1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. YL0919

YL0919 

Cat. No.: HY-100769 Purity: 99.77%
Handling Instructions

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). YL0919 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. YL0919 shows remarkable antidepressant effects in animal models and has the poential for the investigation of depressive disorder.

For research use only. We do not sell to patients.

YL0919 Chemical Structure

YL0919 Chemical Structure

CAS No. : 1339058-04-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
2 mg USD 50 In-stock
Estimated Time of Arrival: December 31
5 mg USD 80 In-stock
Estimated Time of Arrival: December 31
10 mg USD 100 In-stock
Estimated Time of Arrival: December 31
25 mg USD 150 In-stock
Estimated Time of Arrival: December 31
50 mg USD 250 In-stock
Estimated Time of Arrival: December 31
100 mg USD 450 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

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). YL0919 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. YL0919 shows remarkable antidepressant effects in animal models and has the poential for the investigation of depressive disorder[1].

IC50 & Target[1]

5-HT1A Receptor

 

In Vitro

YL0919 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[1].
YL0919 (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 YL0919-mediated inhibition of forskolin-stimulated cAMP formation[1].
YL0919 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[1].

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

In Vivo

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[1].
YL0919 (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, YL0919 displays no effect on the locomotor activity in a separate OFT. Furthermore, the antidepressant-like effect of YL0919 in TST and FST is completely bunted by coadministration with WAY-100635[1].

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

Animal Model: Male ICR mice weighing 18–22 g[1]
Dosage: 1.25, 2.5, and 5 mg/kg
Administration: Oral administration
Result: Had an effect on Antidepressant-like mice in TST and FST.
Molecular Weight

334.84

Formula

C₁₈H₂₃ClN₂O₂

CAS No.

1339058-04-6

SMILES

O=C1C=CC=CN1CC2(O)CCN(CC3=CC=CC=C3)CC2.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 30 mg/mL (89.60 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.47 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.47 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.47 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

YL0919YL 0919YL-09195-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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YL0919
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