Risarestat (CT 112)
(Synonyms: CT 112) 目录号 : GC31474
Risarestat (CT 112) (CT-112) 是一种醛糖还原酶抑制剂，用于治疗糖尿病并发症。
Cas No.:79714-31-1
Sample solution is provided at 25 µL, 10mM.
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Risarestat (CT-112), an aldose reductase inhibitor, is developed for the treatment of diabetic complications.
Risarestat inhibits the accumulation of dulcitol in a dose-dependent manner, except for the 1.0% solution which has an activity comparable to the 0.25% solution[1]. Risarestat peaks in the corneal epithelium, stroma, endothelium and aqueous humor in 30 minutes following instillation, then gradually diminishes time-dependently over a period of 24 hours. Risarestat remains detectable in the lens up to 24 hours, with a peak concentration at 2 hours after instillation[2]. The anterior surface area of superficial cells in the group treated with Risarestat is significantly decreases from a mean value of 881 to 728 microns2. Corneal sensitivity significantly improves from 5.36 to 1.37 g/mm2[3]. Animals treated with Risarestat shows a significant increase in the mean blinkresponse compared to untreated galactose-fed rats and does not differ significantly from controls towards the completion of the 7 month study. Animals treated topically with Risarestat and untreated galactose-fed rats develop bilateral nuclear cataracts within 3 weeks[4].
[1]. Awata T, et al. Effect of an aldose reductase inhibitor, CT-112, on healing of the corneal epithelium in galactose-fed rats. J Ocul Pharmacol. 1988 Fall;4(3):195-201. [2]. Ohashi Y, et al. Intraocular penetration of CT-112, an aldose reductase inhibitor, following topical instillation. J Ocul Pharmacol. 1989 Winter;5(4):325-8. [3]. Hosotani H, et al. Reversal of abnormal corneal epithelial cell morphologic characteristics and reduced corneal sensitivity in diabetic patients by aldose reductase inhibitor, CT-112. Am J Ophthalmol. 1995 Mar;119(3):288-94. [4]. Jacot JL, et al. Diabetic-like corneal sensitivity loss in galactose-fed rats ameliorated with aldose reductase inhibitors. J Ocul Pharmacol Ther. 1998 Apr;14(2):169-80.
Animal experiment: | Rats: The other 5 groups are fed on a 50% galactose diet, and 0.1, 0.25, 0.5 or 1.0% Risarestat ophthalmic solution or its vehicle is instilled in both eyes 4 times a day in each of the 5 treated groups. After 2 weeks, the corneal epithelium is scraped off in all rats and its dulcitol content is determined by gas chromatography[1]. Rabbits: Risarestat is prepared in acetate-buffered saline. 50 μL of 0.5% Risarestat in 7mM acetate-buffered saline (pH 5.2, 290 mOsm) containing 0.15% chlorbutanol as a preservative is instilled to both conjunctival sac of rabbits. This ophthalmic solution is proven to be untoxic to the external eye after 90 days' instillation to the rabbits 9 times a day. The rabbits are then sacrificed at, 15 and 30 minutes, 1, 2, 4, 8, and 24 hours after instillation[2]. |
References: [1]. Awata T, et al. Effect of an aldose reductase inhibitor, CT-112, on healing of the corneal epithelium in galactose-fed rats. J Ocul Pharmacol. 1988 Fall;4(3):195-201. | |
| Cas No. | 79714-31-1 | SDF | |
| 别名 | CT 112 | ||
| Canonical SMILES | O=C(N1)SC(C2=CC=C(OCCCCC)C(OCC)=C2)C1=O | ||
| 分子式 | C16H21NO4S | 分子量 | 323.41 |
| 溶解度 | DMSO : 105 mg/mL (324.67 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.0921 mL | 15.4603 mL | 30.9205 mL |
| 5 mM | 0.6184 mL | 3.0921 mL | 6.1841 mL |
| 10 mM | 0.3092 mL | 1.546 mL | 3.0921 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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1. 首先保证母液是澄清的；
2.
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- Purity: >98.00%
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