G3335
(Synonyms: G3335) 目录号 : GC15085
A PPARγ antagonist III
Cas No.:36099-95-3
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
Kd = 8.34 μM
G3335 is a PPARγ antagonist.
The peroxisome proliferator-activated receptor gamma (PPARgamma) is a key therapeutic drug target for several conditions, such as inflammation, diabetes, hypertension, dyslipidemia, and cancer.
In vitro: Biacore 3000 study based on the surface plasmon resonance technique found that G3335 exhibited a highly specific binding affinity against PPARgamma and was able to block rosiglitazone, a potent PPARgamma agonist, in the stimulation of the interaction between the PPARgamma ligand-binding domain (LBD) and RXRalpha-LBD. Moreover, the yeast two-hybrid assays indicated that G3335 had strong antagonistic activity in perturbing rosiglitazone in the promotion of the PPARgamma-LBD-CBP interaction. In addition, G3335 could competitively bind to PPARgamma against 0.1 microM rosiglitazone to repress reporter-gene expression [1].
In vivo: In a previous study, the effect of rosiglitazone was examined on spinal cord injury (SCI) in rats. The animals were randomly divided into vehicle group, rosiglitazone treated group, and G3335 treated group. Locomotor function recovery was evaluated. Results showed that compared with the vehicle groups, the rosiglitazone could significantly ameliorate locomotor recovery, reduce NF-κB expression, and increase the proliferation of endogenous NPCs. In addition, when the PPAR-γ antagonist G3335 was applied, such effects were abolished [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Ye, F. ,Zhang, Z.S.,Luo, H.B., et al. The dipeptide H-Trp-Glu-OH shows highly antagonistic activity against PPARγ: Bioassay with molecular modeling simulation. ChemBioChem 7, 74-82 (2006).
[2] Meng, Q. Q.,Liang, X.J.,Wang, P., et al. Rosiglitazone enhances the proliferation of neural progenitor cells and inhibits inflammation response after spinal cord injury. Neuroscience Letters 503, 191-195 (2011).
| Cas No. | 36099-95-3 | SDF | |
| 别名 | G3335 | ||
| 化学名 | L-tryptophyl-L-glutamic acid | ||
| Canonical SMILES | OC(CC[C@@H](C(O)=O)NC([C@@H](N)CC1=CNC2=C1C=CC=C2)=O)=O | ||
| 分子式 | C16H19N3O5 | 分子量 | 333.3 |
| 溶解度 | ≥ 14.35mg/mL 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 | 3.0003 mL | 15.0015 mL | 30.003 mL |
| 5 mM | 0.6001 mL | 3.0003 mL | 6.0006 mL |
| 10 mM | 0.3 mL | 1.5002 mL | 3.0003 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。
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