2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. Lesogaberan hydrochloride

Lesogaberan hydrochloride  (Synonyms: AZD-3355 hydrochloride)

Cat. No.: HY-10061B Purity: ≥98.0%
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Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptor. The affinity (Kis) of Lesogaberan hydrochloride for rat GABAB and GABAA receptors, as measured by displacement of [3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan hydrochloride inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.

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

Lesogaberan hydrochloride Chemical Structure

Lesogaberan hydrochloride Chemical Structure

CAS No. : 2925644-17-1

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25 mg USD 1350 In-stock
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Based on 1 publication(s) in Google Scholar

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Lesogaberan hydrochloride Related Antibodies

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Description

Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptor. The affinity (Kis) of Lesogaberan hydrochloride for rat GABAB and GABAA receptors, as measured by displacement of [3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan hydrochloride inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action[1].

IC50 & Target

Ki: 5.1±1.2 nM (rat GABAB), 1.4±0.3 μM (rat GABAA)[1]
EC50: 8.6±0.77 nM (human GABAB receptor)[1]
In Vitro

Lesogaberan hydrochloride (3-30 nM) enhances human islet cell proliferation in vitro[2].

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

Lesogaberan hydrochloride Related Antibodies

Cell Proliferation Assay[2]

Cell Line: Human islet cells
Concentration: 3, 10, and 30 nM
Incubation Time: 4 days
Result: Had a small but nonsignificant promitotic effect at 3 nM, while treatment at higher dosages (10 and 30 nM) led to a 2-3-fold increase in proliferation relative to that of islets cultured in medium alone.
In Vivo

Lesogaberan hydrochloride potently stimulates recombinant human GABAB receptors and inhibits transient lower esophageal sphincter relaxation (TLESR) in dogs, with a biphasic dose-response curve[1].
Oral Lesogaberan (0.08 mg/mL; 48 hours) hydrochloride protects human islet β-cells from apoptosis in islet grafts in mice[2].
Lesogaberan (7 μmol/kg) hydrochloride shows high oral availability (88% in the dog and 100% in the rat) and relatively low systemic clearance in female SpragueDawley rats[1].

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

Animal Model: Diabetic NOD/scid mice were implanted with human islets[2]
Dosage: 0.08 mg/mL
Administration: 48 hours
Result: Significantly reduced the percentages of apoptotic islet cells and increased the frequency of insulin+ β-cells in human islet grafts.
Animal Model: Female Sprague Dawley rats[1]
Dosage: 7 μmol/kg (Pharmacokinetic Analysis)
Administration: Oral
Result: High oral availability (88% in the dog and 100% in the rat) and relatively low systemic clearance. Plasma protein binding was 1% in rat and human plasma.
Clinical Trial
Molecular Weight

177.54

Formula

C3H10ClFNO2P
CAS No.
Appearance

Viscous Liquid

Color

Colorless to light yellow

SMILES

O=P(C[C@H](F)CN)O.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 240 mg/mL (1351.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 100 mg/mL (563.25 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.6325 mL 28.1627 mL 56.3253 mL
5 mM 1.1265 mL 5.6325 mL 11.2651 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • 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: ≥ 6 mg/mL (33.80 mM); Clear solution

    This protocol yields a clear solution of ≥ 6 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (60.0 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: ≥ 6 mg/mL (33.80 mM); Clear solution

    This protocol yields a clear solution of ≥ 6 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (60.0 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 100 mg/mL (563.25 mM); Clear solution; Need ultrasonic

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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: ≥98.0%

COA (245 KB) HNMR (251 KB) MS (177 KB)

Handling Instructions (2659 KB)
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 (stored under nitrogen). 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
H2O / DMSO 1 mM 5.6325 mL 28.1627 mL 56.3253 mL 140.8133 mL
5 mM 1.1265 mL 5.6325 mL 11.2651 mL 28.1627 mL
10 mM 0.5633 mL 2.8163 mL 5.6325 mL 14.0813 mL
15 mM 0.3755 mL 1.8775 mL 3.7550 mL 9.3876 mL
20 mM 0.2816 mL 1.4081 mL 2.8163 mL 7.0407 mL
25 mM 0.2253 mL 1.1265 mL 2.2530 mL 5.6325 mL
30 mM 0.1878 mL 0.9388 mL 1.8775 mL 4.6938 mL
40 mM 0.1408 mL 0.7041 mL 1.4081 mL 3.5203 mL
50 mM 0.1127 mL 0.5633 mL 1.1265 mL 2.8163 mL
60 mM 0.0939 mL 0.4694 mL 0.9388 mL 2.3469 mL
80 mM 0.0704 mL 0.3520 mL 0.7041 mL 1.7602 mL
100 mM 0.0563 mL 0.2816 mL 0.5633 mL 1.4081 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Lesogaberan hydrochloride Related Classifications

Help & FAQs
  • 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.

Keywords:

Lesogaberan2925644-17-1AZD-3355AZD3355AZD 3355GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorIsletCellSurvivalGastroesophagealrefluxdiseaseGERDdiabeteGABABInhibitorinhibitorinhibit

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