Product Details
Product Name:
CAFESTOL |
CAS No.:
469-83-0 |
Purity:
99.08% |
Supply Ability:
10g |
Release date:
2024/11/16 |
Product Introduction
Bioactivity
名稱 | CAFESTOL |
描述 | CAFESTOL is a ERK inhibitor for AP-1-targeted activity against PGE2 production and the mRNA expression of cyclooxygenase (COX)-2 in LPS-activated RAW264.7 cells. Cafestol has strong inhibitory activity on PGE2 production by suppressing the NF-kB activation pathway. |
動(dòng)物實(shí)驗(yàn) | Cafestol can postpone development of T2D in KKAy mice. Forty-seven male KKAy mice were randomized to consume chow supplemented daily with either 1.1 (high), 0.4 (low), or 0 (control) mg of cafestol for 10 weeks. Collected blood samples for fasting glucose, glucagon, and insulin as well as liver, muscle, and fat tissues for gene expression analysis. Isolated islets of Langerhans and measured insulin secretory capacity. After 10 weeks of intervention, fasting plasma glucose was 28-30% lower in cafestol groups compared with the control group (p < 0.01). Fasting glucagon was 20% lower and insulin sensitivity improved by 42% in the high-cafestol group (p < 0.05). Cafestol increased insulin secretion from isolated islets by 75-87% compared to the control group (p < 0.001)[2]. |
體外活性 | The precise molecular mechanism of the antiinflammatory activity of cafestol in terms of prostaglandin E(2) (PGE(2)) production, a critical factor involved in inflammatory responses. Cafestol inhibited both PGE(2) production and the mRNA expression of cyclooxygenase (COX)-2 from lipopolysaccharide (LPS)-treated RAW264.7 cells. This compound strongly decreased the translocation of c-Jun into the nucleus and AP-1 mediated luciferase activity. In kinase assays using purified extracellular signal-regulated kinase 2 (ERK2) or immunoprecipitated ERK prepared from LPS-treated cells in the presence or absence of cafestol, it was found that this compound can act as an inhibitor of ERK2 but not of ERK1 and mitogen-activated protein kinase kinase 1 (MEK 1). Suggest that cafestol may be a novel ERK inhibitor with AP-1-targeted inhibitory activity against PGE(2) production in LPS-activated RAW264.7 cells[1]. |
體內(nèi)活性 | CAFESTOL possesses antidiabetic properties in KKAy mice. Consequently, cafestol may contribute to the reduced risk of developing T2D in coffee consumers and has a potential role as an antidiabetic drug[2]. |
存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 5 mg/mL (15.8 mM)
|
關(guān)鍵字 | Inhibitor | ERK | CAFESTOL | Nuclear factor-kappaB | NF-κB | Cyclooxygenase | PGE synthase | Nuclear factor-κB | COX | Prostaglandin E synthase | inhibit | Extracellular signal regulated kinases |
相關(guān)產(chǎn)品 | TBHQ | Bismuth Subsalicylate | Ibuprofen | Acetaminophen | Diclofenac sodium | Diethylmaleate | Diclofenac Potassium | Lidocaine hydrochloride | Indomethacin sodium hydrate | Glafenine | Trometamol | Revaprazan hydrochloride |
相關(guān)庫(kù) | 抗癌天然產(chǎn)物庫(kù) | 萜類天然產(chǎn)物庫(kù) | 中藥單體化合物庫(kù) | 疼痛相關(guān)化合物庫(kù) | 植物來(lái)源化合物庫(kù) | 激酶抑制劑庫(kù) | 中藥抗炎分子庫(kù) | 天然產(chǎn)物庫(kù) | 高通量篩選天然產(chǎn)物庫(kù) | 抗癌活性化合物庫(kù) |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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