價(jià)格 | ¥195 | ¥518 | ¥828 |
包裝 | 1mg | 5mg | 10mg |
最小起訂量 | 1mg |
發(fā)貨地 | 上海 |
更新日期 | 2024-09-29 |
中文名稱:化合物 BMS626529 | 英文名稱:Temsavir |
CAS:701213-36-7 | 品牌: TargetMol |
產(chǎn)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: 98.06% | 產(chǎn)品類別: 抑制劑 |
貨號(hào): T4665 |
名稱 | Temsavir |
描述 | Temsavir (BMS626529) is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4+ T cells. |
細(xì)胞實(shí)驗(yàn) | Cytotoxicity assays are performed in the presence of serially diluted BMS-626529 for up to 6 days, and cell viability is quantitated using an XTT assay. To determine CC50?values (concentration of drug required to kill 50% of cells), laboratory-adapted peripheral blood mononuclear cells (PBMCs) are initially plated at a density of 0.1×106?cells/mL. In the absence of compounds, the cell densities typically reach 1×106?to 1.2×106/mL after 6 days[1]. |
激酶實(shí)驗(yàn) | Micro BioSpin 6 columns are used to measure the binding of [3H]BMS-488043 or [3H]BMS-626529 to gp120. Binding solutions (30 μL) containing 25 mM Tris-HCl (pH 7.5), 125 mM NaCl, 50 nM gp120JRFL, and serial dilutions of [3H]BMS-488043 or [3H]BMS-626529 are allowed to equilibrate and then adsorbed to a MicroBioSpin 6 column. The column is centrifuged (~14,000 rpm) for 5 min, the eluent is collected, and radioactivity is determined with a scintillation counter. To measure dissociative kinetics, 150 nM [3H]BMS-626529 or 90 nM [3H]BMS-488043 is incubated with 60 nM gp120 at ambient temperature for 1 h to achieve equilibrium binding, and then a large molar excess (14-fold) of soluble CD4 protein is added to drive dissociation. Aliquots are taken at the indicated time intervals, adsorbed to a spin column, and centrifuged, and the radioactivity in the eluent is quantitated. Comparison of the tritium signal from parallel samples with and without the soluble CD4 challenge allowed for the determination of the percent compound bound[1]. |
體外活性 | Temsavir的半最大有效濃度(EC50)值對(duì)絕大多數(shù)病毒分離物均<10 nM。針對(duì)LAI病毒,Temsavir展現(xiàn)出平均EC50值為0.7±0.4 nM。對(duì)于最敏感的病毒,Temsavir的EC50為0.01 nM,而對(duì)于最不敏感的病毒,其EC50值>2,000 nM。在不同人體組織的幾種細(xì)胞類型中檢查了Temsavir的細(xì)胞毒性概況。在培養(yǎng)3或6天后,觀察到MT-2(T淋巴細(xì)胞)、HEK293(腎)、HEp-2(喉)、HepG2(肝)、HeLa(宮頸)、HCT116(結(jié)直腸)、MCF-7(乳腺)、SK-N-MC(神經(jīng)上皮)、HOS(骨)、H292(肺)和MDBK(牛腎)細(xì)胞中的CC50值>200 μM。在6天的培養(yǎng)后,T細(xì)胞系PM1和PBMCs分別獲得105和192 μM的CC50值。這些結(jié)果表明Temsavir在細(xì)胞培養(yǎng)中表現(xiàn)出低細(xì)胞毒性。Temsavir針對(duì)一系列臨床分離物展現(xiàn)出廣譜的抗病毒活性,50%抑制濃度(IC50)范圍從亞nM級(jí)別到>0.1 μM。 |
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 : 8.57 mg/mL (18.1 mM), Sonication is recommended. |
關(guān)鍵字 | inhibit | BMS 626529 | Human immunodeficiency virus | BMS-626529 | Temsavir | Inhibitor | HIV |
相關(guān)產(chǎn)品 | Tenofovir | Chloroquine phosphate | Emtricitabine | Dolutegravir intermediate-1 | Inosine pranobex | Hydroxyurea | Lamivudine | 5-Fluorouracil | Decanedioic acid | Stavudine | Dextran sulfate sodium salt (MW 4500-5500) | Kaempferol |
相關(guān)庫 | 抑制劑庫 | 經(jīng)典已知活性庫 | 已知活性化合物庫 | 抗感染化合物庫 | 抗COVID-19化合物庫 | NO PAINS 化合物庫 | 抗病毒庫 | 臨床期小分子藥物庫 | 藥物功能重定位化合物庫 | 人代謝物化合物庫 |
成立日期 | 2013-04-18 (12年) | 注冊(cè)資本 | 566.265100萬人民幣 |
員工人數(shù) | 100-500人 | 年?duì)I業(yè)額 | ¥ 1億以上 |
主營行業(yè) | 天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù) | 經(jīng)營模式 | 貿(mào)易,工廠,試劑,定制,服務(wù) |
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