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product name
辣椒平, ≥98% (HPLC), solid
品質等級
化驗
≥98% (HPLC)
形狀
solid
顏色
off-white
溶解度
DMSO: >10 mg/mL, clear
儲存溫度
2-8°C
SMILES 字串
Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc3ccc(Cl)cc3
InChI
1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25)
InChI 密鑰
DRCMAZOSEIMCHM-UHFFFAOYSA-N
基因資訊
human ... TRPV1(7442) , TRPV4(59341)
rat ... Trpv1(83810)
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應用
辣椒平作为瞬时受体电位香草醛-1(TRPV1)拮抗剂的应用实例：
- 研究其对辣椒素诱导的胞外信号调节激酶(ERK)磷酸化的影响作用
- 研究TRPV1在大鼠伤害感受器中枢神经末梢的作用
- 公牛精子中TRPV1的功能表征
生化／生理作用
辣椒平(Capsazepine)是人工合成的辣椒素类似物和瞬时受体电位香草醛-1(TRPV1)拮抗剂。在多种癌症中具有抗增殖和抗癌作用，包括口腔鳞状细胞癌、非小细胞肺癌(NSCLC)、乳腺癌和前列腺癌细胞株（HSC-3、H460、MDA-231和PC-3）。辣椒平可恢复在内毒素血症中受损的肺机能，可作为急性肺损伤(ALI)的潜在治疗药物。
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
個人防護裝備
Eyeshields, Gloves, type N95 (US)
其他客户在看
Ablation and regeneration of peripheral and central TRPV1 expressing nerve terminals and the consequence of nociception
Yu SQ and Premkumar LS
Open Medicine : A Peer-Reviewed, Independent, Open-Access Journal, 8(1) (2015)
S Bevan et al.
British journal of pharmacology, 107(2), 544-552 (1992-10-01)
1. Capsazepine is a synthetic analogue of the sensory neurone excitotoxin, capsaicin. The present study shows the capsazepine acts as a competitive antagonist of capsaicin. 2. Capsazepine (10 microM) reversibly reduced or abolished the current response to capsaicin (500 nM)
Jorge De La Chapa et al.
Bioorganic & medicinal chemistry, 27(1), 208-215 (2018-12-12)
We previously demonstrated that capsazepine (CPZ), a synthetic transient receptor potential Vanilloid subtype 1 (TRPV1) antagonist, has significant anti-cancer effects in vivo. The purpose of this study was to develop more potent analogs based upon CPZ pharmacophore and structure-activity relationships
Tatsuo Iwashita et al.
Neuroscience research, 77(1-2), 110-119 (2013-08-22)
Extracellular signal-regulated kinase (ERK) is known to be phosphorylated after exposure to noxious stimuli. In this study, we investigated the response in the dura mater to nociceptive stimulation, which is thought to be responsible for the pathogenesis of headaches, including
Layla D M Cabral et al.
Basic & clinical pharmacology & toxicology, 119(5), 421-427 (2016-04-20)
Acute lung injury (ALI) caused by systemic inflammatory response remains a leading cause of morbidity and mortality in critically ill patients. Management of patients with sepsis is largely limited to supportive therapies, reflecting an incomplete understanding of the underlying pathophysiology.
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