LEI-101

Cat. No.: HY-124283A: FAQs
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LEI-101 is a potent, selective, and orally bioavailable cannabinoid CB2 receptor agonist, with a pEC₅₀ of 8 for hCB2, and a pK_i 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

CAS No. : 2250025-91-1

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CB1 CB2

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Purity & Documentation
References
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Description

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].

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

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.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Mario van der Stelt, et al. Discovery and Optimization of 1-(4-(pyridin-2-yl)benzyl)imidazolidine-2,4-dione Derivatives as a Novel Class of Selective Cannabinoid CB2 Receptor Agonists. J Med Chem. 2011 Oct 27;54(20):7350-62. [Content Brief]

[2]. Partha Mukhopadhyay, et al. The Novel, Orally Available and Peripherally Restricted Selective Cannabinoid CB2 Receptor Agonist LEI-101 Prevents Cisplatin-Induced Nephrotoxicity. Br J Pharmacol. 2016 Feb;173(3):446-58. [Content Brief]

LEI-101 Related Classifications

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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:

LEI-1012250025-91-1LEI101LEI 101Cannabinoid ReceptorkidneydysfunctionneuropathicpainInhibitorinhibitorinhibit

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