell viability assay
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[PMID: 34906762] |
| L929 | EC50 |
30 nM
Compound: 70
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Anti-necroptic activity in mouse L929 cells assessed as TNFalpha/Z-VAD (TSZ) induced necroptosis by measuring cell viability preincubated for 1 hr followed by TSZ addition and measured after 24 hrs by celltiter-glo luminescent cell viability assay
Anti-necroptic activity in mouse L929 cells assessed as TNFalpha/Z-VAD (TSZ) induced necroptosis by measuring cell viability preincubated for 1 hr followed by TSZ addition and measured after 24 hrs by celltiter-glo luminescent cell viability assay
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[PMID: 34906762] |
RIPK1-IN-11 (compound 70) (24 hours; for 1h prior to the treatment of TNFα) efficiently blocks necroptosis induced by TNFα in both human and mouse cells (EC50=17-30 nM)[1].
Pharmacokinetic profiles of compound 70 in male SD rats
| IV (2 mg/kg) | PO (10 mg/kg) | |
| Tmax (h) | 1.2 | |
| Cmax (ng/mL) | 1330 | 1241 |
| AUC0-24 (ng/mL∗h) | 1208 | 3827 |
| t1/2 (ng/mL) | 1.0 | 1.7 |
| CL (mL/min/kg) | 33 | |
| Vd, ss (L/kg) | 2.4 | |
| F (%) | 63% |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
RIPK1-IN-11 (5 mg/kg, 25 mg/kg; p.o.; 7 days; C57BL/6 mouse) exhibits no obvious toxicity in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 female mice (TNF-induced systemic inflammatory response syndrome)[1]
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Dosage:3 mg/kg
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Administration:i.p. for 30 min, followed by injection with TNFα (0.25 μg/g)
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Result:Significantly reduced TNFα-induced temperature loss and ameliorated lethal shock in mice.
Chemical Information
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CAS No. 2173557-02-1
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Molecular Weight 452.53
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Formula C23H24N4O4S
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SMILES
O=C(OC1CCOCC1)NC2=CC(C3=CC=C4N=C(NC(C5CC5)=O)SC4=C3)=CN=C2C
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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-11 Related Classifications
HY-144276 Related Classifications
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