| 名稱 | Doxazosin mesylate |
| 描述 | Doxazosin mesylate (UK 33274 mesylate)(UK 33274) is a quinazoline-derivative. It is a selectively antagonizes postsynaptic α1-adrenergic receptors. |
| 激酶實(shí)驗(yàn) | Protease assays: To determine the inhibition constants (Ki) for each Prt inhibitor, purified HIV-1 RF wild-type Prt (2.5 nM) is incubated at 37 ℃ with 1 μM to 15 μM fluorogenic substrate in reaction buffer (1 M NaCl, 1 mM EDTA, 0.1 M sodium acetate [pH 5.5], 0.1% polyethylene glycol 8000) in the presence or absence of Atazanavir. Cleavage of the substrate is quantified by measuring an increase in fluorescent emission at 490 nM after excitation at 340 nM using a Cytofluor 4000. Reactions are carried out using 1.36 μM, 1.66 μM, 2.1 μM, 3.0 μM, 5.0 μM, or 15 μM substrate in the presence of five concentrations of Atazanavir (1.25 nM to 25 nM). Substrate cleavage is monitored at 5-min intervals for 30 min. Cleavage rates are then determined for each sample at early time points in the reaction, and Ki values are determined from the slopes of the resulting Michaelis-Menten plots. |
| 體外活性 | Doxazosin降低平均動(dòng)脈壓為18％,但不會(huì)影響所有倉鼠的心臟速率.Doxazosin顯著降低Beta TGF-β1感染小鼠前列腺重建（MPR）的濕重. |
| 體內(nèi)活性 | Doxazosin和消膽胺類似地降低血漿總膽固醇,LDL加VLDL膽固醇和平均總甘油三酯分別達(dá)46％,61％和45％。Doxazosin減少乳鼠心肌細(xì)胞原代培養(yǎng)細(xì)胞的活力,Hoechst染色活體染色表明Doxazosin誘導(dǎo)人成心肌細(xì)胞的凋亡。Doxazosin 在HL-1細(xì)胞系中,誘導(dǎo)DNA損傷和細(xì)胞死亡。Doxazosin誘導(dǎo)細(xì)胞凋亡是由特定的胱天蛋白酶-8抑制劑阻斷,caspase-8功能性參與Doxazosi誘導(dǎo)的細(xì)胞凋亡。 Doxazosin拮抗HUVEC細(xì)胞的VEGF介導(dǎo)的血管生成響應(yīng),通過廢除細(xì)胞粘附到纖連蛋白和膠原包被的表面,并抑制細(xì)胞遷移,通過血管內(nèi)皮生長因子的表達(dá)的下調(diào)。Doxazosin增加FADD招募和caspase-8激活,暗示Fas介導(dǎo)細(xì)胞凋亡,作為Doxazosin在前列腺細(xì)胞中作用的基本機(jī)制。 |
| 存儲(chǔ)條件 | Keep away from moisture,
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 8.33 mg/mL (15.21 mM), Solution.
10% DMSO+90% Saline : < 8.33 mg/mL (15.21 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
DMSO : 83.33 mg/mL (152.18 mM), Sonication is recommended.
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| 關(guān)鍵字 | α1-adrenergic receptor | UK-33274 Mesylate | UK33274 Mesylate | UK-33274 | UK33274 | UK 33274 Mesylate | UK 33274 | Mitophagy | Mitochondrial Autophagy | Inhibitor | inhibit | Doxazosin mesylate | Doxazosin | Beta Receptor | Autophagy | AdrenergicReceptor | Adrenergic Receptor |
| 相關(guān)產(chǎn)品 | Guanidine hydrochloride | Naringin | Enzalutamide | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Hemin | Hydroxychloroquine | Sildenafil citrate | Stavudine | Tamoxifen | Paeonol |
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