Arhalofenate (MBX 102)
(Synonyms: 芳卤芬酯; MBX 102; JNJ 39659100) 目录号 : GC31462
A prodrug form of a PPARγ partial agonist
Cas No.:24136-23-0
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
Arhalofenate is an orally bioavailable prodrug form of the free acid form of a peroxisome proliferator-activated receptor γ (PPARγ) partial agonist.1 It is converted to the active free acid form by nonspecific serum esterases. Arhalofenate has weak PPARγ transactivation activity in a reporter assay but strong transrepression activity, reducing LPS-induced chemokine (C-C motif) ligand 2 (CCL2) secretion in isolated mouse peritoneal macrophages. It reduces fasting plasma glucose levels in ob/ob mouse and Zucker diabetic fatty (ZDF) rat models of type 2 diabetes when administered at doses of 125 and 100 mg/kg, respectively. It also decreases fasting free fatty acid, triglyceride, and cholesterol levels in ZDF rats without increasing body weight when administered at a dose of 100 mg/kg.2 Arhalofenate (250 mg/kg) prevents leukocyte and neutrophil infiltration and IL-1β, IL-6, and chemokine (C-X-C motif) ligand 1 (CXCL1) production in air pouch fluid in a mouse model of gout.3
1.Gregoire, F.M., Zhang, F., Clarke, H.J., et al.MBX-102/JNJ39659100, a novel peroxisome proliferator-activated receptor-ligand with weak transactivation activity retains antidiabetic properties in the absence of weight gain and edemaMol. Endocrinol.23(7)975-988(2009) 2.Chandalia, A., Clarke, H.J., Clemens, L.E., et al.MBX-102/JNJ39659100, a novel non-TZD selective partial PPAR-γ agonist lowers triglyceride independently of PPAR-α activationPPAR Res.706852(2009) 3.McWherter, C., Choi, Y.-J., Serrano, R.L., et al.Arhalofenate acid inhibits monosodium urate crystal-induced inflammatory responses through activation of AMP-activated protein kinase (AMPK) signalingArthritis Res. Ther.20(1)204(2018)
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4051 mL | 12.0253 mL | 24.0506 mL |
| 5 mM | 0.481 mL | 2.4051 mL | 4.8101 mL |
| 10 mM | 0.2405 mL | 1.2025 mL | 2.4051 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。