Rimexolone
Rimexolone (Org 6216) is a glucocorticoid steroid with anti-inflammatory activity. Rimexolone can be used as a 1% ophthalmic suspension for the management of ocular inflammation.
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- CAS No.: 49697-38-3
- Formule: C24H34O3
- Masse moléculaire:370.52
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Hepatocyte | EC50 |
0.4 μM
Compound: Rimexolone
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Activation of PXR in human cryopreserved hepatocytes assessed as induction of CYP3A4
Activation of PXR in human cryopreserved hepatocytes assessed as induction of CYP3A4
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[PMID: 20966043] |
| HepG2 | EC50 |
0.68 μM
Compound: Rimexolone
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Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis
Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis
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[PMID: 20966043] |
| HepG2 | EC50 |
1.6 μM
Compound: Rimexolone
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Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
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[PMID: 20966043] |
| HepG2 | EC50 |
4 μM
Compound: Rimexolone
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Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
|
[PMID: 20966043] |
Rimexolone (Org 6216) shows highly enhanced persistence at the injection site, minimal systematic effects and virtually does not induce skin artrophy[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male, 8-12 weeks old C57Black/6 mice with antigen induced arthritis[1]
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Dosage:5, 25, 50, 150, 250, 450 μg/mouse
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Administration:Intraarticular injection, once
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Result:Suppressed the arthritis in a dose-dependent manner.
Significantly prevented osteophyte formation at 450 and 150 μg.
Resulted in a decrease of the inhibition of the chondrocyte proteoglycan synthesis.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 49697-38-3
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Masse moléculaire 370.52
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Formule C24H34O3
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SMILES
C[C@@]12[C@](C(CC)=O)(C)[C@H](C)C[C@@]1([H])[C@]3([H])CCC4=CC(C=C[C@]4(C)[C@@]3([H])[C@@H](O)C2)=O
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Synonyms
Org 6216; Rimexel
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Joosten LA, et al. Protective effect of rimexolone on cartilage damage in arthritic mice: a comparative study with triamcinolone hexacetonide. Agents Actions. 1990 Aug;31(1-2):135-42. [Content Brief]
[2]. Foster CS, et al. Efficacy and safety of rimexolone 1% ophthalmic suspension vs 1% prednisolone acetate in the treatment of uveitis. Am J Ophthalmol. 1996 Aug;122(2):171-82. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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