PRX-07034 hydrochloride 是一种有效的高度选择性5-HT6受体拮抗剂，Ki为 4-8 nM，IC50为 19 nM。PRX-07034 可用于增强工作记忆和认知灵活性的研究。
| 生物活性 | PRX-07034 hydrochloride is a highly selective and potent5-HT6 receptorantagonist with aKi= 4-8 nM and anIC50of 19 nM. PRX-07034 can be used for the research of enhancing working memory and cognitive flexibility[1]. |
| IC50& Target[1] | 5-HT6Receptor 4-8 nM (Ki) | 5-HT6Receptor 19 nM (IC50) | 5-HT1AReceptor 420 nM (Ki) | 5-HT1BReceptor 260 nM (Ki) | 5-HT1DReceptor 2.8 μM (Ki) | 5-HT2AReceptor 2.5 μM (IC50) | 5-HT2BReceptor 2.5 μM (IC50) | 5-HT2CReceptor 3.7 μM (IC50) | Dopamine D3 Receptor 71 nM (Ki) | Histamine H2 Receptor 0.64 μM (Ki) | Opioid μ Receptor 0.45 μM (Ki) |
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体外研究
(In Vitro) | PRX-07034 is both a potent and highly selective 5-HT6 receptor antagonist (≥100-fold selectivity for the 5-HT6 receptor compared to 68 other GPCRs, ion channels, and transporters. PRX-07034 inhibits 5-HT1A, 5-HT1B, 5-HT1D, Dopamine D3, Histamine H2, and Opioid μ receptor with Kis of 420 nM, 260 nM, 2.8 μM, 71 nM, 0.64 μM, and 0.45 μM, respectively. PRX-07034 inhibits 5-HT2A, 5-HT2B, and 5-HT2C receptors with IC50s of 2.5 μM, 2.5 μM, and 3.7 μM, respectively[1].
In functional assays, PRX-07034 demonstrates low antagonist activity for the dopamine D3 receptor (IC50=4.8 μM) and very low agonistic activity for the opioid μ-receptor (EC50=19 μM)[1].
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体内研究
(In Vivo) | PRX-07034 (0.1, 1, or 3 mg/kg; i.p.; 30 min prior to delayed spontaneous alternation testing) selectively enhances a switch to a place discrimination[1].
| Animal Model: | Male Long-Evans rats weighing approximately 350 g[1] | | Dosage: | 0.1, 1, or 3 mg/kg | | Administration: | Injected intraperitoneal | | Result: | 1 and 3 mg/kg (but not 0.1 mg/kg) significantly enhanced delayed spontaneous alternation. The drug at 1 and 3 mg/kg also enhanced switching between a place and response strategy, but did not affect initial learning of either a place or response discrimination. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | -20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 31.25 mg/mL(63.72 mM;ultrasonic and warming and heat to 60℃) H2O : 4.76 mg/mL(9.71 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.0390 mL | 10.1949 mL | 20.3899 mL | | 5 mM | 0.4078 mL | 2.0390 mL | 4.0780 mL | | 10 mM | 0.2039 mL | 1.0195 mL | 2.0390 mL |
*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。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (4.24 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.24 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (4.24 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.24 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (4.24 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.24 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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