包裝規(guī)格:
250mg 1g 5g 10g 25g in glass bottle
產(chǎn)品簡介:
一種抗抑郁藥,為高效的五羥色胺再攝取抑制劑,能抑制 GRK2 活性,IC50?值為 14 μM。
溶解性:
DMSO:100 mg/mL?(266.78 mM;?超聲助溶)
儲備液保存:
-80°C, 6 months
-20°C, 1 month
(sealed storage, away from moisture)
體內(nèi)實(shí)驗(yàn):
1、請依序添加每種溶劑:?10%?DMSO→40%?PEG300→5%?Tween-80→45% Saline
Solubility: ≥ 5 mg/mL (13.34 mM); 澄清溶液
此方案可獲得?≥ 5 mg/mL(飽和度未知)的澄清溶液。
以?1 mL?工作液為例,取?100 μL 50.0 mg/mL?的澄清?DMSO?儲備液加到?400 μL?PEG300?中,混合均勻;再向上述體系中加入?50 μL?Tween-80,混合均勻;然后再繼續(xù)加入?450 μL?生理鹽水?定容至?1 mL。
2、請依序添加每種溶劑:?10%?DMSO→90% (20%?SBE-β-CD?in Saline)
Solubility: ≥ 5 mg/mL (13.34 mM); 澄清溶液
此方案可獲得?≥ 5 mg/mL(飽和度未知)的澄清溶液。
以?1 mL?工作液為例,取?100 μL 50.0 mg/mL?的澄清?DMSO?儲備液加到?900 μL?20% 的?SBE-β-CD?生理鹽水水溶液 中,混合均勻。
2 g SBE-β-CD(磺丁基醚 β-環(huán)糊精)粉末定容于 10 mL 的生理鹽水中,完全溶解至澄清透明。
3、請依序添加每種溶劑:?10%?DMSO→90%?Corn Oil
Solubility: ≥ 5 mg/mL (13.34 mM); 澄清溶液
此方案可獲得?≥ 5 mg/mL(飽和度未知)的澄清溶液,此方案實(shí)驗(yàn)周期在半個月以上的動物實(shí)驗(yàn)酌情使用。
以?1 mL?工作液為例,取?100 μL 50.0 mg/mL?的澄清?DMSO?儲備液加到?900 μL玉米油中,混合均勻。
注:工作液建議您現(xiàn)用現(xiàn)配,當(dāng)天使用。
<1mg/ml表示微溶或不溶。
普西唐提供的所有化合物濃度為內(nèi)部測試所得,實(shí)際溶液度可能與公布值有所偏差,屬于正常的批間細(xì)微差異現(xiàn)象。
請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
體外研究:
Paroxetine (1 μM and 10 μM) distinctly restrains T cell migration induced by?CX3CL1?through inhibiting GRK2. Paroxetine inhibits GRK2 induced activation of?ERK. Paroxetine (10 μM) reduces pro-inflammatory cytokines in LPS-stimulated BV2 cells. Paroxetine (0-5 μM) leads to a dose-dependent inhibition on LPS-induced production of TNF-α and IL-1β in BV2 cells. Paroxetine also inhibits lipopolysaccharide (LPS)-induced nitric oxide (NO) production and inducible nitric oxide synthase (iNOS) expression in BV2 cells. Paroxetine (5 μM) blocks LPS-induced?JNK?activation and attenuates baseline ERK1/2 activity in BV2 cells. Paroxetine relieves microglia-mediated neurotoxicity, and suppresses LPS-stimulated pro-inflammatory cytokines and NO in primary microglial cells.
體內(nèi)研究:
Paroxetine treatment obviously attenuates the symptoms of CIA rats. Paroxetine treatment clearly prevents the histological damage of joints and alleviates T cells infiltration into synovial tissue. Paroxetine reveals a strong effect on inhibiting?CX3CL1?production in synovial tissues. Paroxetine (20 mg/kg/day) reduces the myocyte cross-sectional area in rat and ROS formation in the remote myocardium. Paroxetine reduces the susceptibility to ventricular tachycardia. Paroxetine treatment following MI decreases LV remodeling and susceptibility to arrhythmias, probably by reducing ROS formation. In CCI paroxetine-treated group, paroxetine (10 mg/kg, i.p.) produces hyperalgesia at days 7 and 10 (P<0.01), but a decrease in pain behavior is seen at day 14. Moreover, paroxetine (10 mg/kg) significantly attenuates tactile hypersensitivity when compared to CCI vehicle-treated group.
注意事項(xiàng):
1、為了您的安全和健康,請穿實(shí)驗(yàn)服并戴一次性手套操作。
2、以上信息僅做參考交流之用。