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1-[(4-氯苯基)甲基]-2-(吡咯烷-1-基甲基)苯并咪唑鹽酸鹽
鹽酸克立咪唑
鹽酸克立咪唑|T1822L|TargetMol
價格
詢價
包裝
1removed
最小起訂量
1removed
發(fā)貨地
上海
更新日期
2024-12-12
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產品詳情
中文名稱:
鹽酸克立咪唑
英文名稱:
Clemizole hydrochloride
CAS:
1163-36-6
品牌:
TargetMol
產地:
美國
保存條件:
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
純度規(guī)格:
99.91%
產品類別:
抑制劑
貨號:
T1822L
2024-12-12
鹽酸克立咪唑
Clemizole hydrochloride
1removed/RMB
TargetMol
美國
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
99.91%
抑制劑
Product Introduction
Bioactivity
名稱
Clemizole hydrochloride
描述
Clemizole hydrochloride is an antagonist for H1 histamine receptor. According to the research, Clemizole hydrochloride can inhibit hepatitis C virus (HCV) replication and NS4B's RNA binding.
細胞實驗
Clemizole hydrochloride is dissolved in DMSO and stored, and then diluted with appropriate media before use[1]. Huh7.5 cells are maintained in DMEM supplemented with 1% L-Glutamine, 1% Penicillin, 1% Streptomycin, 1× nonessential amino acids and 10% FBS. Cell lines are passaged twice weekly after treatment with 0.05% trypsin-0.02% EDTA and seeding at a dilution of 1:5. Subconfluent Huh7.5 cells are trypsinized and collected by centrifugation at 700 g for 5 min. The cells are then washed three times in ice-cold RNase-free PBS and resuspended at 1.5×107 cells/mL in PBS. Wild-type or mutant FL-J6/JFH-5′C19Rluc2AUbi RNA for electroporation is generated by transcription of XbaI linearized DNA templates using the T7 MEGAscript kit, followed by purification (RNA transcription and fluorescent labeling). We mixed 5 μg of RNA with 400 μL of washed Huh7.5 cells in a 2-mm-gap cuvette (BTX) and immediately pulsed (0.82 kV, five 99 μs pulses) with a BTX-830 electroporator. After a 10 min recovery at 25°C, pulsed cells are diluted into 10 mL of prewarmed growth medium. Cells from several electroporations are pooled to a common stock and seeded in 6-well plates (5×105 cells per well). After 24 h, medium is replaced and cells are grown in the presence of serial dilutions of the various inhibitory compounds (e.g., Clemizole hydrochloride) identified in the screen. Seventeen commercially available compounds, out of the 18 identified, are analyzed. Untreated cells are used as a negative control for water-soluble compounds. For compounds (e.g., Clemizole hydrochloride) solubilized in DMSO, untreated cells are grown in the presence of corresponding concentrations of the solvent as a negative control. Medium is changed daily. After 72 h of treatment cells are subjected to an Alamar Blue-based viability assay and luciferase assay. After 72 h of treatment cells are incubated for 3 h at 37°C in the presence of 10% Alamar Blue reagent.Plates are then scanned and fluorescence is detected by using FLEXstation II 384. Depending on the inhibitory compound's solvent (e.g., Clemizole hydrochloride), water or DMSO, signal is normalized relatively to untreated samples or samples grown in the presence of DMSO, respectively[1].
體外活性
Clemizole hydrochloride is found to inhibit HCV RNA replication in cell culture that is mediated by its suppression of NS4B's RNA binding, with little toxicity for the host cell. The EC50 of Clemizole on the W55R mutant J6/JFH RNA is ~18 μM (2.25 times the EC50 of the wild-type RNA)[1]. Clemizole is a novel inhibitor of TRPC5 channels. Clemizole efficiently blocks TRPC5 currents and Ca2+ entry in the low micromolar range (IC50=1.0-1.3 μM). Clemizole exhibits a six-fold selectivity for TRPC5 over TRPC4β (IC50=6.4 μM), the closest structural relative of TRPC5, and an almost 10-fold selectivity over TRPC3 (IC50=9.1 μM) and TRPC6 (IC50=11.3 μM). Clemizole hydrochloride as a novel blocker of TRPC5 with a half-maximal inhibitory concentration of 1.1 μM. The concentration-response curves confirmed a concentration-dependent block of TRPC5 by Clemizole and revealed an apparent IC50 of 1.1±0.04 μM[2].
體內活性
Clemizole hydrochloride has an unexpectedly short plasma half-life (measured at 0.15 hours) which is very rapidly biotransformed into a glucuronide (M14) and a dealkylated metabolite (M12) and into a variety of lesser metabolites in C57BL/6J mice[3].
存儲條件
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度
DMSO : 18.11 mg/mL (50 mM)
H2O : 7.25 mg/mL (20 mM)
關鍵字
HCV Protease | TRP Channel | Transient receptor potential channels | Hepatitis C virus | Histamine Receptor | Inhibitor | Clemizole Hydrochloride | inhibit | Clemizole hydrochloride | Clemizole | HCV
相關產品
Famotidine | Meclizine dihydrochloride | Camphor | Lidocaine | Alginic acid | Sodium butanoate | trans-Cinnamaldehyde | Artemisinin | EIDD-1931 | Methyl 2-amino-5-bromobenzoate | 1,4-Cineole | Ribavirin
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抑制劑庫 | 抗癌上市藥物庫 | 經典已知活性庫 | 抗癌活性化合物庫 | 已知活性化合物庫 | 離子通道庫 | 抗病毒庫 | GPCR靶點分子庫 | 膜蛋白靶向化合物庫 | 免疫/炎癥分子化合物庫 | 疼痛相關化合物庫 | 抗癌臨床化合物庫
關鍵字:
克立咪唑鹽酸|||鹽酸克立咪唑|TargetMol
公司簡介
TargetMol Chemicals Inc. 總部位于馬薩諸塞州波士頓,致力于為全球生化領域科學家的研究提供專業(yè)的產品和服務。TargetMol?品牌的客戶群分布于40多個國家和地區(qū),已發(fā)展成為全球知名的化合物庫和小分子化合物研究供應商。 TargetMol?可提供160多種滿足不同需求的化合物庫,以及多種類型的生化試劑產品,包括12000多種抑制劑、16000多種天然產物和各類多肽、抗體、生命科學試劑盒等,此外,我們還建設有CADD(計算機輔助藥物設計)研究中心、藥理實驗室、藥化合成平臺三大技術中心,全方位滿足客戶的定制需求。 憑借我們優(yōu)質的產品和服務、快速高效的全球供應鏈和專業(yè)的技術支持,我們將有效幫助您縮短研發(fā)周期,取得更成功的結果。
成立日期
2013-04-18
(12年)
注冊資本
566.265100萬人民幣
員工人數
100-500人
年營業(yè)額
¥ 1億以上
主營行業(yè)
天然產物,生化試劑,分子生物學,分子砌塊,生物技術服務
經營模式
貿易,工廠,試劑,定制,服務
TargetMol中國(陶術生物)
VIP
3年
公司成立:
12年
注冊資本:
566.265100萬人民幣
企業(yè)類型:
有限責任公司(自然人投資或控股)
主營產品:
小分子抑制劑、藥物篩選化合物庫、藥物篩選等
公司地址:
靜安區(qū)江場三路238號8樓
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