TRO 19622 (Synonyms: NSC 21311) |
| Catalog No.GC13726 |
TRO 19622(TRO 19622)는 세포 생존을 증가시키기 위한 평균 EC50 값이 3.2±0.2 μM인 미토콘드리아 표적 신경보호 화합물입니다.
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Cas No.: 22033-87-0
Sample solution is provided at 25 µL, 10mM.
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Olesoxime (TRO 19622) is a mitochondrial-targeted neuroprotective compound with mean EC50 value for increasing cell survival is 3.2±0.2 µM.
Exposure to Olesoxime (TRO 19622) (ranging from 0.1 to 10 µM) at 1 h after plating significantly protects primary embryonic rat spinal MNs (that had been cultured for 3 days without brain-derived, ciliary and glia-derived neurotrophic factors) from cell death. At a concentration of 10 µM, Olesoxime (TRO 19622) maintains survival of 74±10% of the neurons supported by a combination of neurotrophic factors (brain-derived, ciliary and glia-derived neurotrophic factors). The mean EC50 in this assay is 3.2±0.2 µM. In addition to preserving MN cell bodies, Olesoxime (TRO 19622) also promotes the outgrowth of neurites. At a concentration of 1 µM, which increases cell survival by only 38%, Olesoxime (TRO 19622) increases overall neurite outgrowth per cell by 54%[1]. Olesoxime (TRO 19622) belongs to a new family of cholesterol-oximes identified for its survival-promoting activity on purified motor neurons deprived of neurotrophic factors. Olesoxime (TRO 19622) targets proteins of the outer mitochondrial membrane, concentrates at the mitochondria and prevents permeability transition pore opening mediated by, among other things, oxidative stress[2].
Daily administration of Olesoxime (TRO 19622) (3 or 30 mg/kg sc) to adult mice for more than 2 months is well tolerated without toxicity or adverse effects[1]. When animals are treated orally for 5 days following the lesion, Olesoxime (TRO 19622) increases motor neuron cell body survival in a dose-dependent manner with significant rescue at the highest dose of 100 mg/kg. At this dose, motor neuron survival is 29 ±2% (n=18) corresponding to a 42% increase in survival compared with vehicle-treated animals[3]. Paclitaxel-treated rats that receive prophylactic treatment with 3 mg/kg/d or 30 mg/kg/d Olesoxime (TRO 19622) have 239±17.6 and 247±14.4 IENFs per cm, respectively. For both doses, the decreases are significantly less than the 46% decrease seen in the Paclitaxel-treated rats administered vehicle. However, both doses produce decreases (25% and 22%) that are significantly different relative to the naïve control group[4].
Reference:
[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
Animal experiment: | Mice[3] Eight-week-old C57bl/6 RJ mice are anesthetized using 60 mg/kg i.p. ketamine chlorohydrate. To reduce the risk of gender-related differences in response to Olesoxime (TRO 19622), only female mice are used. The right sciatic nerve is surgically exposed at mid-thigh level, and it is crushed 5 mm proximal to the trifurcation of the sciatic nerve. The nerve is crushed twice for 30 s with hemostatic forceps (width, 1.5 mm) with a 90° rotation between each crush. Sciatic nerve degeneration/regeneration is assessed over 6 weeks by measurement of the compound muscular action potential (CMAP) and histological studies of the damaged area of the sciatic nerve. Olesoxime (TRO 19622) is given subcutaneously at 0.3, 3, and 30 mg/kg. Treatments started the day of the crush injury, and they continued daily for 6 weeks. In total, 15 animals per group are used in the study. Electromyography is performed once a week for 6 weeks using a Neuromatic 2000M electromyograph. Mice are anesthetized using 100 mg/kg i.p. ketamine chlorohydrate. CMAP is measured in the gastrocnemius muscle after a single 0.2-ms stimulation of the sciatic nerve at supramaximal intensity (12.8 mA). The amplitude (millivolts) and the latency (milliseconds) of the action potential are measured. Rats[4] Adult male Sprague-Dawley rats (200-300 g) are used. Olesoxime (TRO 19622) or the vehicle is administered via oral gavage in a volume of 5 mL/kg. The TRO19622doses used here (3-100 mg/kg) are chosen based on prior reports of neuroprotective and analgesic activity. |
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. | |
| Cas No. | 22033-87-0 | SDF | |
| Synonyms | NSC 21311 | ||
| Chemical Name | (8S,9S,10R,13R,14S,17R,E)-10,13-dimethyl-17-((R)-6-methylheptan-2-yl)-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3(2H)-one oxime | ||
| Canonical SMILES | CC(CCC[C@@]([C@@]1([H])CC[C@@]2([H])[C@]([C@]3([H])CC[C@]12C)([H])CCC4=C/C(CC[C@@]43C)=N/O)([H])C)C | ||
| Formula | C27H45NO | M.Wt | 399.65 |
| Solubility | DMF: 2 mg/ml,DMSO: 0.1 mg/ml,Ethanol: 20 mg/ml,Ethanol:PBS (pH 7.2)(1:2): 0.3 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
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- Purity: >99.50%
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Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)
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