吡咯咪唑|T1822|TargetMol

價(jià)格	詢價(jià)
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(chǎn)品詳情

中文名稱:吡咯咪唑	英文名稱:Clemizole
CAS:442-52-4	品牌: TargetMol
產(chǎn)地: 美國(guó)	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: 98.81%	產(chǎn)品類別: 抑制劑
貨號(hào): T1822

Product Introduction

Bioactivity

名稱	Clemizole
描述	Clemizole is an H1 histamine receptor antagonist, can inhibit NS4B's RNA binding and hepatitis C virus (HCV) replication.
細(xì)胞實(shí)驗(yàn)	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 能夠抑制 HCV RNA 在細(xì)胞培養(yǎng)中的復(fù)制，這一作用是通過(guò)其對(duì) NS4B RNA 結(jié)合活性的抑制實(shí)現(xiàn)的，對(duì)宿主細(xì)胞的毒性很小。Clemizole 對(duì) W55R 突變型 J6/JFH RNA 的半抑制濃度（EC50）約為 18 μM（是野生型 RNA EC50 的 2.25 倍）[1]。Clemizole 是 TRPC5 通道的新型抑制劑，能夠在低μM范圍內(nèi)有效阻斷 TRPC5 電流和 Ca2+ 入口（IC50=1.0-1.3 μM）。Clemizole 對(duì) TRPC5 的選擇性是對(duì)其最接近的結(jié)構(gòu)相似體 TRPC4β（IC50=6.4 μM）的六倍，對(duì) TRPC3（IC50=9.1 μM）和 TRPC6（IC50=11.3 μM）的選擇性幾乎為十倍。作為 TRPC5 的新型阻斷劑，Clemizole hydrochloride 的IC50 為 1.1 μM。濃度-反應(yīng)曲線確認(rèn) Clemizole 對(duì) TRPC5 的阻斷作用是濃度依賴性的，并顯示出明顯的 IC50 為 1.1±0.04 μM[2]。
體內(nèi)活性	Clemizole hydrochloride 在 C57BL/6J 小鼠體內(nèi)的血漿半衰期異常短（測(cè)定為0.15小時(shí)），并且非常迅速地轉(zhuǎn)化為一種葡萄糖醛酸苷代謝物（M14）和一個(gè)脫烷基化代謝物（M12），以及多種較小的代謝物[3]。
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 : 22.5 mg/mL (69.05 mM), Sonication is recommended.
關(guān)鍵字	Histamine Receptor \| TRP Channel \| Clemizole \| inhibit \| Hepatitis C virus \| Transient receptor potential channels \| HCV \| Inhibitor \| HCV Protease
相關(guān)產(chǎn)品	Famotidine \| Meclizine dihydrochloride \| Lidocaine \| Alginic acid \| Sodium butanoate \| Amitriptyline hydrochloride \| Trazodone hydrochloride \| Mianserin hydrochloride \| Artemisinin \| EIDD-1931 \| Methyl 2-amino-5-bromobenzoate \| Ribavirin
相關(guān)庫(kù)	抑制劑庫(kù) \| 抗癌活性化合物庫(kù) \| 經(jīng)典已知活性庫(kù) \| 已知活性化合物庫(kù) \| 離子通道庫(kù) \| 抗病毒庫(kù) \| GPCR靶點(diǎn)分子庫(kù) \| 免疫/炎癥分子化合物庫(kù) \| 膜蛋白靶向化合物庫(kù) \| 藥物功能重定位化合物庫(kù) \| 疼痛相關(guān)化合物庫(kù) \| 抗癌臨床化合物庫(kù)

關(guān)鍵字：克立咪唑|||吡咯咪唑|TargetMol

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TargetMol Chemicals Inc. 總部位于馬薩諸塞州波士頓，致力于為全球生化領(lǐng)域科學(xué)家的研究提供專業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶群分布于40多個(gè)國(guó)家和地區(qū)，已發(fā)展成為全球知名的化合物庫(kù)和小分子化合物研究供應(yīng)商。 TargetMol?可提供160多種滿足不同需求的化合物庫(kù)，以及多種類型的生化試劑產(chǎn)品，包括12000多種抑制劑、16000多種天然產(chǎn)物和各類多肽、抗體、生命科學(xué)試劑盒等，此外，我們還建設(shè)有CADD（計(jì)算機(jī)輔助藥物設(shè)計(jì)）研究中心、藥理實(shí)驗(yàn)室、藥化合成平臺(tái)三大技術(shù)中心，全方位滿足客戶的定制需求。憑借我們優(yōu)質(zhì)的產(chǎn)品和服務(wù)、快速高效的全球供應(yīng)鏈和專業(yè)的技術(shù)支持，我們將有效幫助您縮短研發(fā)周期，取得更成功的結(jié)果。

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