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  3. LY3027788 hydrochloride

LY3027788 hydrochloride 

Cat. No.: HY-117606A
Handling Instructions

LY3027788 hydrochloride, a diester analog of LY3020371 which is an mGlu2/3 receptor antagonist, is a potent and orally active prodrug of LY3020371. LY3027788 hydrochloride has antidepressant efficacy.

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

LY3027788 hydrochloride Chemical Structure

LY3027788 hydrochloride Chemical Structure

CAS No. : 1377615-55-8

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Description

LY3027788 hydrochloride, a diester analog of LY3020371 which is an mGlu2/3 receptor antagonist, is a potent and orally active prodrug of LY3020371. LY3027788 hydrochloride has antidepressant efficacy[1][2].

IC50 & Target[1]

mGluR2

 

mGluR3

 

In Vitro

LY3027788 (4.8-27 mg/kg; a single p.o.) produces antidepressant-like decreases in immobility times in the forced-swim test in mice[1].
LY3027788 (4.8-16 mg/kg; a single p.o.) enhances the locomotor stimulant effects of quinpirole at the dose of 16 mg/kg in the locomotor activity assay in mice[1].
LY3027788 (10-30 mg/kg; a single p.o.) dose dependently increases the wake time of rats without engendering rebound hypersomnolence[1].
LY3027788 (a single p.o.) leads to the rapid and dose-proportionate appearance of the pharmacologically active species LY3020371 in plasma of both mouse (4.8-27 mg/kg) and rat (3-30 mg/kg)[1].

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

In Vivo

LY3027788 (4.8-27 mg/kg; a single p.o.) produces antidepressant-like decreases in immobility times in the forced-swim test in mice[1].
LY3027788 (4.8-16 mg/kg; a single p.o.) enhances the locomotor stimulant effects of quinpirole at the dose of 16 mg/kg in the locomotor activity assay in mice[1].
LY3027788 (10-30 mg/kg; a single p.o.) dose dependently increases the wake time of rats without engendering rebound hypersomnolence[1].
LY3027788 (a single p.o.) leads to the rapid and dose-proportionate appearance of the pharmacologically active species LY3020371 in plasma of both mouse (4.8-27 mg/kg) and rat (3-30 mg/kg)[1].

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

Animal Model: Male Sprague-Dawley mice (20-25 g)[1]
Dosage: 4.8, 16, 27 mg/kg
Administration: A single p.o. (60 minutes prior to testing)
Result: Potent and efficacious with a minimal effective dose of 16 mg/kg in the mouse forced-swim assay.
The ED60 was 8.2 mg/kg.
Molecular Weight

628.04

Formula

C₂₅H₃₂ClF₂NO₁₁S

CAS No.
SMILES

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

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Keywords:

LY3027788LY 3027788LY-3027788mGluRMetabotropic glutamate receptorsLY3020371mGlu2/3prodrugantidepressantInhibitorinhibitorinhibit

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LY3027788 hydrochloride
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HY-117606A
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