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

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

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LY367385 hydrochloride Chemical Structure

LY367385 hydrochloride Chemical Structure

CAS No. : 2829282-00-8

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10 mM * 1 mL in DMSO
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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 inhibiting 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].

MedChemExpress (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].

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

Molecular Weight

245.66

Formula

C10H12ClNO4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (508.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 50 mg/mL (203.53 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 4.0707 mL 20.3533 mL 40.7067 mL 101.7667 mL
5 mM 0.8141 mL 4.0707 mL 8.1413 mL 20.3533 mL
10 mM 0.4071 mL 2.0353 mL 4.0707 mL 10.1767 mL
15 mM 0.2714 mL 1.3569 mL 2.7138 mL 6.7844 mL
20 mM 0.2035 mL 1.0177 mL 2.0353 mL 5.0883 mL
25 mM 0.1628 mL 0.8141 mL 1.6283 mL 4.0707 mL
30 mM 0.1357 mL 0.6784 mL 1.3569 mL 3.3922 mL
40 mM 0.1018 mL 0.5088 mL 1.0177 mL 2.5442 mL
50 mM 0.0814 mL 0.4071 mL 0.8141 mL 2.0353 mL
DMSO 60 mM 0.0678 mL 0.3392 mL 0.6784 mL 1.6961 mL
80 mM 0.0509 mL 0.2544 mL 0.5088 mL 1.2721 mL
100 mM 0.0407 mL 0.2035 mL 0.4071 mL 1.0177 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • 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.

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LY367385 hydrochloride
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