Naveglitazar racemate
(Synonyms: LY519818 racemate) 目录号 : GC31450
Naveglitazarracemate是Naveglitazar的外消旋体。Naveglitazar是过氧化物酶体增殖物激活受体(PPAR)α-γ双重，γ显性激动剂，在动物模型具有降低葡萄糖潜力。
Cas No.:916085-47-7
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
Kinase experiment: | Plasma protein binding of Naveglitazar is investigated using [3H]Naveglitazar and an ultracentrifugation technique. Mouse, rat, and monkey plasma is spiked at concentrations of 0.1, 1, 10, 100, and 1000 ng of [3H]Naveglitazar/mL and incubated for 1 h at 37°C. After incubation, three 1.2 mL aliquots are centrifuged at 130,000 rpm for 3.25 h at 37°C. Aliquots of the unbound fraction are diluted with 10 mL of scintillation fluid and analyzed by liquid scintillation counting[1]. |
Animal experiment: | The single-dose plasma pharmacokinetics of Naveglitazar, LY591026, and radioactivity are studied in male ICR mice, and male Fischer 344 rats after oral administration of [14C]Naveglitazar. A separate study is conducted in rats to evaluate the pharmacokinetics of Naveglitazar and LY591026 after the administration of a single 10 mg/kg dose of each compound. Mice and rats are administered a 10 mg/kg oral dose of [14C]Naveglitazar with a specific activity of 50 μCi/kg[1]. Mice[1] Mice are divided into three groups. Group 1 animals (n=3 per time point) are housed in shoebox cages and are used to determine the pharmacokinetics of Naveglitazar, LY591026, and radioactivity. Blood samples are collected for plasma from mice via cardiac puncture at 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, and 120 h postdose. Group 2 mice are housed in metabolism cages (n=3 per cage) for the collection of excreta to determine the mass balance and metabolism of Naveglitazar. Urine, feces, and cage wash are collected in 24 h intervals for up to 120 h. The third group of animals (n=3 per time point) are housed in shoebox cages and used to evaluate the metabolites present in plasma. Rat[1] Rats are divided into three groups. Group 1 animals (n=3 per time point) are housed in shoebox cages and are used to determine the pharmacokinetics of Naveglitazar, LY591026, and radioactivity. Blood samples are collected for plasma from rats via cardiac puncture at 0.5, 1, 2, 4, 8, 12, 24, 48, and 72 h postdose. Group 2 rats (n=4) are individually housed in metabolism cages for the collection of excreta to determine the mass balance and metabolism of Naveglitazar. Urine, feces, and cage wash are collected in 24 h intervals for up to 120 h. Group 3 animals, which are bile-cannulated rats (n=4), are individually housed in metabolism cages for the collection of excreta to determine the mass balance and metabolism of Naveglitazar. Urine, feces, and cage wash are collected in 24 h intervals for up to 72 h, whereas bile is collected in 8-h intervals. In a separate study, rats are given Naveglitazar or LY591026. In this study, blood samples for plasma are collected at 0.5, 1, 2, 4, 8, 12, and 24 h to determine pharmacokinetics of each analyte. |
References: [1]. Yi P, et al. The disposition and metabolism of naveglitazar, a peroxisome proliferator-activated receptor alpha-gamma dual, gamma-dominant agonist in mice, rats, and monkeys. Drug Metab Dispos. 2007 Jan;35(1):51-61. | |
Naveglitazar racemate is the racemate of Naveglitazar. Naveglitazar is a nonthiozolidinedione peroxisome proliferator-activated receptor (PPAR) α-γ dual, γ-dominant agonist that has shown glucose-lowering potential in animal models and in the clinic.
Naveglitazar, a non-thiazolidinediones (TZD), functions as a potent and efficacious insulin sensitizer in rodents, possessing a novel profile that may result in an improved therapeutic agent for the treatment of type 2 diabetes and associated dyslipidemia. The extent of in vitro binding of [3H]Naveglitazar to plasma proteins is evaluated by ultracentrifugation in mouse, rat, and monkey plasma. The mean percentages±S.E.M. of protein binding of radioactivity in plasma over the concentration range of 0.1 to 1000 ng/ml after in vitro incubation at 37°C for 60 min are 99.5%±0.1% (mice), 99.6%±0.1% (rat), and 99.6%±0.3% (monkey). These results show that Naveglitazar is highly bound to plasma proteins among the species examined, and binding is independent of concentration[1].
[14C]Naveglitazar is quickly absorbed and moderately metabolized before elimination. After oral administration, 47, 31, and 62% of the radioactivity, as assessed by AUC values, are circulating as metabolites in mice, rats, and monkeys, respectively. Half-lives for Naveglitazar and radioactivity are similar within each species; however, monkeys have substantially longer half-lives in comparison to mice and rats. Naveglitazar and radioactivity are slowly cleared from the system circulation in all species evaluated[1].
[1]. Yi P, et al. The disposition and metabolism of naveglitazar, a peroxisome proliferator-activated receptor alpha-gamma dual, gamma-dominant agonist in mice, rats, and monkeys. Drug Metab Dispos. 2007 Jan;35(1):51-61.
| Cas No. | 916085-47-7 | SDF | |
| 别名 | LY519818 racemate | ||
| Canonical SMILES | O=C(O)C(OC)CC1=CC=C(OCCCOC2=CC=C(OC3=CC=CC=C3)C=C2)C=C1 | ||
| 分子式 | C25H26O6 | 分子量 | 422.47 |
| 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 | 2.367 mL | 11.8352 mL | 23.6703 mL |
| 5 mM | 0.4734 mL | 2.367 mL | 4.7341 mL |
| 10 mM | 0.2367 mL | 1.1835 mL | 2.367 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。