Y-9738
目录号 : GC32596
Y-9738是一种降血脂药。
Cas No.:59399-41-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Male Sprague-Dawley rats are used in this work. Rats (140 to 180 g) are fed a high cholesterol diet for 10 days. This diet contains 1% cholesterol, 0.2% sodium cholate and 5% olive oil. Y-9738 is orally administered to the animals once a day throughout the experimental period. All animals are starved overnight (about 20 h) after the last treatment and sacrificed by carotid incision. Blood and liver are collected for lipid analysis[1]. |
References: [1]. Kobayakawa T, et al. Experimental hyper-beta-lipoproteinemia and its amelioration by a novel hypolipidemic agent. Atherosclerosis. 1978 Jul;30(3):219-25. | |
Y-9738 is a hypolipidemic agent.
Y-9738 is a hypolipidemic agent. At 100 mg/kg Y-9738 lowers the cholesterol level by 36% and clearly diminishes the intensity of the β-lipoprotein band with a tendency for the α-lipoprotein band to be intensified. Y-9738 causes a dose-dependent decrease in serum cholesterol, triglyceride and heparin-precipitable β-lipoprotein cholesterol. Furthermore, Y-9738 reduces the intensity of the β-lipoprotein band shown by electrophoresis, and increases that of the α-lipoprotein band[1].
[1]. Kobayakawa T, et al. Experimental hyper-beta-lipoproteinemia and its amelioration by a novel hypolipidemic agent. Atherosclerosis. 1978 Jul;30(3):219-25.
| Cas No. | 59399-41-6 | SDF | |
| Canonical SMILES | O=C(OCC)CC1=C(OCC)OC(C2=CC=C(Cl)C=C2)=N1 | ||
| 分子式 | C15H16ClNO4 | 分子量 | 309.74 |
| 溶解度 | Soluble in DMSO | 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 | 3.2285 mL | 16.1426 mL | 32.2851 mL |
| 5 mM | 0.6457 mL | 3.2285 mL | 6.457 mL |
| 10 mM | 0.3229 mL | 1.6143 mL | 3.2285 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
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，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Effects of ethyl-2-(4-chlorophenyl)-5-ethoxy-4-oxazole acetate (Y-9738) on the serum lipids of patients with hyperlipidemia and/or hypo-HDL-emia
Arzneimittelforschung 1984;34(6):730-3.PMID:6541494doi
With the view of examining the serum lipid metabolism-improving action of a new compound, ethyl-2-(4-chlorophenyl)-5-ethoxy-4-oxazole acetate (Y-9738), 900 mg was administered to 47 patients with various diseases associated with hyperlipidemia and/or hypo-HDL (high density lipoprotein)-emia for successive 16 weeks. Serum HDL-cholesterol increased significantly 4 weeks after the administration (mean 11.8%, p less than 0.01). In the patients with hypo-HDL-emia who showed the initial level of 50 mg/dl or less, the degree of increase was more remarkable (mean 16,4%, p less than 0.01), and a significant increase was noted until 12 weeks later. Further, a similar change was noted in respect to serum HDL-phospholipid. The main apoprotein of HDL, apoprotein A (I + II) began to increase significantly 4 weeks after the institution of the administration. At the end of the trial, it increased by mean 31% (p less than 0.01). Y-9738 did not exert any significant effect on serum total cholesterol, triglyceride and phospholipid, but it caused a reduction in so-called atherogenic indexes.
Experimental hyper-beta-lipoproteinemia and its amelioration by a novel hypolipidemic agent
Atherosclerosis 1978 Jul;30(3):219-25.PMID:209804DOI:10.1016/0021-9150(78)90048-5.
Experimental models for hyper-beta-lipoproteinemia were established in rats and the effects of certain hypolipidemic drugs were studied with these models. In the hyperlipemia induced in rats by feeding a high cholesterol diet, Y-9738 [ethyl 2(4-chlorophenyl)-5-ethoxy-4-oxazoleacetate] produced a dose-dependent reduction of serum cholesterol: such hypolipidemic activity was estimated to be about 7 times as great as that of clofibrate. On the other hand, clofibrate induced hepatomegaly at 100 mg/kg, whereas Y-9738 did not at this dosage, which is about 10 times the effective dose. Hyperlipemia induced by high cholesterol and thiouracil was characterized by increased beta-lipoprotein (heparin-calcium and disc electrophoresis). In this model, Y-9738 showed a dose-dependent lowering effect on beta-lipoprotein cholesterol with a marked decrease in the beta/alpha lipoprotein ratio. A tendency was noted for alpha-lipoprotein to be increased. In contrast, clofibrate exerted no effect on this hyper-beta-lipoproteinemia. These results suggest that the above models may be of value in exploring hyper-beta-lipoproteinemia and that Y-9738 may be more useful than clofibrate in the therapy of hyperlipemia.