1. GPCR/G Protein
    Neuronal Signaling
  2. Cannabinoid Receptor
  3. LEI-101

LEI-101 

Cat. No.: HY-124283A
Handling Instructions

LEI-101 is a potent, selective, and orally bioavailable cannabinoid CB2 receptor agonist, with a pEC50 of 8 for hCB2, and a pKi of less than 4 for hERG. LEI-101 is ~100-fold more potent in binding to CB2 receptors than to CB1 receptors.

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

LEI-101 Chemical Structure

LEI-101 Chemical Structure

CAS No. : 2250025-91-1

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Description

LEI-101 is a potent, selective, and orally bioavailable cannabinoid CB2 receptor agonist, with a pEC50 of 8 for hCB2, and a pKi of less than 4 for hERG. LEI-101 is ~100-fold more potent in binding to CB2 receptors than to CB1 receptors[1][2].

In Vivo

LEI-101 (2, 6, and 20 mg/kg, po) shows in vivo activity in a spinal nerve ligation model of neuropathic pain in rats[1].
LEI‐101 (p.o. or i.p.) at 3 or 10 mg/kg dose-dependently prevents kidney dysfunction and/or morphological damage induced by cisplatin in mice[2].

Animal Model: Neuropathy-induced mechanical allodynia in male wistar rats[1].
Dosage: 2, 6, and 20 mg/kg.
Administration: PO, single dose.
Result: Induced a dose-dependent antinociceptive effect after 2 h of dosing.
Animal Model: Fed male Wistar rats[1].
Dosage: 1 mg/kg iv and 5 mg/kg po (Pharmacological Analysis).
Administration: IV and PO.
Result: Exhibited T1/2 of 1.7 h and 0.8 h for po and iv administration.
Had a low clearance and 100% oral bioavailability.
Molecular Weight

508.99

Formula

C₂₃H₂₆ClFN₄O₄S

CAS No.

2250025-91-1

SMILES

O=C1N(C2CC2)C(CN1CC3=CC=C(C4=NC(CN5CCS(CC5)(=O)=O)=C(F)C=C4)C=C3)=O.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

LEI-101LEI101LEI 101Cannabinoid ReceptorkidneydysfunctionneuropathicpainInhibitorinhibitorinhibit

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LEI-101
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