Pirinixil (BR-931)
(Synonyms: 匹立昔尔; BR-931) 目录号 : GC31488
Pirinixil (BR-931) 是一种低毒的降血脂药。
Cas No.:65089-17-0
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, weighing 220 to 230 g at the start of each experiment, are used in all studies. They are kept in an air-conditioned environment, with controlled lighting and free access to water. Dietary treatments are (A) standard diet for rats and (B) 2% cholesterol+2% cholic acid regimen. Both diets are administered ad libitum, respectively for 1 and 2 weeks (standard diet) and for 2 weeks (cholesterolcholic acid diet). Groups of 5 rats in each of the 3 experiments (1 and 2 weeks with the standard diet, 2 weeks with the cholesterol-cholic acid diet) are administered Pirinixil daily in carboxymethylcellulose vehicle by gastric intubation, at the doses of 20 mg/kg. Controls are given a similar volume of vehicle daily by intubation[1]. |
References: [1]. D'Atri G, et al. Clofibrate, pirinixil (BR 931) and WY-14,643 do not affect body cholesterol in Sprague-Dawley rats. Atherosclerosis. 1980 Nov;37(3):475-83. | |
Pirinixil is a hypolipidemic agent of low toxicity.
Pirinixil is a hypolipidemic agent of low toxicity. Total cholesterol is reduced by Pirinixi in the spleen, kidney and heart of rats. Pirinixil decreases the estimated total body cholesterol approximately 40%[1]. Pirinixil increases plasma cholesterol levels significantly without affecting plasma triglycerides. Liver cholesterol and triglycerides are markedly reduced by Pirinixil, while combined plasma and liver lipid levels decrease approximately 20%. Liver HMG-CoA reductase activity is not affected, but cholesterol 7α-hydroxylase is significantly reduced by Pirinixil[2].
[1]. D'Atri G, et al. Clofibrate, pirinixil (BR 931) and WY-14,643 do not affect body cholesterol in Sprague-Dawley rats. Atherosclerosis. 1980 Nov;37(3):475-83. [2]. Kritchevsky D, et al. Increased plasma cholesterol and decreased body lipid levels in Wistar rats following pirinixil(BR 931) treatment. Pharmacol Res Commun. 1979 Jun;11(6):475-82.
| Cas No. | 65089-17-0 | SDF | |
| 别名 | 匹立昔尔; BR-931 | ||
| Canonical SMILES | O=C(NCCO)CSC1=NC(NC2=CC=CC(C)=C2C)=CC(Cl)=N1 | ||
| 分子式 | C16H19ClN4O2S | 分子量 | 366.87 |
| 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 | 2.7258 mL | 13.6288 mL | 27.2576 mL |
| 5 mM | 0.5452 mL | 2.7258 mL | 5.4515 mL |
| 10 mM | 0.2726 mL | 1.3629 mL | 2.7258 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。
Clofibrate, pirinixil (BR 931) and WY-14,643 do not affect body cholesterol in Sprague-Dawley rats
Cholesterol levels in plasma and different tissues were determined in Sprague-Dawley male rats, on standard and cholesterol-cholic acid enriched diets, after short term treatment with the absorbable hypolipidemic agents, clofibrate, WY-14,643 and Pirinixil (BR 931). The objective of the study was to evaluate the mode of action of these drugs in decreasing plasma cholesterol, be it by increased tissue mobilization, or by redistribution from plasma to tissues. After one or two weeks on a standard diet, none of the three agents significantly affected total body cholesterol stores. In spite of the liver enlargement induced by all three, in no case was total liver cholesterol significantly raised. Only clofibrate significantly increased colonic cholesterol concentrations. On a cholesterol-cholic acid regimen, some cholesterol mobilization was noted with all three drugs. However, only Pirinixil significantly reduced total liver cholesterol as well as the estimated total body cholesterol. A parallel effect of diet and drugs on plasma and body cholesterol pools is not constantly observed. In the examined rat model, clofibrate and two chemically unrelated compounds with a probably similar mechanism of action, markedly reduce plasma cholesterol levels while not affecting or decreasing total body cholesterol stores.
Pilot study of pirinixil (BR 931) in various forms of hyperlipoproteinemias
Plasma lipoprotein composition in cholesterol fed rabbits treated with pirinixil (BR 931), a new lipid lowering agent
Increased plasma cholesterol and decreased body lipid levels in Wistar rats following pirinixil (BR 931) treatment
Pharmacological profile of BR-931, a new hypolipidemic agent that increases high-density lipoproteins
BR-931 [4-chloro-6-(2,3-xylidino)-2-pyrimidinylthio-(N-beta-hydroxyethyl)-acetamide], a new hypolipidemic agent of low toxicity, was evaluated in several tests of lipolysis and hyperlipidemia in rats, and in the cholesterol-induced atherosclerosis in rabbits. Significant hypolipidemic activity was observed in rats with doses of the agent at 12.5--50 mg/kg. In the Triton-induced hyperlipidemia, 50 mg BR-931 per kg was equieffective as 200 mg of clofibrate (CPIB) per kg. In contrast with CPIB, BR-931 exerted a powerful antilipolytic activity against epinephrine, ACTH, nicotine and cold exposure. BR-931 was particularly effective in diet-induced hyperlipidemias. Ethanol lipemia was totally prevented by the agent at 100 mg/kg. With Nath's diet, doses as low as 25 mg/kg significantly reduced hypercholesterolemia and hypertriglyceridemia. In these last two tests, the distribution of lipoprotein cholesterol was also determined. CPIB did not affect HDL cholesterol levels that had been decreased by the diets; in contrast, BR-931, already at doses of 50 mg/kg, brought the HDL/total cholesterol ratio back toward normal. A significant HDL cholesterol increase, together with some reduction of atheromatosis, was also observed in cholesterol-fed rabbits. BR-931, a potent inducer of liver peroxisones and of mitochondrial carmitine acetyltransferase, appears to be a hypolipidemic agent of high efficacy and low toxicity for the clinical treatment of hyperlipidemias and atherosclerosis.