GW501516
(Synonyms: 2-(4-((2-(4-(三氟甲基)苯基)-5-甲基噻唑-4-基)甲基硫基)-2-甲基苯氧基)乙酸,GW 1516; GSK-516) 目录号 : GC15318
A selective PPARδ-agonist with anti-obesity activity
Cas No.:317318-70-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | GW 501516 is dissolved in DMSO. Cells are starved by incubation in 0.2% FCS DMEM for 9 h, then pre-incubated with GW 501516, at a final concentration of 2.5 and 5 µM, or 0.05% DMSO as control for 3 hours, followed by stimulation with 150 µM palmitate bound to 8.0% BSA for 12 h[3]. |
Animal experiment: | Rats: Female Sprague Dawley rats, 12 weeks of age, are allocated to a sham-operated group and 3 OVX groups; high-dose GW 501516 (OVX-GW5), low-dose GW 501516 (OVX-GW1), and a control group (OVX-CTR), respectively. Animals receive GW 501516 or vehicle (methylcellulose) daily for 4 months by gavage. Bone mineral density (BMD) is assessed by dual x-ray absorptiometry at the femur, spine, and whole body[2]. Mice: Mice are randomly allocated to different groups and receive therapeutic diet and treatment. The GW 501516-containing rodent diet is made by evenly adding GW 501516 to the control diet to a final concentration of 0.04% w/w. In the control diet, 10% of the total calories are from fat (5.5% from soybean oil and 4.5% from lard)[3]. |
References: [1]. Wei ZL, et al. A short and efficient synthesis of the pharmacological research tool GW501516 for the peroxisome proliferator-activated receptor delta. J Org Chem. 2003 Nov 14;68(23):9116-8. | |
GW501516 is subtype-selective small-molecule agonist of peroxisome proliferator-activated receptor δ (PPARδ) with Ki value of 1.1nM [1].
GW501516 is discovered by combinatorial chemistry and structure-based drug design to use as an ideal chemical tool to study the function of the ubiquitously expressed PPARδ. In the cell-based transfection assay, it induces expression of a GAL4-responsive reporter gene with EC50 value of 1.2nM. GW501516 shows more than 1000-fold selective for PPARδ over other subtypes. PPARδ is expressed in many tissues that contribute to cholesterol flux, and is a RXR of partner. As an agonist of PPARδ, GW501516 is found to increase the expression of ABCA1 as well as the apoA1-specific cholesterol efflux. In primate model of human metabolic disease, GW501516 increases the level of HDLc and lowers the fasting triglycerides. GW501516 also produces fewer, yet larger, LDL and VLDL particles results in a less atherogenic lipid composition. Furthermore, GW501516 partially corrects the hyperinsulinemia in primates without adverse effects on glycemic control [1, 2].
References:
[1] Wei ZL, Kozikowski AP. A short and efficient synthesis of the pharmacological research tool GW501516 for the peroxisome proliferator-activated receptor delta. J Org Chem. 2003 Nov 14;68(23):9116-8.
[2] Oliver WR Jr, Shenk JL, Snaith MR, Russell CS, Plunket KD, Bodkin NL, Lewis MC, Winegar DA, Sznaidman ML, Lambert MH, Xu HE, Sternbach DD, Kliewer SA, Hansen BC, Willson TM. A selective peroxisome proliferator-activated receptor delta agonist promotes reverse cholesterol transport. Proc Natl Acad Sci U S A. 2001 Apr 24;98(9):5306-11.
| Cas No. | 317318-70-0 | SDF | |
| 别名 | 2-(4-((2-(4-(三氟甲基)苯基)-5-甲基噻唑-4-基)甲基硫基)-2-甲基苯氧基)乙酸,GW 1516; GSK-516 | ||
| 化学名 | 2-[2-methyl-4-[[4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl]methylsulfanyl]phenoxy]acetic acid | ||
| Canonical SMILES | CC1=C(C=CC(=C1)SCC2=C(N=C(S2)C3=CC=C(C=C3)C(F)(F)F)C)OCC(=O)O | ||
| 分子式 | C21H18F3NO3S2 | 分子量 | 453.5 |
| 溶解度 | ≥ 18.05 mg/mL in DMSO, ≥ 44.6 mg/mL in EtOH | 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 | 2.2051 mL | 11.0254 mL | 22.0507 mL |
| 5 mM | 0.441 mL | 2.2051 mL | 4.4101 mL |
| 10 mM | 0.2205 mL | 1.1025 mL | 2.2051 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。