RN-0001
RN-0001 is a cyclophilin (Cyp) inhibitor with Ki values of 4.1 nM and 12.0 nM against CypA and CypD, respectively, and an EC50 of 916 nM for CypD. RN-0001 binds directly to CypD, inhibits the peptidyl-prolyl cis-trans isomerase activities of CypD and CypA, and prevents CypD-dependent mitochondrial permeability transition pore opening. RN-0001 improves mitochondrial function, reduces ROS production, inhibits the expression of lipogenic markers, blocks the nuclear translocation of NF-κB p65, and decreases the release of activated caspase-3 and cytochrome c. RN-0001 can be used in the research of alcohol-associated liver disease.
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- CAS. Nr.: 252731-57-0
- Formel: C66H120N12O13
- Molecular Weight:1289.73
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
RN-0001 (multiple concentrations; 30 min ambient temperature, 15 min 30°C reaction) exhibits weak direct calcineurin inhibition (IC50 = 2276 nM) and moderately enhanced inhibition when complexed with cyclophilin A (IC50 = 1551 nM) in a cell-free assay[1].
RN-0001 (multiple concentrations) preserves mitochondrial calcium retention capacity with an EC50 of 916 nM in a cell-free isolated mitochondrial assay[1].
RN-0001 (multiple concentrations) has reduced immunosuppressive activity, inhibiting IL-2 release with an EC50 of 347.90 nM in a cell-based immune cell assay[1].
RN-0001 (0.01-10 μM; 24 h) improves viability in ethanol-injured AML12 hepatocytes (IC50 = 102.7 μM) and RAW264.7 macrophages (IC50 = 60.73 μM) in a concentration-dependent manner, with superior efficacy to Debio-025 at matching doses[1].
RN-0001 (0.01-10 μM; 24 h) concentration-dependently reduces LDH release, apoptosis, and aberrant expression of lipogenic, inflammatory, oxidative stress, and apoptotic proteins in ethanol-injured AML12 hepatocytes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:AML12 cells
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Concentration:0.01, 0.1, 1 and 10 μM
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Incubation Time:24 h
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Result:Reduced cell apoptosis.
RN-0001 (10 mg/kg; i.p.; once every 2 days; for 90 consecutive days) is well tolerated and causes no adverse effects in healthy 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/6J (male, 7 weeks old, NIAAA chronic-plus-binge ethanol feeding model)[1]
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Dosage:10 mg/kg
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Administration:i.p.; daily
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Result:Partially reversed alcohol-induced weight loss.
Reduced serum levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST), triglycerides (TG), and total cholesterol (TC).
Decreased serum pro-inflammatory cytokines TNF-α and IL-6.
Normalized liver weight/body weight ratio.
Reduced liver free fatty acid (FFA) and TG levels.
Decreased hepatic fat droplet accumulation and macrophage infiltration, resulting in a lower NAFLD Activity Score (NAS).
Reversed aberrations in key proteins involved in mitochondrial function (DRP1, FIS1, MFN1, MFN2, OPA1), oxidative stress (CYP2E1, iNOS), antioxidation (p-NRF2, NRF2, SOD1, CAT), and apoptosis (cleaved caspase-3, Cyto C, Bcl2, BAX).
Reduced mitochondrial swelling post-ethanol exposure.
Chemical Information
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CAS. Nr. 252731-57-0
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Molecular Weight 1289.73
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Formel C66H120N12O13
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
RN-0001 Related Classifications
HY-P11489 Related Classifications
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- RN-0001
- 252731-57-0
- RN0001
- RN 0001
- Cyclophilin
- Reactive Oxygen Species (ROS)
- NF-κB
- Caspase
- Apoptosis
- NF-κB p65
- AML12 hepatocytes
- alcohol-associated liver disease
- reactive oxygen species
- peptidyl-prolyl cis-trans isomerase
- CypA
- mitochondrial permeability transition pore
- cytochrome c
- CypD
- cleaved caspase-3
- Inhibitor
- inhibitor
- inhibit