1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. LY266097 hydrochloride

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.

LY266097 hydrochloride Chemical Structure

LY266097 hydrochloride Chemical Structure

CAS No. : 172895-39-5

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Based on 1 publication(s) in Google Scholar

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Description

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[1].

IC50 & Target[1]

5-HT2B Receptor

9.8 (pKi)

5-HT2A Receptor

7.7 (pKi)

5-HT2C Receptor

7.6 (pKi)

In Vitro

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.

In Vivo

LY266097 (0.6?mg/kg for 2-day administration) rescues Escitalopram-induced decrease in dopamine (DA) [1].
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.

Animal Model: Male Sprague-Dawley rats weighing 250-350 g[1]
Dosage: 0.6 mg/kg
Administration: Administered i.p. alone or concomitantly with Escitalopram (2 mg/kg) for 2 days
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.
Molecular Weight

407.33

Formula

C21H24Cl2N2O2

CAS No.
Appearance

Solid

Color

Light yellow to light brown

SMILES

CC1=CC2=C(NC3=C2CCNC3CC4=CC=C(OC)C(OC)=C4Cl)C=C1.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

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
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4550 mL 12.2751 mL 24.5501 mL
5 mM 0.4910 mL 2.4550 mL 4.9100 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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In Vivo:

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.

  • Protocol 1

    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.
In Vivo Dissolution Calculator
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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+
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
References

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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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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LY266097 hydrochloride
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