| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
Olesoxime (formerly known as TRO 19622; RG-6083) is a mitochondrial-targeted neuroprotective agent with EC50 value for increasing cell survival is 3.2±0.2 µM. Olesoxime, with a cholesterol-like structure, displays neuroprotective properties in preclinical studies, it has been demonstrated that the compound promotes the function and survival of neurons and other cell types under disease-relevant stress conditions through interactions with the mitochondrial permeability transition pore (mPTP).
| ln Vitro |
After being treated without neurotrophic factors derived from the brain, ciliary body, or glia, primary embryonic rat spinal MN were significantly protected against cell damage and death by exposure to Olesoxime (TRO 19622) at concentrations ranging from 0.1 to 10 µM one hour after inoculation. This protection persisted for three days in culture. Olesoxime (TRO 19622), at a concentration of 10 µM, sustains 74±10% neuronal survival by the action of a mixture of neurotrophic factors, including those produced from the brain, ciliary bodies, and glial cells. In this test, the average EC50 was 3.2±0.2 µM. Olesoxime (TRO 19622) not only shields MN cell bodies but also encourages neurite development. At a 1 µM concentration, olesoxime (TRO 19622) only slightly improved cell viability but significantly boosted neurite development per cell by 54% [1]. A novel class of cholesterol oximes known as olesoxime (TRO 19622) was discovered due to its ability to increase the survival of pure motor neurons in the absence of neurotrophic factors. Olesoxime (TRO 19622) selectively targets proteins in the outer membrane of the mitochondria, focusing on the mitochondria and inhibiting oxidative stress-mediated permeability transition pore opening, among other processes[2].
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| ln Vivo |
Adult mice receiving daily subcutaneous injections of Olesoxime (TRO 19622) (3 or 30 mg/kg) for more than two months was well tolerated without toxicity or adverse effects [1]. Olesoxime (TRO 19622) increased motor neuron cell body survival in a dose-dependent manner when animals were treated orally for five days post-lesion; at this dose, motor neuron survival was 29 ±2% (n=18), a 42% increase in survival compared to vehicle-treated animals [3]. Paclitaxel-treated rats receiving prophylactic treatment with 3 mg/kg/d or 30 mg/kg/d Olesoxime (TRO 19622) had 239±17.6 and 247±14.4 IENF/cm, respectively. For both doses, the decrease was significantly smaller than the 46% seen in vehicle-administered paclitaxel-treated rats.
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| References |
[1]. Martin LJ, et al. Olesoxime, a cholesterol-like neuroprotectant for the potential treatment of amyotrophic lateral sclerosis. IDrugs. 2010 Aug;13(8):568-80.
[2]. Bordet T, et al. Olesoxime (TRO19622): A Novel Mitochondrial-Targeted Neuroprotective Compound. Pharmaceuticals (Basel). 2010 Jan 28;3(2):345-368 [3]. Bordet T, et al. Identification and characterization of cholest-4-en-3-one, oxime (TRO19622), a novel drug candidate for amyotrophic lateral sclerosis. J Pharmacol Exp Ther. 2007 Aug;322(2):709-20. [4]. Xiao WH, et al. Olesoxime (cholest-4-en-3-one, oxime): analgesic and neuroprotective effects in a rat model of painful peripheral neuropathy produced by the chemotherapeutic agent, paclitaxel. Pain. 2009 Dec 15;147(1-3):202-9 |
| Molecular Formula |
C27H45NO
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|---|---|
| Molecular Weight |
399.6523
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| CAS # |
22033-87-0
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| SMILES |
O/N=C1CC[C@]2(C)[C@@]3([H])CC[C@]4(C)[C@@H]([C@H](C)CCCC(C)C)CC[C@@]4([H])[C@]3([H])CCC2=C\1
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| InChi Key |
QNTASHOAVRSLMD-SIWSWZRQSA-N
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| InChi Code |
InChI=1S/C27H45NO/c1-18(2)7-6-8-19(3)23-11-12-24-22-10-9-20-17-21(28-29)13-15-26(20,4)25(22)14-16-27(23,24)5/h17-19,22-25,29H,6-16H2,1-5H3/b28-21+/t19-,22+,23-,24+,25+,26+,27-/m1/s1
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| Chemical Name |
(8S,9S,10R,13R,14S,17R,E)-10,13-dimethyl-17-((R)-6-methylheptan-2-yl)-1,2,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-3H-cyclopenta[a]phenanthren-3-one oxime
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| Synonyms |
NSC 21311; NSC-21311; NSC21311; TRO-19622; TRO19622; TRO19622; RG6083; RG 6083; RG-6083;
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| 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)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~125.11 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.26 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.26 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.26 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5022 mL | 12.5109 mL | 25.0219 mL | |
| 5 mM | 0.5004 mL | 2.5022 mL | 5.0044 mL | |
| 10 mM | 0.2502 mL | 1.2511 mL | 2.5022 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.
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