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

Lesogaberan hydrochloride (Synonyms: AZD-3355 hydrochloride)

Cat. No.: HY-10061B Purity: ≥98.0%
Handling Instructions

Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. 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

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5 mg USD 400 In-stock
Estimated Time of Arrival: December 31
10 mg USD 680 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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 receptors. 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].

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

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 hydrochloride (0.08 mg/mL; 48 hours) protects human islet β-cells from apoptosis in islet grafts in mice[2].
Lesogaberan hydrochloride (7 μmol/kg) shows high oral availability (88% in the dog and 100% in the rat) and relatively low systemic clearance in female SpragueDawley rats[1].

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.
Molecular Weight

177.54

Formula

C₃H₁₀ClFNO₂P

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)

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
10 mM 0.5633 mL 2.8163 mL 5.6325 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Product Name:
Lesogaberan hydrochloride
Cat. No.:
HY-10061B
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