2. Immunology/Inflammation NF-κB Metabolic Enzyme/Protease Apoptosis
  3. Cyclophilin Reactive Oxygen Species (ROS) NF-κB Caspase Apoptosis
  4. 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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RN-0001

RN-0001 Chemical Structure

CAS No. : 252731-57-0

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RN-0001 Related Antibodies

Top Publications Citing Use of Products

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Cyclophilin A Cyclophilin B Cyclophilin C Cyclophilin D Cyclophilin G Cyclophilin E

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Description

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[1].

In Vitro

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.

RN-0001 Related Antibodies

Apoptosis Analysis[1]

Cell Line: AML12 cells
Concentration: 0.01, 0.1, 1 and 10 μM
Incubation Time: 24 h
Result: Reduced cell apoptosis.
Parmacokinetics
Species Dose Route Cmax T1/2
Rat[1] 1 mg/kg i.v. 3670 ng/mL 3.17 h
Rat[1] 3 mg/kg i.v. 7470 ng/mL 3.53 h
Rat[1] 10 mg/kg i.v. 24800 ng/mL 5.06 h
In Vivo

RN-0001 (10 mg/kg; i.p.; once daily for 11 consecutive days) effectively alleviates ethanol-induced liver injury, mitochondrial dysfunction, steatosis and inflammatory responses in a mouse model of ALD[1].
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.

Animal Model: C57BL/6J (male, 7 weeks old, NIAAA chronic-plus-binge ethanol feeding model)[1]
Dosage: 10 mg/kg
Administration: i.p.; daily
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.
Molecular Weight

1289.73

Formula

C66H120N12O13
CAS No.
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Storage

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Purity & Documentation
References
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RN-0001 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RN-0001252731-57-0RN0001RN 0001CyclophilinReactive Oxygen Species (ROS)NF-κBCaspaseApoptosisNuclear factor-κBNuclear factor-kappaBNF-κB p65AML12 hepatocytesalcohol-associated liver diseasereactive oxygen speciespeptidyl-prolyl cis-trans isomeraseCypAmitochondrial permeability transition porecytochrome cCypDcleaved caspase-3Inhibitorinhibitorinhibit

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