| Size | Price | |
|---|---|---|
| 100mg | ||
| Other Sizes |
| ln Vitro |
Rimexolone (Org 6216) exhibits little to no skin atrophy, little to no systemic effects, and greatly improved persistence at the injection site [1].
|
|---|---|
| ln Vivo |
In mice with arthritis induced by monoarticular antigen, rimexolone (Org 6216) (0-450 μg/mouse; intra-articular injection; once) exhibits sustained anti-inflammatory effects [1].
|
| Animal Protocol |
Animal/Disease Models: Male, 8-12 weeks old C57Black/6 mice, suffering from antigen-induced arthritis [1]
Doses: 5, 25, 50, 150, 250, 450 μg/mouse Route of Administration: intra-articular injection , primary Experimental Results: inhibition of arthritis in a dose-dependent manner. 450 and 150 μg Dramatically prevented osteophyte formation. Resulting in diminished inhibition of chondrocyte proteoglycan synthesis. |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Systemic absorption. Following intravenous injection of radiolabeled rimexolone into rats, over 80% of the dose is excreted in the feces as rimexolone and its metabolites. Metabolism/Metabolites Extensive metabolism. Following intravenous injection of radiolabeled rimexolone into rats, over 80% of the dose is excreted in the feces as rimexolone and its metabolites. Metabolites showed lower activity or no activity than rimexolone in human glucocorticoid receptor binding assays. Biological Half-Life Due to a large number of samples below the limit of quantitation (80 pg/mL), the serum half-life of rimexolone cannot be reliably estimated. However, based on the time required to reach steady state, the half-life appears to be short (1–2 hours). |
| Toxicity/Toxicokinetics |
Use of the medication during pregnancy and lactation ◉ Overview of use during lactation
Currently, there is no information available regarding the use of limexodus eye drops during lactation. Due to limited absorption by the eye, limexodus eye drops are not expected to have any adverse effects on breastfed infants. After using the eye drops, to significantly reduce the amount of medication entering breast milk, press the tear duct at the corner of the eye for at least 1 minute, then blot away any excess medication with absorbent paper. ◉ Effects on breastfed infants As of the revision date, no relevant published information was found. ◉ Effects on breastfeeding and breast milk As of the revision date, no relevant published information was found. |
| References |
|
| Additional Infomation |
Rimesodium is a 20-oxosteroid. Rimesodium is a 1% eye drop, belonging to the glucocorticoid steroid class. It is used to treat ocular inflammation. Its brand name is Vexol. Rimesodium is a corticosteroid. Its mechanism of action is as a corticosteroid hormone receptor agonist. Rimesodium is a derivative of prednisolone, a synthetic glucocorticoid with anti-inflammatory and immunosuppressive properties. After binding to cytoplasmic glucocorticoid receptors and entering cells, rimesodium activates specific glucocorticoid response elements, thereby altering gene expression. These alterations include inducing the synthesis of the anti-inflammatory protein IκB-α and inhibiting the synthesis of nuclear factor κB (NF-κB). Therefore, the production of pro-inflammatory cytokines such as interleukin-1 (IL-1), IL-2, and IL-6 is downregulated, and the activation of cytotoxic T lymphocytes is suppressed. Thus, an overall reduction in chronic inflammation and autoimmune responses can be achieved. Drug Indications For the treatment of inflammation following ophthalmic surgery and anterior uveitis. FDA Label Mechanism of Action Rimesolidone is a glucocorticoid receptor agonist. The anti-inflammatory effects of corticosteroids are thought to be related to lipocortin, a phospholipase A2 inhibitory protein that controls the biosynthesis of prostaglandins and leukotrienes by inhibiting arachidonic acid. By binding to glucocorticoid receptors, the drug ultimately leads to alterations in the transcription of genes involved in lipocortin and prostaglandins. Pharmacodynamics Rimesolidone is a systemic glucocorticoid. Corticosteroids inhibit inflammatory responses induced by a variety of mechanical, chemical, or immune stimuli. They inhibit inflammation-related edema, cell infiltration, capillary dilation, fibroblast proliferation, collagen deposition, and scar formation.
|
| Molecular Formula |
C24H34O3
|
|---|---|
| Molecular Weight |
370.525
|
| Exact Mass |
370.25
|
| CAS # |
49697-38-3
|
| PubChem CID |
5311412
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.1±0.1 g/cm3
|
| Boiling Point |
507.0±50.0 °C at 760 mmHg
|
| Melting Point |
258-268ºC
|
| Flash Point |
274.5±26.6 °C
|
| Vapour Pressure |
0.0±3.0 mmHg at 25°C
|
| Index of Refraction |
1.559
|
| LogP |
4.01
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
27
|
| Complexity |
749
|
| Defined Atom Stereocenter Count |
8
|
| SMILES |
CCC(=O)[C@]1([C@@H](C[C@@H]2[C@@]1(C[C@@H]([C@H]3[C@H]2CCC4=CC(=O)C=C[C@]34C)O)C)C)C
|
| InChi Key |
QTTRZHGPGKRAFB-OOKHYKNYSA-N
|
| InChi Code |
InChI=1S/C24H34O3/c1-6-20(27)24(5)14(2)11-18-17-8-7-15-12-16(25)9-10-22(15,3)21(17)19(26)13-23(18,24)4/h9-10,12,14,17-19,21,26H,6-8,11,13H2,1-5H3/t14-,17+,18+,19+,21-,22+,23+,24-/m1/s1
|
| Chemical Name |
(8S,9S,10R,11S,13S,14S,16R,17S)-11-hydroxy-10,13,16,17-tetramethyl-17-propanoyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-one
|
| Synonyms |
Rimexolone Org-6216 Rimexel Vexol
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6988 mL | 13.4942 mL | 26.9884 mL | |
| 5 mM | 0.5398 mL | 2.6988 mL | 5.3977 mL | |
| 10 mM | 0.2699 mL | 1.3494 mL | 2.6988 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00471419 | COMPLETED | Drug: Rimexolone | Dry Eye | Alcon Research | 2006-07 | Phase 3 |
| NCT02816905 | COMPLETED | Drug: 0.1 % Dexamethasone Drug: 0.1% Fluorometholone Drug: 1% Rimexolone |
Intraocular Pressure | Cairo University | 2015-10 | Phase 4 |
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