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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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| 250mg |
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YL-0919 is a novel, potent and orally bioactive antidepressant acting as 5-HT1A receptor agonist (Ki=0.19 nM) and selective serotonin reuptake inhibitor.
| Targets |
5-HT1A Receptor
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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]. |
| 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]. |
| Animal Protocol |
Male ICR mice weighing 18–22 g
1.25, 2.5, and 5 mg/kg Oral administration |
| References |
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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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| Appearance |
Solid powder
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| SMILES |
C1CN(CCC1(CN2C=CC=CC2=O)O)CC3=CC=CC=C3.Cl
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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 |
|---|---|
| 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.
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