PRX-07034 hydrochloride|cas:903580-39-2|西域试剂

PRX-07034 hydrochloride,98.09%

产品编号：Bellancom-14559| CAS NO：903580-39-2| 分子式：C₂₁H₂₉Cl₂N₃O₄S| 分子量：490.44

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-14559	￥800.00	杭州北京（现货）
Bellancom-14559	￥1300.00	杭州北京（现货）
Bellancom-14559	￥2500.00	杭州北京（现货）
Bellancom-14559	￥4000.00	杭州北京（现货）
Bellancom-14559	￥6500.00	杭州北京（现货）

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PRX-07034 hydrochloride

产品介绍

PRX-07034 hydrochloride 是一种有效的高度选择性 5-HT6 受体拮抗剂，K_i 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 potent 5-HT6 receptor antagonist with a K_i= 4-8 nM and an IC₅₀ of 19 nM. PRX-07034 can be used for the research of enhancing working memory and cognitive flexibility.

体外研究

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 K_is 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.
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) .

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Long-Evans rats weighing approximately 350 g
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.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Long-Evans rats weighing approximately 350 g
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 31.25 mg/mL (63.72 mM; ultrasonic and warming and heat to 60°C)

H₂O : 4.76 mg/mL (9.71 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
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。