MHY553
(Synonyms: NSC 33005) 目录号 : GC49521
An agonist of PPARα
Cas No.:6265-56-1
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
MHY553 is an agonist of peroxisome proliferator-activated receptor α (PPARα).1 It activates PPARα in HepG2 cells in a reporter assay when used at a concentration of 1 µM but does not activate PPARβ or PPARγ at 10 µM. MHY553 (3 µM) prevents triglyceride accumulation induced by the liver X receptor (LXR) agonist T0901317 in HepG2 cells, as well as scavenges reactive oxygen species (ROS) and peroxynitrite in cell-free assays (IC50s = 39.7 and 2.39 µM, respectively).1,2 It also inhibits β-glucuronidase and tyrosinase (IC50s = 8.9 and 0.01 µM for the bovine liver and mushroom enzymes, respectively).3,4 MHY553 (5 mg/kg) reduces age-induced increases in liver weight and triglyceride levels in a rat model of hepatic steatosis.1
1.Kim, S.M., Lee, B., An, H.J., et al.Novel PPARα agonist MHY553 alleviates hepatic steatosis by increasing fatty acid oxidation and decreasing inflammation during agingOncotarget8(28)46273-46285(2017) 2.Jung, H.J., Kim, S.M., Kim, D.H., et al.2,4-Dihydroxyphenyl-benzo[d]thiazole (MHY553), a synthetic PPARα agonist, decreases age-associated inflammatory responses through PPARα activation and RS scavenging in the skinExp. Gerontol.143111153(2021) 3.Khan, K.M., Rahim, F., Halim, S.A., et al.Synthesis of novel inhibitors of β-glucuronidase based on benzothiazole skeleton and study of their binding affinity by molecular dockingBioorg. Med. Chem.19(14)4286-4294(2011) 4.Ha, Y.M., Park, J.Y., Park, Y.J., et al.Synthesis and biological activity of hydroxy substituted phenyl-benzo[d]thiazole analogues for antityrosinase activity in B16 cellsBioorg. Med. Chem. Lett.21(8)2445-2449(2011)
| Cas No. | 6265-56-1 | SDF | Download SDF |
| 别名 | NSC 33005 | ||
| Canonical SMILES | OC1=CC(O)=C(C2=NC3=CC=CC=C3S2)C=C1 | ||
| 分子式 | C13H9NO2S | 分子量 | 243.3 |
| 溶解度 | DMSO: 24.5 mg/ml | 储存条件 | -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 | 4.1102 mL | 20.5508 mL | 41.1015 mL |
| 5 mM | 0.822 mL | 4.1102 mL | 8.2203 mL |
| 10 mM | 0.411 mL | 2.0551 mL | 4.1102 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。
2,4-Dihydroxyphenyl-benzo[d]thiazole (MHY553), a synthetic PPARα agonist, decreases age-associated inflammatory responses through PPARα activation and RS scavenging in the skin
Exp Gerontol 2021 Jan;143:111153.PMID:33189833DOI:10.1016/j.exger.2020.111153.
We previously reported that 2,4-dihydroxyphenyl-benzo[d]thiazole (MHY553) is a PPARα agonist, which has been shown to inhibit tyrosinase activity in murine melanocyte and alleviate hepatic steatosis in aged rats. This study investigated the effects of MHY553 on the age-related occurrence of inflammatory responses via the molecular modulation of the nuclear factor-κB (NF-κB) signaling pathway in the skin of aged rats and skin fibroblast cells. Moreover, we investigated the antioxidant effect of MHY553 via in vitro assays of reactive oxygen species (ROS) and peroxynitrite (ONOO-) scavenging activities. We also scrutinized the ability of MHY553 as a PPARα activator in aged rat skin and H2O2-induced Hs27 fibroblast cells. In vivo experiments were performed in young, aged, and MHY553-fed aged rats (3 mg or 5 mg∙kg -1∙day -1 for 4 weeks). MHY553 dose-dependently scavenged ROS and ONOO-. Furthermore, we found that MHY553 suppressed the NF-κB transcription factor and downregulated mitogen-activated protein kinase (MAPK)/activator protein-1 (AP-1) signaling. MHY553 also inhibited the expression of pro-inflammatory cytokines including COX-2, iNOS, IL-1β, and IL-6. Our findings indicate the MHY553 scavenges ROS/reactive nitrogen species and inhibits inflammatory cytokines through PPARα activation in the skin. Thus, these results suggest that MHY553 may be of therapeutic interest for protecting skin from oxidative stress-induced damage and intrinsic aging.
Novel PPARα agonist MHY553 alleviates hepatic steatosis by increasing fatty acid oxidation and decreasing inflammation during aging
Oncotarget 2017 Jul 11;8(28):46273-46285.PMID:28545035DOI:10.18632/oncotarget.17695.
Hepatic steatosis is frequently observed in obese and aged individuals. Because hepatic steatosis is closely associated with metabolic syndromes, including insulin resistance, dyslipidemia, and inflammation, numerous efforts have been made to develop compounds that ameliorate it. Here, a novel peroxisome proliferator-activated receptor (PPAR) α agonist, 4-(benzo[d]thiazol-2-yl)benzene-1,3-diol (MHY553) was developed, and investigated its beneficial effects on hepatic steatosis using young and old Sprague-Dawley rats and HepG2 cells.Docking simulation and Western blotting confirmed that the activity of PPARα, but not that of the other PPAR subtypes, was increased by MHY553 treatment. When administered orally, MHY553 markedly ameliorated aging-induced hepatic steatosis without changes in body weight and serum levels of liver injury markers. Consistent with in vivo results, MHY553 inhibited triglyceride accumulation induced by a liver X receptor agonist in HepG2 cells. Regarding underlying mechanisms, MHY553 stimulated PPARα translocation into the nucleus and increased mRNA levels of its downstream genes related to fatty acid oxidation, including CPT-1A and ACOX1, without apparent change in lipogenesis signaling. Furthermore, MHY553 significantly suppresses inflammatory mRNA expression in old rats. In conclusion, MHY553 is a novel PPARα agonist that improved aged-induced hepatic steatosis, in part by increasing β-oxidation signaling and decreasing inflammation in the liver. MHY553 is a potential pharmaceutical agent for treating hepatic steatosis in aging.