1. Neuronal Signaling GPCR/G Protein
  2. Sigma Receptor 5-HT Receptor Adrenergic Receptor
  3. BMY-14802 hydrochloride

BMY-14802 hydrochloride  (Synonyms: BMY-14802-1; BMS 181100 hydrochloride)

Cat. No.: HY-108509 Purity: 98.02%
COA Handling Instructions

BMY-14802 hydrochloride (BMY-14802-1) is a selective and orally active sigma receptor antagonist with an IC50 of 112 nM. BMY-14802 hydrochloride is also a 5-HT1A and adrenergic α1 receptors agonist. BMY-14802 hydrochloride has antipsychotic effects.

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

BMY-14802 hydrochloride Chemical Structure

BMY-14802 hydrochloride Chemical Structure

CAS No. : 105565-55-7

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Solid + Solvent
10 mM * 1 mL in DMSO
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Solution
10 mM * 1 mL in DMSO USD 97 In-stock
Solid
5 mg USD 88 In-stock
10 mg USD 140 In-stock
25 mg USD 295 In-stock
50 mg USD 500 In-stock
100 mg USD 850 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

BMY-14802 hydrochloride (BMY-14802-1) is a selective and orally active sigma receptor antagonist with an IC50 of 112 nM. BMY-14802 hydrochloride is also a 5-HT1A and adrenergic α1 receptors agonist. BMY-14802 hydrochloride has antipsychotic effects[1][2][3].

IC50 & Target[1]

sigma Receptor

112 nM (IC50)

5-HT1A Receptor

 

α1-adrenergic receptor

 

In Vitro

Similar to other 5-HT1A agonists, BMY-14802 hydrochloride affects the firing of 5-HTergic and catecholaminergic neurons and affects behaviors mediated by 5-HT in a 5-HT1A-sensitive manner. BMY-14802 hydrochloride is devoid of significant affinity for the D2 receptor[3].

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

In Vivo

BMY-14802 (5 mg/kg, 10 mg/kg or 20 mg/kg, ip; once) hydrochloride shows anti-dyskinetic efficacy across a 4-fold dose range against L-DOPA-induced dyskinesias (LID) and is also effective in reducing D1 and D2 receptor agonist-induced dyskinesias. Importantly, at anti-LID doses, BMY-14802 hydrochloride does not affect the efficacy of L-DOPA against lesion-induced akinesia[2].

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

Molecular Weight

384.85

Formula

C18H23ClF2N4O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

[H]Cl.OC(C1=CC=C(F)C=C1)CCCN2CCN(C3=NC=C(F)C=N3)CC2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (324.80 mM; Need ultrasonic; 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 2.5984 mL 12.9921 mL 25.9841 mL
5 mM 0.5197 mL 2.5984 mL 5.1968 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (5.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.08 mg/mL (5.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
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)

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). 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 2.5984 mL 12.9921 mL 25.9841 mL 64.9604 mL
5 mM 0.5197 mL 2.5984 mL 5.1968 mL 12.9921 mL
10 mM 0.2598 mL 1.2992 mL 2.5984 mL 6.4960 mL
15 mM 0.1732 mL 0.8661 mL 1.7323 mL 4.3307 mL
20 mM 0.1299 mL 0.6496 mL 1.2992 mL 3.2480 mL
25 mM 0.1039 mL 0.5197 mL 1.0394 mL 2.5984 mL
30 mM 0.0866 mL 0.4331 mL 0.8661 mL 2.1653 mL
40 mM 0.0650 mL 0.3248 mL 0.6496 mL 1.6240 mL
50 mM 0.0520 mL 0.2598 mL 0.5197 mL 1.2992 mL
60 mM 0.0433 mL 0.2165 mL 0.4331 mL 1.0827 mL
80 mM 0.0325 mL 0.1624 mL 0.3248 mL 0.8120 mL
100 mM 0.0260 mL 0.1299 mL 0.2598 mL 0.6496 mL
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BMY-14802 hydrochloride Related Classifications

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  • Do most proteins show cross-species activity?

    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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BMY-14802 hydrochloride
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