| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Targets |
5-HT1A Receptor
YL-0919 targets the 5-hydroxytryptamine receptor 1A (5-HT1A) as an agonist and the serotonin transporter (SERT) as a selective serotonin reuptake inhibitor. It has a Ki of 0.19 nM for the 5-HT1A receptor and inhibits 5-HT uptake with IC50 values of 1.78 nM in rat cerebral cortical synaptosomes and 1.93 nM in human recombinant cells. |
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| ln Vitro |
Hypidone hydrochloride inhibits the uptake of [3H]-5-HT into rat cerebral cortical synaptosomes and HEK293 cells that are stable hSERT-expressing cells with IC50 values of 1.78 nM and 1.93, respectively[1].
Hypidone hydrochloride (0.01 nM-10 μM) exhibits a concentration-dependent inhibitory effect on cAMP formation, which is stimulated by forskolin with an IC50 of approximately 23.9 nM. Furthermore, WAY-100635 inhibits the inhibition of forskolin-stimulated cAMP formation mediated by hydridone hydrochloride in antagonism studies[1]. Hypidone hydrochloride demonstrates affinities to rat 5-HT1A receptors, serotonin transporter (SERT) with high affinity (Ki=0.19 and 0.72 nM, respectively); however, its affinity to NET and DAT is low, as it blocks [3H]win35428 and [3H]nisoxetine binding with Ki values of 650 nM and 2652 nM, respectively[1]. YL-0919 is a potent 5-HT1A receptor agonist with a Ki of 0.19 nM and a selective serotonin reuptake inhibitor with IC50 values of 1.78 nM and 1.93 nM. It shows remarkable antidepressant effects in animal models. The compound is a novel antidepressant candidate with dual activity on the serotonergic system. |
| ln Vivo |
Hypidone hydrochloride (YL0919) (oral administration; 1.25 or 5 mg/kg; 4 weeks) and fluoxetine (10 mg/kg) reverse the inhibition of locomotor activity in CUS rats[1].
Hypidone hydrochloride (oral administration; 1.25, 2.5, and 5 mg/kg; 4 weeks) dramatically shortens the immobility period in TST during mice FST in mice. Furthermore, in a different OFT, hypidone hydrochloride has no effect on locomotor activity. Furthermore, coadministration of WAY-100635 completely bunts the antidepressant-like effect of hypidone hydrochloride in TST and FST[1]. YL-0919 has shown remarkable antidepressant effects in animal models. As an orally active compound with dual activity as a 5-HT1A receptor agonist and a selective serotonin reuptake inhibitor, it is expected to exhibit efficacy in preclinical models of depression. Further studies are needed to fully characterize its pharmacokinetic and pharmacodynamic profiles. |
| Enzyme Assay |
The in vitro receptor binding assay for YL-0919 typically involves measuring its binding affinity to the 5-HT1A receptor using radioligand binding techniques. Membranes from cells expressing the recombinant receptor are incubated with a radiolabeled ligand and varying concentrations of the test compound. The Ki value is determined from the competition binding curves.
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| Cell Assay |
The in vitro cellular assay for YL-0919 typically involves measuring its ability to inhibit 5-HT uptake. Rat cerebral cortical synaptosomes or human recombinant cells are incubated with radiolabeled 5-HT and varying concentrations of the compound. The amount of 5-HT taken up is measured, and the IC50 value is determined from the dose-response curve.
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| Animal Protocol |
Male ICR mice weighing 18–22 g
1.25, 2.5, and 5 mg/kg Oral administration In vivo animal studies for YL-0919 typically involve the use of rodent models of depression, such as the forced swim test or tail suspension test. Animals are administered the compound via oral gavage at various doses, and behavioral responses are assessed. The compound's antidepressant effects are evaluated by comparing treated and control groups. |
| ADME/Pharmacokinetics |
YL-0919 has a molecular weight of 334.84 g/mol and a molecular formula of C18H22N2O2·HCl. It is soluble in DMSO (67 mg/mL) and ethanol (34 mg/mL), but insoluble in water. The compound should be stored under recommended conditions. The purity is typically ≥98%. Further detailed PK parameters are available from the manufacturer's data sheets.
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| Toxicity/Toxicokinetics |
Specific toxicology data for YL-0919 are not extensively reported in the public domain. The compound is intended for research use only and should be handled with appropriate laboratory safety precautions. Standard safety assessments would be required before any clinical application. Researchers should consult the safety data sheet for detailed handling and disposal information.
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| References |
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| Additional Infomation |
YL-0919 (Hypidone hydrochloride) is a novel orally active antidepressant agent with dual activity as a highly selective 5-HT uptake blocker and an effective 5-HT1A receptor agonist. It has a Ki of 0.19 nM for the 5-HT1A receptor and inhibits 5-HT uptake with an IC50 of 1.78 nM. The compound shows remarkable antidepressant effects in animal models. It has not yet entered clinical trials and is strictly for preclinical research purposes.
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| Molecular Formula |
C18H23CLN2O2
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|---|---|
| Molecular Weight |
334.8404
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| Exact Mass |
334.14
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| Elemental Analysis |
C, 64.57; H, 6.92; Cl, 10.59; N, 8.37; O, 9.56
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| CAS # |
1339058-04-6
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| PubChem CID |
122412736
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| Appearance |
White to off-white solid powder
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| Melting Point |
216 - 218 °C
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
23
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| Complexity |
444
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl[H].O([H])C1(C([H])([H])N2C([H])=C([H])C([H])=C([H])C2=O)C([H])([H])C([H])([H])N(C([H])([H])C2C([H])=C([H])C([H])=C([H])C=2[H])C([H])([H])C1([H])[H]
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| InChi Key |
OXILSFMNCPZGAH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H22N2O2.ClH/c21-17-8-4-5-11-20(17)15-18(22)9-12-19(13-10-18)14-16-6-2-1-3-7-16;/h1-8,11,22H,9-10,12-15H2;1H
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| Chemical Name |
1-[(1-benzyl-4-hydroxypiperidin-4-yl)methyl]pyridin-2-one;hydrochloride
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| Synonyms |
YL-0919; YL 0919; YL0919
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~67 mg/mL (~200.1 mM)
Ethanol: ~34 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.47 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.47 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.47 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Link: https://clinicaltrials.gov/ct2/show/NCT04598607
Conditions:Major Depressive DisorderLink: https://clinicaltrials.gov/ct2/show/NCT03739632
Conditions:Major Depressive DisorderLink: https://clinicaltrials.gov/ct2/show/NCT03404466
Conditions:Major Depressive Disorder
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