RPR107393 free base
目录号 : GC31556
RPR107393freebase是一种有效的选择性角鲨烯合酶(squalenesynthase)抑制剂，抑制鼠肝微粒体角鲨烯合成酶，IC50值为0.8±0.2nM。
Cas No.:197576-78-6
Sample solution is provided at 25 µL, 10mM.
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RPR107393 free base is a selective squalene synthase inhibitor, which inhibits rat liver microsomal squalene synthase with an IC50 of 0.8±0.2 nM.
RPR107393 is a selective squalene synthase inhibitor with subnanomolar potency. RPR107393 inhibits rat liver microsomal squalene synthase with an IC50 value of 0.8±0.2 nM (n=4)[1]. In the time-course study, cells are treated with ER-27856 (1 μM), RPR-107393 (10 μM), Atorvastatin (1 μM), or NB-598 (1 μM) for 2-24 h, and lipid biosynthesis during the last 2 h of the incubation is determined. RPR-107393 (10 μM) inhibits Cholesterol biosynthesis and reduces triglyceride biosynthesis. Similarly, 1 μM RPR-107393 inhibits Cholesterol and triglyceride biosynthesis by 82.4% and 70.0%, respectively[2].
One hour after RPR107393 (10 mg/kg p.o.), Cholesterol biosynthesis is reduced by 92% with an approximate ED50 value of 5 mg/kg. Six hours after RPR107393 (10 mg/kg p.o.) administration, Cholesterol biosynthesis is reduced by 74% (the time for 50% inhibition is ~7 hr). An 82% inhibition of hepatic Cholesterol biosynthesis is observed 10 hr after RPR107393 (25 mg/kg p.o.), but the effect is no longer apparent at 21 hr. Inhibition of Cholesterol biosynthesis by Zaragozic acid or RPR107393 is associated with an accumulation of radiolabeled diacid products in the liver. RPR107393 is a potent Cholesterol-lowering agent in rats. RPR107393 (30 mg/kg p.o. b.i.d.) lowers serum Cholesterol by 35% after 2 days and by nearly 50% after 3 days of treatment[1].
[1]. Amin D, et al. RPR107393, a potent squalene synthase inhibitor and orally effective Cholesterol-lowering agent: comparison with inhibitors of HMG-CoA reductase. J Pharmacol Exp Ther. 1997 May;281(2):746-52. [2]. Hiyoshi H, et al. Squalene synthase inhibitors suppress triglyceride biosynthesis through the farnesol pathway in rat hepatocytes. J Lipid Res. 2003 Jan;44(1):128-35.
Animal experiment: | Rats[1]Sprague-Dawley rats weighing 60 to 70 g are given rodent diet and kept under reverse-lighting conditions (lights on, 3:00 p.m. to 3:00 a.m.). Cholestyramine is included in the diet for 2 days before the study to stimulate liver Cholesterol biosynthetic capacity. Drugs are suspended in 0.5% methyl cellulose or dissolved in saline (Zaragozic acid). RPR107393 (10 mg/kg) is given p.o. by gavage, and Zaragozic acid is given s.c.. After a specified time period, the animals receive [14C]Mevalonolactone (15 μCi/kg; 40 Ci/mol) by s.c. injection. Fifteen minutes later, the animals are killed with CO2. The livers are removed, and 0.5 g of the liver is saponified in 2 mL of 15% KOH/ethanol overnight at 80°C. Samples are extracted with petroleum ether in alkaline conditions, and [14C]Cholesterol is quantified by HPLC. |
References: [1]. Amin D, et al. RPR107393, a potent squalene synthase inhibitor and orally effective Cholesterol-lowering agent: comparison with inhibitors of HMG-CoA reductase. J Pharmacol Exp Ther. 1997 May;281(2):746-52. | |
| Cas No. | 197576-78-6 | SDF | |
| Canonical SMILES | OC1(C2=CC=C(C3=CC=C4N=CC=CC4=C3)C=C2)CN5CCC1CC5 | ||
| 分子式 | C22H22N2O | 分子量 | 330.42 |
| 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 | 3.0265 mL | 15.1323 mL | 30.2645 mL |
| 5 mM | 0.6053 mL | 3.0265 mL | 6.0529 mL |
| 10 mM | 0.3026 mL | 1.5132 mL | 3.0265 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。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet