GW0742

製品コードS8020 バッチS802001

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C21H17F4NO3S2
分子量 471.49 CAS No. 317318-84-6
Solubility (25°C)* 体外 DMSO 94 mg/mL (199.36 mM)
Ethanol 44 mg/mL (93.32 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
2%DMSO 40%PEG300 2%Tween80 56%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 3.000mg/ml (6.36mM) Taking the 1 mL working solution as an example, add 20 μL of 150 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 20 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 560 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 GW0742 is a potent and highly selective PPARβ/δ agonist, with IC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ.
in vitro GW0742 shows activity aganist hPPARα, hPPARγ and hPPARδ with EC50 of 1.1 μM, 2 μM and 1 nM, respectively, in cell based transactivation assay. [1] This compound (0.2 μM and 1 μM) significant increases in reporter activity of PPARβ/δ in N/TERT-1 keratinocytes. It (1 μM) results in significant inhibition in the average number of N/TERT-1 keratinocytes. The chemical (1 μM) results in an increase in the number of cells in the G1 phase and a decrease in the number of cells in the S phase. It (1 μM) causes a significant increase in the mRNA encoding ADRP, a known PPARβ/δ target gene, in N/TERT-1 keratinocytes as well as mouse primary keratinocytes. This agent (1 μM) results in significantly reduced phosphorylation of retinoblastoma (Rb) and a significantly lower level of p42/44 ERK in N/TERT-1 cells. It (1 μM) leads to an increase in the mRNA encoding a number of known markers of terminal differentiation including TG-I, SPR1A, K10 and involucrin. [2] This compound at 100 μM produces a significant reduction in low-KCl-induced neuronal cell death in cerebellar granule neurons. It at 100 μM induces a pronounced increase in cell death as measured by LDH release after 48 hr of incubation. The chemical at 100 μM produces a pronounced increase in c-Jun expression at 6 hours in cerebellar granule neuron cultures. It at 100 μM increases PPARα-mediated transactivation dependent on the presence of 1.5% BSA in MCF-7 cells. [3]
in vivo GW0742 (10 mg/kg) promotes reverse cholesterol transport in C57BL6/J mice. This compound (10 mg/kg) increases the fecal excretion of HDLderived cholesterol despite no effect on HDL cholesterol catabolism in C57BL6/J mice. It decreases NPC1L1 mRNA expression in the small intestine of mice. [4] This chemical (30 mg/kg), prior to induction of LPS-mediated pulmonary inflammation, results in a significant decrease in leukocyte recruitment into the pulmonary space in Male BALB/c mice. It (30 mg/kg) significantly decreases protein and mRNA levels of the pro-inflammatory cytokines IL-6, IL-1beta and TNFalpha in Bronchial alveolar lavage fluid of mice. [5]
特徴 Both GW0742 and L-165041 activate PPARβ, but not PPARγ or PPARα in platelets.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 N/TERT-1 keratinocytes
濃度 ~1 μM
反応時間 6 days
実験の流れ N/TERT-1 keratinocytes are seeded onto 6-well tissue culture dishes at 3×104 cells per well in Ker-SFM. Twenty-four hours later, cell number is measured with a Z1 coulter particle counter to determine plating efficiency (Day 0). For the remaining cells, medium is changed to Ker-SFM/DF-K, and cells are treated in triplicate with 0.1% DMSO, 0.1 μM or 1 μM GW0742. Cell number is determined at daily intervals, and the remaining cells are retreated with fresh media and this compound each day for up to 6 days.
動物実験 動物モデル Wild-type C57BL/6 female mice
投薬量 10 mg/kg
投与方法 Supplemented chow diet

参考

  • https://pubmed.ncbi.nlm.nih.gov/12699745/
  • https://pubmed.ncbi.nlm.nih.gov/17254750/
  • https://pubmed.ncbi.nlm.nih.gov/15211590/
  • https://pubmed.ncbi.nlm.nih.gov/20169010/
  • https://pubmed.ncbi.nlm.nih.gov/18622687/

カスタマーフィードバック

Data from [Data independently produced by , , Neuropharmacology, 2016, 113(Pt A):396-406. ]

Data from [Data independently produced by , , Sci Rep, 2017, 7:45234]

Data from [Data independently produced by , , Lab Invest, 2016, 96(2):218-29]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

PPAR-γ agonists reactivate the ALDOC-NR2F1 axis to enhance sensitivity to temozolomide and suppress glioblastoma progression [ Cell Commun Signal, 2024, 22(1):266] PubMed: 38741139
PPAR-γ agonists reactivate the ALDOC-NR2F1 axis to enhance sensitivity to temozolomide and suppress glioblastoma progression [ Cell Commun Signal, 2024, 22(1):266] PubMed: 38741139
A drug repurposing study identifies novel FOXM1 inhibitors with in vitro activity against breast cancer cells [ Med Oncol, 2024, 41(8):188] PubMed: 38918225
SWIM domain protein ZSWIM4 is required for JAK2 inhibition resistance in breast cancer [ Life Sci, 2021, 279:119696] PubMed: 34102191
Vascular PPARβ/δ Promotes Tumor Angiogenesis and Progression. [ Cells, 2019, 8(12)] PubMed: 31842402
PPAR δ inhibition protects against palmitic acid-LPS induced lipidosis and injury in cultured hepatocyte L02 cell. [ Int J Med Sci, 2019, 16(12):1593-1603] PubMed: 31839747
PPAR δ inhibition protects against palmitic acid-LPS induced lipidosis and injury in cultured hepatocyte L02 cell [ Int J Med Sci, 2019, 16(12):1593-1603] PubMed: 31839747
PPARβ/δ, a Novel Regulator for Vascular Smooth Muscle Cells Phenotypic Modulation and Vascular Remodeling after Subarachnoid Hemorrhage in Rats. [Zhang H, et al. Sci Rep, 2017, 7:45234] PubMed: 28327554
WNT/β-catenin signaling regulates cigarette smoke-induced airway inflammation via the PPARδ/p38 pathway. [Guo L, et al. Lab Invest, 2016, 96(2):218-29] PubMed: 26322419
PPARβ/δ activation protects against corticosterone-induced ER stress in astrocytes by inhibiting the CpG hypermethylation of MicroRNA-181a [Ji J, et al. Neuropharmacology, 2016, 10.1016/j.neuropharm.2016.10.022] PubMed: 27789312

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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