LY266097 hydrochloride
Based on 1 Customer Validation
LY266097 hydrochloride is a selective 5-HT2B receptor antagonist with pKis of 7.7, 9.8, and 7.6 for 5-HT2A, 5-HT2B, 5-HT2C, respectively. 5-HT2B receptor blockade contributes to the research in depression.
For research use only. We do not sell to patients.
- Purity: 98.41%
- CAS No.: 172895-39-5
- Formula: C21H24Cl2N2O2
- Molecular Weight:407.33
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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All 5-HT Receptor Isoforms
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Biological Activity
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5-HT2A Receptor |
5-HT2B Receptor |
5-HT2C Receptor |
5-HT2B Receptor 9.8 (pKi) |
5-HT2A Receptor 7.7 (pKi) |
5-HT2C Receptor 7.6 (pKi) |
LY266097 is a highly selective 5-HT2B receptor antagonist with a pKi of 9.7 for the human cloned 5-HT2B receptor and a 100-fold greater selectivity over human 5-HT2C and 5-HT2A sites[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
The administration of LY266097 alone or its addition on the last 3 days of a 14-day Escitalopram regimen increases pyramidal neuron firing and burst activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats weighing 250-350 g[1]
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Dosage:0.6 mg/kg
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Administration:Administered i.p. alone or concomitantly with Escitalopram (2 mg/kg) for 2 days
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Result:Short-term administration (0.6 mg/kg/day for 2 days; i.p.) alone had no effect on these parameters, its co-administration counteracted the inhibitory effect of escitalopram on the firing activity of DA neurons, resulting in a recovery to control level.
Chemical Information
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CAS No. 172895-39-5
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Appearance Solid
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Molecular Weight 407.33
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Formula C21H24Cl2N2O2
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Color Light yellow to light brown
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SMILES
CC1=CC2=C(NC3=C2CCNC3CC4=CC=C(OC)C(OC)=C4Cl)C=C1.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : 62.5 mg/mL (153.44 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (5.11 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Rami Hamati, et al. Serotonin-2B receptor antagonism increases the activity of dopamine and glutamate neurons in the presence of selective serotonin reuptake inhibition. Neuropsychopharmacology. 2020 Nov;45(12):2098-2105. [Content Brief]
[2]. Luc Maroteaux, et al. New therapeutic opportunities for 5-HT 2 receptor ligands. Pharmacol Ther. 2017 Feb;170:14-36. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4550 mL | 12.2751 mL | 24.5501 mL | 61.3753 mL |
| 5 mM | 0.4910 mL | 2.4550 mL | 4.9100 mL | 12.2751 mL | |
| 10 mM | 0.2455 mL | 1.2275 mL | 2.4550 mL | 6.1375 mL | |
| 15 mM | 0.1637 mL | 0.8183 mL | 1.6367 mL | 4.0917 mL | |
| 20 mM | 0.1228 mL | 0.6138 mL | 1.2275 mL | 3.0688 mL | |
| 25 mM | 0.0982 mL | 0.4910 mL | 0.9820 mL | 2.4550 mL | |
| 30 mM | 0.0818 mL | 0.4092 mL | 0.8183 mL | 2.0458 mL | |
| 40 mM | 0.0614 mL | 0.3069 mL | 0.6138 mL | 1.5344 mL | |
| 50 mM | 0.0491 mL | 0.2455 mL | 0.4910 mL | 1.2275 mL | |
| 60 mM | 0.0409 mL | 0.2046 mL | 0.4092 mL | 1.0229 mL | |
| 80 mM | 0.0307 mL | 0.1534 mL | 0.3069 mL | 0.7672 mL | |
| 100 mM | 0.0246 mL | 0.1228 mL | 0.2455 mL | 0.6138 mL |
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