YM-53601 free base
目录号 : GC31516
A squalene synthase inhibitor
Cas No.:182959-28-0
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: | Rats[1]Rats are given a single oral administration of YM-53601 at the concentration of 50 mg/kg, followed 1 h later by intraperitoneal injection of [14C] acetate (40.5 μCi per animal). The rats and the hamsters are anaesthetized with diethyl ether and killed 1 h after the [14C]-acetate injection. Cholesterol biosynthesis is assayed[1]. |
References: [1]. Ugawa T, et al. YM-53601, a novel squalene synthase inhibitor, suppresses lipogenic biosynthesis and lipid secretion in rodents. Br J Pharmacol. 2003 May;139(1):140-6. | |
YM-53601 is a squalene synthase inhibitor (IC50s = 79 and 90 nM in HepG2 cells and rat liver microsomes, respectively).1 It inhibits cholesterol biosynthesis in rats (ED50 = 32 mg/kg).1 YM-53601 dose-dependently reduces plasma triglyceride and non-HDL cholesterol levels in hamsters fed both normal and high-fat diets. It also reduces viral RNA, core and NS3 protein production, and secreted viral particles in Huh7.5.1-8 cells infected with the hepatitis C virus (HCV) strain JFH-1 without affecting cell viability at concentrations ranging from 0.5 to 1.5 μM.2 YM-53601 (1-10 μM) confers protection against cytotoxicity induced by the bacterial pore-forming toxin pneumolysin in HBE1 and normal human bronchial epithelial (NHBE) cells.3
1.Ugawa, T., Kakuta, H., Moritani, H., et al.YM-53601, a novel squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in several animal speciesBr. J. Pharmacol.13163-70(2000) 2.Saito, K., Shirasago, Y., Suzuki, T., et al.Targeting cellular squalene synthase, an enzyme essential for cholesterol biosynthesis, is a potential antiviral strategy against hepatitis C virusJ. Virol.89(4)2220-2232(2015) 3.Statt, S., Ruan, J.W., Hung, L.Y., et al.Statin-conferred enhanced cellular resistance against bacterial pore-forming toxins in airway epithelial cellsAm. J. Respir. Cell Mol. Biol.53(5)689-702(2015)
| Cas No. | 182959-28-0 | SDF | |
| Canonical SMILES | F/C(COC1=CC(NC2=C3C=CC=C2)=C3C=C1)=C4CN5CCC/4CC5 | ||
| 分子式 | C21H21FN2O | 分子量 | 336.4 |
| 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 | 2.9727 mL | 14.8633 mL | 29.7265 mL |
| 5 mM | 0.5945 mL | 2.9727 mL | 5.9453 mL |
| 10 mM | 0.2973 mL | 1.4863 mL | 2.9727 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。