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  3. LY3020371 hydrochloride

LY3020371 hydrochloride 

Cat. No.: HY-123820
Handling Instructions

LY3020371 hydrochloride is a potent, selective metabotropic glutamate 2/3 receptor (mGlu2/3) antagonist with Ki of 5.3 and 2.5 nM, potently blocks cAMP formation with IC50 of 16.2 nM. LY3020371 hydrochloride exerts an antidepressant-like signature in vivo.

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LY3020371 hydrochloride Chemical Structure

LY3020371 hydrochloride Chemical Structure

CAS No. : 1377615-44-5

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Description

LY3020371 hydrochloride is a potent, selective metabotropic glutamate 2/3 receptor (mGlu2/3) antagonist with Ki of 5.3 and 2.5 nM, potently blocks cAMP formation with IC50 of 16.2 nM[1]. LY3020371 hydrochloride exerts an antidepressant-like signature in vivo[2].

IC50 & Target[1]

mGluR2

5.3 nM (Ki)

mGluR3

2.5 nM (Ki)

In Vitro

LY3020371 hydrochloride (LY3020371.HCl) displaces binding of the mGlu2/3 agonist ligand [3H]-459477 with high affinity (hmGlu2 Ki=5.26 nM; hmGlu3 Ki=2.50 nM)[1].
LY3020371 hydrochloride (LY3020371.HCl) (0.1 nM-100 μM; 1 hours) potently blocks mGlu2/3 agonist (DCG-IV)-inhibited, forskolin-stimulated cAMP formation (IC50=16.2 nM), an effect that was similarly observed in hmGlu3-expressing cells ( IC50=6.21 nM)[1].
LY3020371 hydrochloride (LY3020371.HCl) blocks agonist-suppressed spontaneous Ca2+ oscillations (IC50=34 nM) and in an intact hippocampal slice preparation (IC50=46 nM)[1].

In Vivo

LY3020371 hydrochloride (LY3020371.HCl) (Intravenous injection; 3-15 mg/kg) in rats leads to cerebrospinal fluid drug levels that are expected to effectively block mGlu2/3receptors[1].
LY3020371 hydrochloride (LY3020371) (intraperitoneal injection; 3 mg/kg, 10 mg/kg; 2 hours) has clear wake promoting effects, resulting in a large reduction in NREM sleep in the Wistar rats during the light phase[3].

Molecular Weight

395.81

Formula

C₁₅H₁₆ClF₂NO₅S

CAS No.

1377615-44-5

SMILES

O=C([[email protected]@]1(N)[[email protected]]2([H])[[email protected]@H](C(O)=O)[[email protected]]2([H])[[email protected]](O)[[email protected]]1CSC3=CC=C(F)C(F)=C3)O.[H]Cl

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Storage

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

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Product Name:
LY3020371 hydrochloride
Cat. No.:
HY-123820
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