| 中文名称: | PLX5622 | ||||
|---|---|---|---|---|---|
| 英文名称: | PLX5622 | ||||
| 别名: | 6-氟-N-((5-氟-2-甲氧基吡啶-3-基)甲基)-5-((5-甲基-1H-吡咯并[2,3-b]吡啶-3-基)甲基)吡啶 -2-胺 6-Fluoro-N-((5-fluoro-2-methoxypyridin-3-yl)methyl)-5-((5-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl)pyridin-2-amine | ||||
| CAS No: | 1303420-67-8 | 分子式: | 21H19F2N5O | 分子量: | 395.41 |
| CAS No: | 1303420-67-8 | ||||
| 分子式: | 21H19F2N5O | ||||
| 分子量: | 395.41 | ||||
| MDL: | MFCD32201039 | ||||
包装规格：
5mg 25mg 100mg in glass bottle
产品简介：
一种高度选择性的、能透过血脑屏障的、口服有效的 CSF1R 抑制剂 (IC50= 0.016 µM; Ki= 5.9 nM)，可用于病程发展前和过程中，扩大的和特异性的小胶质细胞的清除。PLX5622 具有较好的药理学特性。
溶解性：
溶于DMSO(50mg/ml)
储备液保存：
-80°C 6 months
-20°C 1 month
-20°C 1 month
体内实验：
1、请依序添加每种溶剂：5% DMSO→95% (0.5% Hypromellose→1% Tween-80) (Note: To make 100 mL diluent (0.5% Hypromellose→1% Tween-80), add 25 mL of 2% Hypromellose stock and 4 mL of 25% Tween-80 stock to 71 mL ddH2O)
Solubility: 6.5 mg/mL (16.44 mM); 悬浊液; 超声加热助溶
2、请依序添加每种溶剂：5% DMSO→95% (20% Ethoxylated hydrogenated castor oil in Saline)
Solubility: 5 mg/mL (12.65 mM); 澄清溶液; 超声助溶.
3、请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% Saline
Solubility: ≥ 3.12 mg/mL (7.89 mM); 澄清溶液
此方案可获得 ≥ 3.12 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 31.2 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。
4、请依序添加每种溶剂：10% DMSO→90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.32 mM); 澄清溶液
此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。
5、请依序添加每种溶剂：10% DMSO→90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.32 mM); 澄清溶液
此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
Solubility: 6.5 mg/mL (16.44 mM); 悬浊液; 超声加热助溶
2、请依序添加每种溶剂：5% DMSO→95% (20% Ethoxylated hydrogenated castor oil in Saline)
Solubility: 5 mg/mL (12.65 mM); 澄清溶液; 超声助溶.
3、请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% Saline
Solubility: ≥ 3.12 mg/mL (7.89 mM); 澄清溶液
此方案可获得 ≥ 3.12 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 31.2 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。
4、请依序添加每种溶剂：10% DMSO→90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.32 mM); 澄清溶液
此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。
5、请依序添加每种溶剂：10% DMSO→90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.32 mM); 澄清溶液
此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
靶点：
IC50: 0.016 µM (CSF1R); Ki: 5.9 nM (CSF1R)
体外研究：
PLX5622 (1-20 μM; 3 days) effectively depletes microglia without affecting oligodendrocytes or astrocytes in cerebellar slices. PLX5622 (4 μM; 3 days) causes a 30-40% reduction in NG2+ or PDGFRα+ cells, and this increased to 90-95% at 20 μM. No reduction of NG2+ or PDGFRα+ OPCs is observed in slices exposed to 1 μM or 2 μM PLX5622 despite robust (~95%) depletion of the microglial cells.
体内研究：
Pharmacodynamics of PLX5622 in preclinical studies
PLX5622 (1200 ppm; chow; for 3 weeks or 3 days; adult C57/Bl6 wild type mice) leads to around 80% of microglia lost after 3 days of treatment and a 99% microglia loss after 3 weeks of treatment. PLX5622 (adult C57/Bl6 wild type mice aged 3 months; diet for 3 weeks) decreases microglia in cortex, striatum, cerebellum and hippocampus.
PLX5622 (50 mg/kg; intraperitoneal injection; once (neonatal rat) or twice (adult rat) a day; for a total of 14 days) depletes microglia by 80-90% within 3 days of treatment, which increases to > 90% by 7 days. After 14 days of PLX5622 treatment, microglia is depleted by > 96% in both neonates and adults while preserving baseline astrocyte quantity. (A single daily injection of 0.65% PLX5622 suspended in 5% dimethyl sulfoxide and 20% Kolliphor RH40 in 0.01 M PBS is sufficient for neonatal microglia depletion, adult depletion requires injections twice daily).
PLX5622 (formulated in AIN-76A standard chow at 1200 mg/kg; for 28 days) leads to reduction in microglia throughout the CNS in 14-month-old 5xfAD mice.
Preparation of gavage dosing suspensions for PLX5622.
PLX5622 is dissolved in DMSO at a concentration that is 20x the final dosing solution. The compound stock is protected from light. A fresh stock is made each week.
The components of the diluent generally are prepared a day or more in advance because they take time to dissolve completely: a) 2% hydroxypropyl methyl cellulose (HPMC): 2.0 g powder was brought to 100 mL deionized water; b) 25% Polysorbate 80 (PS80): 25 g was brought to 100 mL deionized water. To make 100 mL diluent, add 25 mL of 2% HPMC stock (0.5% final) and 4 mL of 25% PS80 stock (1% final) to 71 mL deionized water to have final 100 mL. Final composition after mixing with compound: 0.5% HPMC, 1% PS80, 5% DMSO. On each dosing day, the compound stock is diluted 20-fold as follows: 19 volumes of diluent are measured into the tube, and 1 volume of the 20x compound/DMSO stock is added. The cap is closed and the content of the tube is mixed by inversion and placed in a sonicating water bath to make a uniform suspension.
PLX5622 (1200 ppm; chow; for 3 weeks or 3 days; adult C57/Bl6 wild type mice) leads to around 80% of microglia lost after 3 days of treatment and a 99% microglia loss after 3 weeks of treatment. PLX5622 (adult C57/Bl6 wild type mice aged 3 months; diet for 3 weeks) decreases microglia in cortex, striatum, cerebellum and hippocampus.
PLX5622 (50 mg/kg; intraperitoneal injection; once (neonatal rat) or twice (adult rat) a day; for a total of 14 days) depletes microglia by 80-90% within 3 days of treatment, which increases to > 90% by 7 days. After 14 days of PLX5622 treatment, microglia is depleted by > 96% in both neonates and adults while preserving baseline astrocyte quantity. (A single daily injection of 0.65% PLX5622 suspended in 5% dimethyl sulfoxide and 20% Kolliphor RH40 in 0.01 M PBS is sufficient for neonatal microglia depletion, adult depletion requires injections twice daily).
PLX5622 (formulated in AIN-76A standard chow at 1200 mg/kg; for 28 days) leads to reduction in microglia throughout the CNS in 14-month-old 5xfAD mice.
Preparation of gavage dosing suspensions for PLX5622.
PLX5622 is dissolved in DMSO at a concentration that is 20x the final dosing solution. The compound stock is protected from light. A fresh stock is made each week.
The components of the diluent generally are prepared a day or more in advance because they take time to dissolve completely: a) 2% hydroxypropyl methyl cellulose (HPMC): 2.0 g powder was brought to 100 mL deionized water; b) 25% Polysorbate 80 (PS80): 25 g was brought to 100 mL deionized water. To make 100 mL diluent, add 25 mL of 2% HPMC stock (0.5% final) and 4 mL of 25% PS80 stock (1% final) to 71 mL deionized water to have final 100 mL. Final composition after mixing with compound: 0.5% HPMC, 1% PS80, 5% DMSO. On each dosing day, the compound stock is diluted 20-fold as follows: 19 volumes of diluent are measured into the tube, and 1 volume of the 20x compound/DMSO stock is added. The cap is closed and the content of the tube is mixed by inversion and placed in a sonicating water bath to make a uniform suspension.
保存条件：
-20° C
注意事项：
1、为了您的安全和健康，请穿实验服并戴一次性手套操作。
2、以上信息仅做参考交流之用。
2、以上信息仅做参考交流之用。
UN码：
HazardClass：
危害声明：
安全说明：
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参考文献 & 客户发表文献
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
