Indeglitazar (PPM 204)
(Synonyms: PPM 204) 目录号 : GC31408
Indeglitazar (PPM 204) (PPM 204) 是一种可口服的 PPAR 泛激动剂，适用于所有三种 PPARα, PPARδ和PPARγ；。
Cas No.:835619-41-5
Sample solution is provided at 25 µL, 10mM.
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Indeglitazar is an orally available peroxisome proliferator-activated receptor (PPAR) pan-agonist for all three PPAR subtypes alpha (α), delta (δ) and gamma (γ).
In an assay of preadipocyte differentiation, measuring in part functional insulin sensitization capability of the cells, Indeglitazar shows an EC50 of 0.32 μM compared with Rosiglitazone, which shows an EC50 of 13 nM, although the maximal response obtained from the 2 compounds is comparable[1].
An initial assessment of in vivo activity is carried out using the Zucker rat model of diabetes. The significant lowering of glucose, HbA1C, triglycerides, and total cholesterol are observed after i.v. treatment with 10 mg/kg Indeglitazar once per day for 3 weeks. Notably, the level of Adiponectin (on day 21) is essentially unchanged in treated vs. untreated animals (4.8 mcg/mL vs. 4.9 mcg/mL), thus the observed reductions in glucose and HbA1C are achieved in an adiponectin-independent fashion. These differences in the effects of Indeglitazar in vivo may be a consequence of synergy between the 3 PPAR activities or because of the SPPARM profile of the compound, or a combination of these factors. The oral activity of Indeglitazar is assessed in the ob/ob model of diabetes and insulin resistance. Indeglitazar significantly decreases glucose, insulin, triglycerides, and free fatty acid levels[1].
[1]. Artis DR, et al. Scaffold-based discovery of Indeglitazar, a PPAR pan-active anti-diabetic agent. Proc Natl Acad Sci U S A. 2009 Jan 6;106(1):262-7.
Kinase experiment: | The purified PPAR_ LBD protein is diluted to 12 mg/mL and 1mM of Indeglitazar and 2x molar excess of steroid receptor coactivator-1 (SRC-1) peptide are added before crystallization by mixing equal volumes of a protein/compound sample with reservoir solution containing 27% polyethylene glycol (PEG) 4000, 0.1 M 2-(bis-(2-hydroxy-ethyl)-amino)-2-hydroxymethyl- propane-1,3-diol (BisTris) buffer at pH 6.5, 0.2 M ammonium acetate, and 5% glycerol. The crystals are soaked in cryo-protective buffer (30% PEG 4000, 0.1 M BisTris buffer at pH 6.5, 0.2 M ammonium acetate, and 5% glycerol) before flash-freezing in liquid nitrogen for data collection[1]. |
Animal experiment: | Rats[1]Indeglitazar is administered once daily i.v. as a solution (10% SolutolHS15,10%ethanol,80%saline) to ZDF/GmiCrl-fa/fa rats. Treatment is initiated at age 7-8 weeks, and blood samples are analyzed before the treatment and 21 days after the treatment.Mice[1]Ob/ob mouse study. Indeglitazar (10 mg/kg) or Pioglitazone (30 mg/kg) are orally administered to 9-week-old B6.V-Lepob mice for 14 days. Compounds are suspected in 0.5% methylcellulose and 2% Tween 80 before dosing. On the last day, blood is collected for insulin, triglyceride, free fatty acid, and adiponectin measurements. |
References: [1]. Artis DR, et al. Scaffold-based discovery of Indeglitazar, a PPAR pan-active anti-diabetic agent. Proc Natl Acad Sci U S A. 2009 Jan 6;106(1):262-7. | |
| Cas No. | 835619-41-5 | SDF | |
| 别名 | PPM 204 | ||
| Canonical SMILES | O=C(O)CCC1=CN(S(=O)(C2=CC=C(OC)C=C2)=O)C3=C1C=C(OC)C=C3 | ||
| 分子式 | C19H19NO6S | 分子量 | 389.42 |
| 溶解度 | DMSO : 33 mg/mL (84.74 mM) | 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 | 2.5679 mL | 12.8396 mL | 25.6792 mL |
| 5 mM | 0.5136 mL | 2.5679 mL | 5.1358 mL |
| 10 mM | 0.2568 mL | 1.284 mL | 2.5679 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
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet