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- 详细信息
- 文献和实验
- 技术资料
- 库存：
60
- 英文名：
Pardoprunox hydrochloride (SLV-308 hydrochloride)
- CAS号：
269718-83-4
- 供应商：
上海莼试
- 保存条件：
Store at -20°C
- 规格：
2mg 5mg 10mg 50mg 100mg
本产品仅供科学实验研究使用! 不能用于临床或动物诊断！
化学性质:
Pardoprunox hydrochloride (SLV-308 hydrochloride)规格：2mg 5mg 10mg 50mg 100mg
CAS：269718-83-4
别名：N/A
化学名：N/A
分子式：C12H16ClN3O2
分子量：269.73
溶解度：DMF: 1 mg/ml,DMSO: 5 mg/ml,Ethanol: 0.1 mg/ml,PBS (pH 7.2): 5 mg/ml
储存条件：Store at -20°C
General tips：For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition: Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述:
Pardoprunox hydrochloride is a novel partial dopamine D2 and D3 receptor agonist and serotonin 5-HT1A receptor agonist, D2 (pKi = 8.1) and D3 receptor (pKi = 8.6) partial agonist and 5-HT1A receptor (pKi = 8.5) full agonist.IC50 value: 8.1/8.6/8.5 (pKi, for D2/ D3/5-HT1A receptor)Target: dopamine D2 and D3 receptor, 5-HT1A receptorin vitro: Pardoprunox also binds to D4 (pKi = 7.8), α1-adrenergic (pKi = 7.8), α2-adrenergic (pKi = 7.4), and 5-HT7 receptors (pKi = 7.2) with lower affinity. Pardoprunox acts as a potent but partial D(2) receptor agonist (pEC50 = 8.0 and pA2 = 8.4) with an efficacy of 50% on forskolin stimulated cAMP accumulation. At human recombinant dopamine D3 receptors, Pardoprunox acts as a partial agonist in the induction of [35S]GTPgammaS binding (intrinsic activity of 67%; pEC(50) = 9.2) and antagonized the dopamine induction of [35S]GTPgammaS binding (pA2 = 9.0). Pardoprunox acts as a full 5-HT1A receptor agonist on forskolin induced cAMP accumulation at cloned human 5-HT1A receptors but with low potency (pEC50 = 6.3) [1].in vivo: Pardoprunox induces contralateral turning behaviour in rats with unilateral 6-hydroxydopamine-induced lesions of the substantia nigra pars compacta (SNpc) (MED=0.03mg/kg; po). In MPTP-treated common marmosets, Pardoprunox dose-dependently increases locomotor activity (MED=0.03mg/kg; po) and decreases motor disability (MED=0.03mg/kg; po). In contrast Pardoprunox attenuated novelty-induced locomotor activity (MED=0.01mg/kg; po), (+)-amphetamine-induced hyperlocomotion (MED=0.3mg/kg; po) and apomorphiinduced climbing (MED=0.6mg/kg; po) in rodents. Pardoprunox also induces 5-HT1A receptor-mediated behaviours, including flat body posture and lower lip retraction (MED=0.3mg/kg; po). Collectively, these findings demonstrate that Pardoprunox possesses dopamine D2/3 partial agonist effects, 5-HT1A agonist effects and reduces parkinsonism in animal models. functional D2 receptor partial agonist activity and is effective in experimental models predictive of efficacy in PD.[2][1]. Glennon JC, et al. In vitro characterization of SLV308 (7-[4-methyl-1-piperazinyl]-2(3H)-benzoxazolone, monohydrochloride): a novel partial dopamine D2 and D3 receptor agonist and serotonin 5-HT1A receptor agonist. Synapse. 2006 Dec 15;60(8):599-608. [2]. Jones CA, et al. An in vivo pharmacological evaluation of pardoprunox (SLV308)--a novel combined dopamine D(2)/D(3) receptor partial agonist and 5-HT(1A) receptor agonist with efficacy in experimental models of Parkinson's disease. Eur Neuropsychopharmaco
使用方法:
1. 常用筛选浓度
注意：用来筛选稳转株的工作浓度需要根据细胞类型，培养基，生长条件和细胞代谢率而变化，推荐使用浓度为50-1000μg/mL。对于第一次使用的实验体系建议通过建立杀灭曲线(kill curve)，即剂量反应性曲线，来确定最佳筛选浓度。
一般而言，哺乳动物细胞50-500μg/mL;细菌/植物细胞20-200μg/mL;真菌300-1000μg/mL。
2. 杀灭曲线的建立
注意：为了筛选得到稳定表达目的蛋白的细胞株，需要确定能够杀死未转染宿主细胞的抗生素浓度，可通过建立杀灭曲线(剂量反应曲线)来实现，至少选择5个浓度。
1) 第一天：未转化的细胞按照20-25%的细胞密度铺在合适的培养板上，37℃，CO2培养过夜;注：对于需要更高密度来检测活力的细胞，可增加接种量。
2) 根据细胞类型，设定合适范围内的浓度梯度。以哺乳动物细胞为例，可设定50，100，250，500，750，1000μg/mL。先用去离子水或者PBS buffer按照1:10的比例将母液稀释到5 mg/ml，然后按照下表稀释到相应浓度的工作液。
3) 第二天：替换旧的培养基，换用新鲜配制的含有相应浓度药物的培养基。每个浓度做三个平行孔。
4) 接下来每3-4天更换新的含药物培养基。
5) 按照固定的周期(如每2天)进行活细胞计数来确定阻止未转染细胞生长的恰当浓度。选择在理想的天数(通常是7-10天)内能够杀死绝大多数细胞的浓度为稳定转染细胞筛选用的工作浓度。
3. 稳定转染细胞的筛选
1) 转染48h后，用含有适当浓度的潮霉素B筛选培养基来传代细胞(直接传代或者稀释后传代)。
注意：细胞处于活跃分裂状态时抗生素的杀伤。则当细胞过于稠密，其效率会降低。为了得到较好的筛选效果，最好将细胞稀释至丰度不超过25%
2) 每隔3-4天更换含有药物的筛选培养液。
3) 筛选7天后观察并评估细胞克隆(集落)的形成情况。集落的形成可能还需要一周或者更多的时间，这取决于宿主细胞类型，转染，以及筛选效果。
4) 挑取并转移5-10个抗性克隆于35mm细胞培养板，继续用含药物的筛选培养液维持培养7天。
5) 之后更换正常培养基培养即可。
公司正在出售的产品:
蛋白酶抑制剂混合物实验步骤:
(1)实验开始前将RNA提取液于65℃水浴锅中预热,离心管中加入ME(巯基乙醇),(10mL加80ul,50mL中加入300ul)
(2)取约0.8g菌丝体(液体培养获得的菌丝用真空抽滤即可！固体培养就更好说了),在液氮中迅速磨成精细粉末,装入50mL离心管,按1g材料8mL的量加入预热的RNA提取液,颠倒混匀
(3)65℃水浴3-10 min,期间混匀2-3次
(4)加入等体积的酚(注意是酸酚pH4.5)::yi戊醇(25:24:1)抽提(10,000rpm,4℃,5 min)
(5)取上清,等体积的yi戊醇(24:1)抽提(10,000rpm,4℃,5 min)
(6)加入1/4V体积10M LiCl溶液,4℃放置6h以上(或过夜)
(7)10,000rpm,4℃离心20min
(8)弃上清,用500ul SSTE溶解沉淀
(9)酚::yi戊醇(25:24:1)抽提两次,:yi戊醇(24:1)抽提1次(10,000rpm,4℃,5min)
(10)加2V体积的无水乙醇,在-70℃冰箱沉淀30min以上
(11)12,000rpm,4℃离心20 min
(12)弃上清.沉淀用70%酒精漂洗一次,干燥
(13)加200ul的DEPC处理水溶解
(14)用非变性琼脂糖凝胶电泳和紫外分光光度计扫描检测RNA的质量(在抽提过程中,若蛋白质含量或其它的杂质还较多,可以增加抽提次数)
| 产品名称 | Pardoprunox hydrochloride (SLV-308 hydrochloride) | 产品货号 | CS-01Y76609 |
| 规格 | 2mg 5mg 10mg 50mg 100mg | CAS号 | 269718-83-4 |
| 含量 | >98.00% | 分子式 | C12H16ClN3O2 |
| 分子量 | 269.73 | 用途 | 仅供科研研究使用 |
Pardoprunox hydrochloride (SLV-308 hydrochloride)规格：2mg 5mg 10mg 50mg 100mg
CAS：269718-83-4
别名：N/A
化学名：N/A
分子式：C12H16ClN3O2
分子量：269.73
溶解度：DMF: 1 mg/ml,DMSO: 5 mg/ml,Ethanol: 0.1 mg/ml,PBS (pH 7.2): 5 mg/ml
储存条件：Store at -20°C
General tips：For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition: Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述:
Pardoprunox hydrochloride is a novel partial dopamine D2 and D3 receptor agonist and serotonin 5-HT1A receptor agonist, D2 (pKi = 8.1) and D3 receptor (pKi = 8.6) partial agonist and 5-HT1A receptor (pKi = 8.5) full agonist.IC50 value: 8.1/8.6/8.5 (pKi, for D2/ D3/5-HT1A receptor)Target: dopamine D2 and D3 receptor, 5-HT1A receptorin vitro: Pardoprunox also binds to D4 (pKi = 7.8), α1-adrenergic (pKi = 7.8), α2-adrenergic (pKi = 7.4), and 5-HT7 receptors (pKi = 7.2) with lower affinity. Pardoprunox acts as a potent but partial D(2) receptor agonist (pEC50 = 8.0 and pA2 = 8.4) with an efficacy of 50% on forskolin stimulated cAMP accumulation. At human recombinant dopamine D3 receptors, Pardoprunox acts as a partial agonist in the induction of [35S]GTPgammaS binding (intrinsic activity of 67%; pEC(50) = 9.2) and antagonized the dopamine induction of [35S]GTPgammaS binding (pA2 = 9.0). Pardoprunox acts as a full 5-HT1A receptor agonist on forskolin induced cAMP accumulation at cloned human 5-HT1A receptors but with low potency (pEC50 = 6.3) [1].in vivo: Pardoprunox induces contralateral turning behaviour in rats with unilateral 6-hydroxydopamine-induced lesions of the substantia nigra pars compacta (SNpc) (MED=0.03mg/kg; po). In MPTP-treated common marmosets, Pardoprunox dose-dependently increases locomotor activity (MED=0.03mg/kg; po) and decreases motor disability (MED=0.03mg/kg; po). In contrast Pardoprunox attenuated novelty-induced locomotor activity (MED=0.01mg/kg; po), (+)-amphetamine-induced hyperlocomotion (MED=0.3mg/kg; po) and apomorphiinduced climbing (MED=0.6mg/kg; po) in rodents. Pardoprunox also induces 5-HT1A receptor-mediated behaviours, including flat body posture and lower lip retraction (MED=0.3mg/kg; po). Collectively, these findings demonstrate that Pardoprunox possesses dopamine D2/3 partial agonist effects, 5-HT1A agonist effects and reduces parkinsonism in animal models. functional D2 receptor partial agonist activity and is effective in experimental models predictive of efficacy in PD.[2][1]. Glennon JC, et al. In vitro characterization of SLV308 (7-[4-methyl-1-piperazinyl]-2(3H)-benzoxazolone, monohydrochloride): a novel partial dopamine D2 and D3 receptor agonist and serotonin 5-HT1A receptor agonist. Synapse. 2006 Dec 15;60(8):599-608. [2]. Jones CA, et al. An in vivo pharmacological evaluation of pardoprunox (SLV308)--a novel combined dopamine D(2)/D(3) receptor partial agonist and 5-HT(1A) receptor agonist with efficacy in experimental models of Parkinson's disease. Eur Neuropsychopharmaco
使用方法:
1. 常用筛选浓度
注意：用来筛选稳转株的工作浓度需要根据细胞类型，培养基，生长条件和细胞代谢率而变化，推荐使用浓度为50-1000μg/mL。对于第一次使用的实验体系建议通过建立杀灭曲线(kill curve)，即剂量反应性曲线，来确定最佳筛选浓度。
一般而言，哺乳动物细胞50-500μg/mL;细菌/植物细胞20-200μg/mL;真菌300-1000μg/mL。
2. 杀灭曲线的建立
注意：为了筛选得到稳定表达目的蛋白的细胞株，需要确定能够杀死未转染宿主细胞的抗生素浓度，可通过建立杀灭曲线(剂量反应曲线)来实现，至少选择5个浓度。
1) 第一天：未转化的细胞按照20-25%的细胞密度铺在合适的培养板上，37℃，CO2培养过夜;注：对于需要更高密度来检测活力的细胞，可增加接种量。
2) 根据细胞类型，设定合适范围内的浓度梯度。以哺乳动物细胞为例，可设定50，100，250，500，750，1000μg/mL。先用去离子水或者PBS buffer按照1:10的比例将母液稀释到5 mg/ml，然后按照下表稀释到相应浓度的工作液。
3) 第二天：替换旧的培养基，换用新鲜配制的含有相应浓度药物的培养基。每个浓度做三个平行孔。
4) 接下来每3-4天更换新的含药物培养基。
5) 按照固定的周期(如每2天)进行活细胞计数来确定阻止未转染细胞生长的恰当浓度。选择在理想的天数(通常是7-10天)内能够杀死绝大多数细胞的浓度为稳定转染细胞筛选用的工作浓度。
3. 稳定转染细胞的筛选
1) 转染48h后，用含有适当浓度的潮霉素B筛选培养基来传代细胞(直接传代或者稀释后传代)。
注意：细胞处于活跃分裂状态时抗生素的杀伤。则当细胞过于稠密，其效率会降低。为了得到较好的筛选效果，最好将细胞稀释至丰度不超过25%
2) 每隔3-4天更换含有药物的筛选培养液。
3) 筛选7天后观察并评估细胞克隆(集落)的形成情况。集落的形成可能还需要一周或者更多的时间，这取决于宿主细胞类型，转染，以及筛选效果。
4) 挑取并转移5-10个抗性克隆于35mm细胞培养板，继续用含药物的筛选培养液维持培养7天。
5) 之后更换正常培养基培养即可。
公司正在出售的产品:
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| Drospirenone | 类粘蛋白2(ORM2)检测试剂盒 |
| Glutaurine | MAX二聚化蛋白1(mxd1)试剂盒 ELISA |
| JTC-801 | 可溶性半乳糖苷结合凝集素3(Lgals3)ELISA Kit |
| Tazarotenic Acid | 水闸蛋白14(CLDN14)ELISA检测试剂盒 |
| BMS 753 | 主要穹窿蛋白(MVP)检测试剂盒 |
| Budesonide-d8 | 泛素蛋白D(UBD)试剂盒 ELISA |
| Gestodene | Caspase 12, Casp-12 Elisa Kit |
| Toremifene | 类似60S核糖蛋白L21(LOC382344)ELISA Kit |
| (-)-Viriditoxin | 小乳腺表皮粘蛋白(SBEM)ELISA检测试剂盒 |
| (R)-(-)-Mellein | 桩蛋白(Pax)试剂盒 ELISA |
| Deferasirox-d4 | 磷酸化核因子κB抑制蛋白α(pIKBα)检测试剂盒 |
| Ethynodiol diacetate | Pardoprunox hydrochloride (SLV-308 hydrochloride)羰基化蛋白(PC)ELISA Kit |
| S-NEPC | 切除修复交叉互补基因1(ERCC1)ELISA检测试剂盒 |
| 受磷蛋白(PLN)ELISA Kit | IPO-38蛋白(IPO38) 试剂盒 ELISA |
蛋白酶抑制剂混合物实验步骤:
(1)实验开始前将RNA提取液于65℃水浴锅中预热,离心管中加入ME(巯基乙醇),(10mL加80ul,50mL中加入300ul)
(2)取约0.8g菌丝体(液体培养获得的菌丝用真空抽滤即可！固体培养就更好说了),在液氮中迅速磨成精细粉末,装入50mL离心管,按1g材料8mL的量加入预热的RNA提取液,颠倒混匀
(3)65℃水浴3-10 min,期间混匀2-3次
(4)加入等体积的酚(注意是酸酚pH4.5)::yi戊醇(25:24:1)抽提(10,000rpm,4℃,5 min)
(5)取上清,等体积的yi戊醇(24:1)抽提(10,000rpm,4℃,5 min)
(6)加入1/4V体积10M LiCl溶液,4℃放置6h以上(或过夜)
(7)10,000rpm,4℃离心20min
(8)弃上清,用500ul SSTE溶解沉淀
(9)酚::yi戊醇(25:24:1)抽提两次,:yi戊醇(24:1)抽提1次(10,000rpm,4℃,5min)
(10)加2V体积的无水乙醇,在-70℃冰箱沉淀30min以上
(11)12,000rpm,4℃离心20 min
(12)弃上清.沉淀用70%酒精漂洗一次,干燥
(13)加200ul的DEPC处理水溶解
(14)用非变性琼脂糖凝胶电泳和紫外分光光度计扫描检测RNA的质量(在抽提过程中,若蛋白质含量或其它的杂质还较多,可以增加抽提次数)
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文献和实验相关实验
Guanidine Hydrochloride Purification of Proteins From SDS
Pepstatin A (2.0 mg/ml)10 ml Leupeptin (1.0 mg/ml)10 ml Aprotinin (5.0 mg/ml)(Protease Inhibitor Cocktail Sigma #P8340)Denaturation Buffer6 M guanidine hydrochloride 57.3 g G-HCl20 mM Hepes 7.9 2 ml 1M Hepes pH 7.910 mM KCl 0.074 g KCl0.5 mM DTT 100 ml 0.5 M
Guanidine Hydrochloride Purification of Proteins From SDS PAGE
(Sigma #P7626) 10 ml Pepstatin A (2.0 mg/ml) 10 ml Leupeptin (1.0 mg/ml) 10 ml Aprotinin (5.0 mg/ml) (Protease Inhibitor Cocktail Sigma #P8340) Denaturation Buffer 6 M guanidine hydrochloride 57.3 g G-HCl 20 mM Hepes 7.9 2 ml 1M Hepes pH 7.9 10 mM
Packed column subcritical and/or supercritical fluid chromatography (p-sub or pSFC) has been used as a powerful chiral separation technique, whereby a mobile phase produces low viscosity, a high diffusion coefficient, and a solvating power. P
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Pardoprunox hydrochloride (SLV-308 hydrochloride)
￥600 - 3200
