LY3020371

SKU:BHB21900799
Overview
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LY3020371 (CAS 1377615-75-2) is an antagonist. Reported to act on hmGluR2, hmGluR3. Relevant to GPCR/G Protein and Neuronal Signaling research. Molecular formula C15H15F2NO5S, molecular weight 359.35 g/mol.
CAS Number 1377615-75-2
Molecular Weight 359.35 g/mol
Target hmGluR2, hmGluR3
Storage See Certificate of Analysis
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Catalog no. Size
HY-131289-50MG 50 mg
HY-131289-100MG 100 mg
HY-131289-250MG 250 mg
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Field Specification
Target hmGluR2, hmGluR3
CAS no. 1377615-75-2
Applications
  • Functional Assay (In Vitro)
Molecular weight 359.35
Molecular formula C15H15F2NO5S
SMILES O=C([C@@]1(N)[C@]2([H])[C@@H](C(O)=O)[C@]2([H])[C@H](O)[C@H]1CSC3=CC=C(F)C(F)=C3)O
Storage Refer to Certificate of Analysis (CoA) for storage conditions
Shipping Room temperature in continental US; may vary elsewhere.
Catalog no. (Mfr.) HY-131289
Main SKU BHB21900799
Antagonists

Compound Overview

LY3020371 is a potent, selective antagonist of the metabotropic glutamate (mGlu) 2/3 receptors, with Ki values of 5.26 nM at hmGluR2 and 2.50 nM at hmGluR3. It can be used in depression research[1][2]. It has the molecular formula C15H15F2NO5S and a molecular weight of 359.35 g/mol.

Physical & Chemical Properties

CAS Number 1377615-75-2
Molecular Formula C15H15F2NO5S
Molecular Weight 359.35 g/mol
SMILES O=C([C@@]1(N)[C@]2([H])[C@@H](C(O)=O)[C@]2([H])[C@H](O)[C@H]1CSC3=CC=C(F)C(F)=C3)O
Target hmGluR2, hmGluR3
Signaling Pathway GPCR/G Protein; Neuronal Signaling
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Shipping Room temperature in continental US; may vary elsewhere.

Biological Activity

IC50 & Target[1]

hmGluR2

5.26 nM (Ki)

hmGluR3

2.50 nM (Ki)

Literature Cited

Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.

[1]. Witkin JM, In vitro pharmacological and rat pharmacokinetic characterization of LY3020371, a potent and selective mGlu 2/3 receptor antagonist. Neuropharmacology. 2017 Mar 15;115:100-114.

[2]. Witkin JM, et al. Comparative Effects of LY3020371, a Potent and Selective Metabotropic Glutamate (mGlu) 2/3 Receptor Antagonist, and Ketamine, a Noncompetitive N-Methyl-d-Aspartate Receptor Antagonist in Rodents: Evidence Supporting the Use of mGlu2/3 A

[3]. Witkin JM, et al. mGlu2/3 receptor antagonism: A mechanism to induce rapid antidepressant effects without ketamine-associated side-effects. Pharmacol Biochem Behav. 2020 Mar;190:172854.

Safety

For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.

In Vitro

LY3020371 (0.1 nM-100 μM) displaces the mGlu2/3 agonist ligand [3H]-459477 from its binding sites competitively and with high affinity[1]. LY3020371 (0.1 nM-100 μM) prevents DCG-IV-induced inhibition of forskolin-stimulated cAMP production, with IC50=16.2 nM for mGlu2 and IC50=6.21 nM for mGlu3, in cells expressing the recombinant human receptors[1]. LY3020371 (0.3-30000 nM) antagonizes LY379268-inhibited cAMP formation in a concentration-dependent manner[1]. LY3020371 (1-10000 nM) reverses the LY379268-suppressed, K+-evoked glutamate release, with an IC50 of 86 nM[1]. LY3020371 (0.3-10000 nM) completely blocks the LY379268-suppressed response in a concentration-dependent manner, with an IC50 of 33.9 nM[1].

In Vivo

LY3020371 (0.3-3 mg/kg, a single i.v.) significantly raises how many dopamine cells are spontaneously active in the rat ventral tegmental area (VTA)[2]. Tissue oxygen in the anterior cingulate cortex (ACC) of rats rises dose dependently with LY3020371 (1-10 mg/kg, i.p., weekly for 5 weeks)[2]. In freely moving rats, LY3020371 (10 mg/kg, a single i.p.) elevates monoamine efflux in the medial prefrontal cortex[2]. Cumulative wake time in rats increases dose- and time-dependently with LY3020371 (1-30 mg/kg, a single i.v.), without rebound hypersomnolence[2]. In the rat forced-swim assay, LY3020371 (0.1-10 mg/kg, a single i.v.) shortens the period during which rats stay immobile in the forced-swim test[2].

Animal ModelMale Sprague-Dawley rats (230-350 g)[1]
Dosage0.3, 1, 3 mg/kg
AdministrationI.v. daily 5 days per week for 2 weeks
ResultIncreased the number of actively firing dopamine neurons in the VTA of anesthetized rats.

Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.

Q.Why is there no price listed?
A.Every size of this product is quoted on inquiry. Send us the size you need and we will come back with price and lead time.
Q.Can this be used in humans or for diagnostics?
A.No. This product is supplied For Research Use Only. It is not for diagnostic or therapeutic procedures and not for human or veterinary use.

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bioRxiv. 2026 Feb 11.

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