Hypidone hydrochloride YL0919|cas:1339058-04-6|西域试剂

Hypidone hydrochloride YL0919,99.82%

产品编号：Bellancom-100769| CAS NO：1339058-04-6| 分子式：C₁₈H₂₃ClN₂O₂| 分子量：334.84

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货号	价格	库存与货期
Bellancom-100769	￥900.00	杭州北京（现货）
Bellancom-100769	￥1500.00	杭州北京（现货）
Bellancom-100769	￥1900.00	杭州北京（现货）
Bellancom-100769	￥2800.00	杭州北京（现货）
Bellancom-100769	￥4500.00	杭州北京（现货）

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Hypidone hydrochloride YL0919

产品介绍

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。

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 [³H]-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 [³H]-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 [³H]nisoxetine and [³H]win35428 binding with Ki values of 650 nM and 2652 nM respectively.

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

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.

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

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.

体内研究

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

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.

性状

Solid

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 (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: ≥ 2.5 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。
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: ≥ 2.5 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。
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: ≥ 2.5 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。