貨號	規格	價格	上海	北京	武漢	南京
S82903-1mg	99.7%	￥170.00 S82903-1mg ￥170.00 現貨	9 9	-	-	-
S82903-2mg	99.7%	￥280.00 S82903-2mg ￥280.00 現貨	8 8	-	-	-
S82903-5mg	99.7%	￥390.00 S82903-5mg ￥390.00 現貨	8 8	-	-	-
S82903-10mg	99.7%	￥490.00 S82903-10mg ￥490.00 現貨	5 5	-	-	-
S82903-25mg	99.7%	￥730.00 S82903-25mg ￥730.00 現貨	5 5	-	-	-
S82903-50mg	99.7%	￥1180.00 S82903-50mg ￥1180.00 現貨	5 5	-	-	-
S82903-100mg	99.7%	￥2230.00 S82903-100mg ￥2230.00 現貨	5 5	-	-	-

產品介紹

Hypidone hydrochloride (YL0919) is an orally active antidepressant agent with dual activity as a highly seletive?5-HT uptake?blocker and an effective?5-HT1A?receptor?agonist (Ki=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

產品描述：

靶點：

5-HT1A Receptor;5-HTReceptor

體外研究：

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 (Ki=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

體內研究：

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.

參考文獻：

1. Chen, H. X. et al. Antidepressant-like activity of YL-0919: a novel combined selective serotonin reuptake inhibitor and 5-HT1A receptor agonist. PloS one 8, e83271, doi:10.1371/journal.pone.0083271 (2013). 2. Qin, J. J. et al. The role of activation of the 5-HT1A receptor and adenylate cyclase in the antidepressant-like effect of YL-0919, a dual 5-HT1A agonist and selective serotonin reuptake inhibitor. Neuroscience letters 582, 104-108, 2014.09.009 (2014)

溶解性：

Soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.986 ml	14.932 ml	29.865 ml
5 mM	0.597 ml	2.986 ml	5.973 ml
10 mM	0.299 ml	1.493 ml	2.986 ml
50 mM	0.06 ml	0.299 ml	0.597 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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