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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C19H21ClN2O2S |
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分子量 | 376.90 | CAS No. | 138977-28-3 | ||||
Solubility (25°C)* | 体外 | DMSO | 75 mg/mL (198.99 mM) | ||||
Ethanol | 38 mg/mL (100.82 mM) | ||||||
Water | Insoluble | ||||||
体内 (毎回新しく調製した物を用意してください) |
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* <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. |
製品説明 | Capsazepine acts as a competitive antagonist of capsaicin and a transient receptor potential vanilloid type 1(TRPV1) antagonist. If you want to do cell experiments, please select batch 01. |
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in vitro | Capsazepine(CPZ) at a concentration of 94.2 µg/ml (IC50 concentration of capsazepine) exhibits a statistically significant inhibition of osteoclast growth and proliferation[2]. Capsazepine converts the NKA into Na-ATPase. CPZ inhibits K+-dependent activity but allows Na-ATPase associated with Na+ transport. CPZ has no effect on Na-ATPase measured in the absence of K+. CPZ also inhibits para-nitrophenyl phosphatase activity, albeit with a lower affinity. CPZ strongly reduces the steady-state EP level and the Na+ affinity for phosphorylation decreased 3-fold after CPZ treatment. In summary, CPZ blocks an Na+/K+ cycle in the NKA but leaves an Na+ cycle intact, reducing the transport stoichiometry of the pump[3]. Capsazepine inhibits osteoclast formation and bone resorption in a dose dependent manner in bone marrow-osteoblast co-cultures and RANKL generated osteoclast cultures. Capsazepine also suppresses RANKL induced IκB and ERK1/2 phosphorylation and causes apoptosis of mature osteoclasts and also inhibits alkaline phosphatase activity and bone nodule formation in calvarial osteoblast cultures[4]. |
in vivo | Capsazepine pre-treatment prevents the increase in respiratory system resistance and decreases the increase in tissue damping during endotoxemia. Capsazepine also attenuates lung injury by a reduction in the collapsed area of the lung parenchyma induced by lipopolysaccharide (LPS). |
細胞アッセイ | 細胞株 | Murine macrophage cell line RAW 264.7 |
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濃度 | 94.2 µg/ml | |
反応時間 | 72 h | |
実験の流れ | The cells are plated and treated with different concentrations of the test compounds and allowed to proliferate for 72 h. After 72 h of proliferation the cells are fixed in 10% formalin saline (50 μl/well) for 30 min. Then the cells are stained with crystal violet (0.05% w/v) for 30 min. The wells are then washed thoroughly with distilled water to remove any unbound dye and destained with Sorenson's buffer (0.1 M sodium citrate in 50% ethanol, pH 4.2). The absorbance of the extracted stain is measured at 540 nm. |
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動物実験 | 動物モデル | Adult male Swiss mice |
投薬量 | 15 mg/kg | |
投与方法 | s.c. |
Mechanical manipulation of cancer cell tumorigenicity via heat shock protein signaling [ Sci Adv, 2023, 9(27):eadg9593] | PubMed: 37418519 |
Microglial Piezo1 senses Aβ fibril stiffness to restrict Alzheimer's disease [ Neuron, 2022, S0896-6273(22)00954-0] | PubMed: 36368316 |
The effect of Ma-Xin-Gan-Shi decoction on asthma exacerbated by respiratory syncytial virus through regulating TRPV1 channel [ J Ethnopharmacol, 2022, 291:115157] | PubMed: 35247474 |
Generation of GCaMP6s-Expressing Zebrafish to Monitor Spatiotemporal Dynamics of Calcium Signaling Elicited by Heat Stress [ Int J Mol Sci, 2021, 22(11)5551] | PubMed: 34074030 |
Evodiamine induces ROS-Dependent cytotoxicity in human gastric cancer cells via TRPV1/Ca2+ pathway [ Chem Biol Interact, 2021, 351:109756] | PubMed: 34808100 |
Ca2+-permeable TRPV1 pain receptor knockout rescues memory deficits and reduces amyloid-β and tau in a mouse model of Alzheimer's disease. [ Hum Mol Genet, 2020, 29(2):228-237] | PubMed: 31814000 |
Dual-targeting Rutaecarpine-NO donor hybrids as novel anti-hypertensive agents by promoting release of CGRP [Ma J Eur J Med Chem, 2019, 168:146-153] | PubMed: 30818175 |
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。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。