Hypidone hydrochloride - CAS:1339058-04-6

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Hypidone hydrochloride (Synonyms:YL0919)

目录号 : KM4840 CAS No. : 1339058-04-6 纯度 : 98%

Data Sheet 产品使用指南

Hypidone hydrochloride (YL0919) 是一种口服活性抗抑郁剂，具有双重活性，是一种高选择性的 5-HT uptake 阻滞剂和有效的 5-HT_1A receptor 激动剂 (K_i=0.19 nM)。Hypidone hydrochloride 对大鼠大脑皮层突触体和 HEK293 细胞摄取 [³H]-5-HT 有抑制作用，IC₅₀s 分别为 1.78 nM 和 1.93 nM。Hypidone hydrochloride 在动物模型中表现出明显的抗抑郁作用，对抑郁症的研究具有重要意义。

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生物活性

Hypidone hydrochloride (YL0919) is an orally active antidepressant agent with dual activity as a highly seletive 5-HT uptake blocker and an effective 5-HT_1A receptor agonist (K_i=0.19 nM). Hypidone hydrochloride inhibits the uptake of [H]-5-HT into rat cerebral cortical synaptosomes and HEK293 cells with IC₅₀s of 1.78 nM and 1.93 nM, respectively. Hypidone hydrochloride shows remarkable antidepressant effects in animal models and has the poential for the investigation of depressive disorder.

体外研究

Hypidone hydrochloride inhibits the uptake of [H]-5-HT into rat cerebral cortical synaptosomes and HEK293 cells stably expressing hSERT with IC₅₀ values of 1.78 nM and 1.93,respectively.
Hypidone hydrochloride (0.01 nM-10 μM) concentration-dependently inhibits forskolin-stimulated cAMP formation, exerts a concentration-dependent inhibitory effect on cAMP formation with an IC₅₀ of approximately 23.9 nM. And in antagonism studies, WAY-100635 prevents Hypidone hydrochloride-mediated inhibition of forskolin-stimulated cAMP formation.
Hypidone hydrochloride shows affinities to rat 5-HT1A receptors, SERTs, NETs, and DATs, it binds to 5-HT1A receptor, serotonin transporter (SERT) with high affinity (K_i=0.19 and 0.72 nM, respectively), but its affinity to NET and DAT are low, blocking [H]nisoxetine and [H]win35428 binding with Ki values of 650 nM and 2652 nM respectively.

体内研究

Hypidone hydrochloride (YL0919) (oral administration; 1.25 or 5 mg/kg; 4 weeks) and fluoxetine (10 mg/kg) reverses the inhibition of locomotor activity in CUS rats.
Hypidone hydrochloride (oral administration; 1.25, 2.5, and 5 mg/kg; 4 weeks) significantly reduces the immobility time in TST in mcie FST in mice. Besides, Hypidone hydrochloride displays no effect on the locomotor activity in a separate OFT. Furthermore, the antidepressant-like effect of Hypidone hydrochloride in TST and FST is completely bunted by coadministration with WAY-100635.

Animal Model:	Male ICR mice weighing 18–22 g
Dosage:	1.25, 2.5, and 5 mg/kg
Administration:	Oral administration
Result:	Had an effect on Antidepressant-like mice in TST and FST.

分子式

C₁₈H₂₃ClN₂O₂

分子量

334.84

CAS号

1339058-04-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 30 mg/mL (89.60 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.9865 mL	14.9325 mL	29.8650 mL
5 mM	0.5973 mL	2.9865 mL	5.9730 mL
10 mM	0.2987 mL	1.4933 mL	2.9865 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。-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: ≥ 2.5 mg/mL (7.47 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.47 mM，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 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-CD in saline)
Solubility: ≥ 2.5 mg/mL (7.47 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.47 mM，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。
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (7.47 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.47 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。