RIPK1-IN-35
RIPK1-IN-35 is a selective and orally active RIPK1 inhibitor with an IC50 of 5.33 nM. RIPK1-IN-35 has a potent protective effect against necroptosis in both human and murine cells. RIPK1-IN-35 shows good therapeutic effects in both TNF-α-induced systemic inflammatory response syndrome and DSS (HY-116282C)-induced inflammatory bowel disease models. RIPK1-IN-35 can be used to the study of inflammatory diseases related to necroptosis.
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- CAS No.: 3103886-96-7
- 화학식: C26H18D3F3N6O5
- 분자량:557.50
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보관:
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
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
RIPK1 5.33 nM (IC50) |
In Vitro
RIPK1-IN-35 (Compound 44) (0.01 nM-10 μM, 18 h) protects cells from TSZ (TNF-α, BV6 (HY-16701) and Z-VAD-FMK (HY-16658B))-induced necroptosis of human and mouse cell lines with EC50s of 18.1 and 11.5 nM in U937 and L929 cells[1].
RIPK1-IN-35 (0-300 nM, 5 h) significantly and dose-dependently inhibits the phosphorylation of RIPK1 as well as its downstream proteins RIPK3 and MLKL in HT-29 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-29 cells
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Concentration:0, 1, 3, 10, 30 and 100 nM
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Incubation Time:Pretreated for 1 h and added TSZ for 4 h
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Result:Significantly and dose-dependently inhibited the phosphorylation of RIPK1 as well as its downstream proteins RIPK3 and MLKL.
Parmacokinetics
In Vivo
RIPK1-IN-35 (10 mg/kg, p.o., once daily for 7 days) demonstrats a significant therapeutic effect in the DSS-induced inflammatory bowel disease (IBD) model, effectively alleviating the clinical symptoms and pathological damage of the disease[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:The model of systemic inflammatory response syndrome (SIRS) induced by TNF-α established in C57BL/6J mice (female, 6-8 weeks old)[1]
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Dosage:3 and 10 mg/kg
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Administration:Oral administration (p.o.), single dose
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Result:Dosage-dependently alleviated the sudden drop in body temperature caused by TNF-α.
Provided 80% and 100% survival protection rates respectively at doses of 3 mg/kg and 10 mg/kg.
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Animal Model:DSS-induced IBD model established in C57BL/6J mice (female, 6-8 weeks old)[1]
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Dosage:10 mg/kg
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Administration:Oral administration (p.o.), once daily for 7 days
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Result:Significantly reduced the weight loss caused by DSS and improved the DAI score.
Significantly improved the phenomenon of colonic shortening.
Significantly alleviated severe epithelial damage, necrosis and infiltration of inflammatory cells, with a more intact mucosal structure and reduced inflammatory infiltration.
신청
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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CAS No. 3103886-96-7
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Unlabeled CAS 3103886-80-9
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분자량 557.50
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화학식 C26H18D3F3N6O5
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SMILES
O=C(NC1=NNC(C2=CC=C3N(CCOC3=C2)C(CC4=C(C=CC(OC(F)F)=C4)F)=O)=C1)C5=NN(C([2H])([2H])[2H])C(C=C5)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RIPK1-IN-35 Related Classifications
HY-178762S Related Classifications
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