1. GPCR/G Protein
    Neuronal Signaling
  2. mGluR
  3. LY367385 hydrochloride

LY367385 hydrochloride 

Cat. No.: HY-107515A
Handling Instructions

LY367385 hydrochloride is a highly selective and potent mGluR1a antagonist. LY367385 hydrochloride has an IC50 of 8.8 μM for inhibits of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with >100 μM for mGlu5a. LY367385 hydrochloride has neuroprotective, anticonvulsant and antiepileptic effects.

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

LY367385 hydrochloride Chemical Structure

LY367385 hydrochloride Chemical Structure

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 110 In-stock
Estimated Time of Arrival: December 31
5 mg USD 100 In-stock
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10 mg USD 170 In-stock
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25 mg USD 350 In-stock
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50 mg USD 550 In-stock
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100 mg USD 950 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

LY367385 hydrochloride is a highly selective and potent mGluR1a antagonist. LY367385 hydrochloride has an IC50 of 8.8 μM for inhibits of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with >100 μM for mGlu5a. LY367385 hydrochloride has neuroprotective, anticonvulsant and antiepileptic effects[1][2].

IC50 & Target[1]

mGluR1a

8.8 μM (IC50)

In Vitro

LY367385 combined with N-methyl-D-aspartate (NMDA) during the toxic pulse attenuates neuronal degeneration in a concentration-dependent fashion, with a maximal reduction of NMDA toxicity ranging from 40 to 60%. LY367385 shows greater efficacy than LY367366 and neither of these compounds influenced neuronal viability per se. LY367385 shows potent neuroprotective effects, with causing a 50% reduction in (S)-3,5-Dihydroxyphenylglycine (DHPG) potentiation at a concentration of 10 nM. Under experimental conditions at higher concentrations of antagonist, LY367385 a completely antagonized the amplification of NMDA toxicity by DHPG[2].

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

In Vivo

LY367385 has been administered intracerebroventricularly (i.c.v.) to DBA/2 mice and lethargic mice (lh/lh), and focally into the inferior colliculus of genetically epilepsy prone rats (GEPR). In DBA/2 mice, LY367385 produces a rapid, transient suppression of sound-induced clonic seizures ED50 = 12 nM, i.c.v., 5 min). In lethargic mice, LY367385 significantly reduces the incidence of spontaneous spike and wave discharges on the electroencephalogram, from 30 to >150 min after the administration of LY367385, 250 nM, i.c.v[3].
In genetically epilepsy prone rats, LY367385 reduces sound-induced clonic seizures. LY367385, 160 nM bilaterally, fully suppresses clonic seizures after 2-4 h[3].

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

Molecular Weight

245.66

Formula

C₁₀H₁₂ClNO₄

SMILES

OC([[email protected]](C1=C(C=C(C(O)=O)C=C1)C)N)=O.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (508.83 mM; Need ultrasonic)

H2O : 12.5 mg/mL (50.88 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0707 mL 20.3533 mL 40.7067 mL
5 mM 0.8141 mL 4.0707 mL 8.1413 mL
10 mM 0.4071 mL 2.0353 mL 4.0707 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (8.47 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (8.47 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (8.47 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

LY367385LY 367385LY-367385mGluRMetabotropic glutamate receptorsmGluR1aepilepsyneuroprotectiveexcitotoxicquisqualate-inducedphosphoinositideInhibitorinhibitorinhibit

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Product Name:
LY367385 hydrochloride
Cat. No.:
HY-107515A
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