LY3020371 hydrochloride

Name: LY3020371 hydrochloride
Brand: MedChemExpress
SKU: HY-123820
Rating: 4.5 (1 reviews)

Cat. No.: HY-123820 Purity: 99.13%: FAQs
Data Sheet SDS COA Handling Instructions

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LY3020371 hydrochloride is a potent, selective metabotropic glutamate 2/3 receptor (mGlu2/3) antagonist with K_i 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.

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

LY3020371 hydrochloride Chemical Structure

CAS No. : 1377615-44-5

Size	Price	Stock	Quantity
5 mg	USD 650	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 980	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 3000	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 5000	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of LY3020371 hydrochloride:

LY3020371 Get quote

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mGluR1 mGluR2 mGluR3 mGluR4 mGluR5 mGluR6 mGluR7 mGluR8 mGluR

Biological Activity
Purity & Documentation
References
Customer Review

Description

LY3020371 hydrochloride is a potent, selective metabotropic glutamate 2/3 receptor (mGlu2/3) antagonist with K_i 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

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 K_i=5.26 nM; hmGlu3 K_i=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].

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

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].

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

Molecular Weight

395.81

Formula

C₁₅H₁₆ClF₂NO₅S

CAS No.

1377615-44-5

Appearance

Solid

Color

White to off-white

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.[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 : 250 mg/mL (631.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5265 mL	12.6323 mL	25.2646 mL
5 mM	0.5053 mL	2.5265 mL	5.0529 mL
10 mM	0.2526 mL	1.2632 mL	2.5265 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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 (5.26 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 (5.26 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.26 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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

Purity: 99.13%

Select Batch:

Data Sheet (276 KB) SDS (251 KB)

COA (250 KB) HNMR (284 KB) LCMS (266 KB)

Handling Instructions (2659 KB)

References

[1]. Witkin JM, et al. In vitro pharmacological and rat pharmacokinetic characterization of LY3020371, a potent and selective mGlu2/3 receptor antagonist. Neuropharmacology. 2017 Mar 15;115:100-114. [Content Brief]

[2]. Witkin JM, et al. Preclinical predictors that the orthosteric mGlu2/3 receptor antagonist LY3020371 will not engender ketamine-associated neurotoxic, motor, cognitive, subjective, or abuse-liability-related effects. Pharmacol Biochem Behav. 2017 Apr;155:4 [Content Brief]

[3]. Wood CM, et al. Investigating the role of mGluR2 versus mGluR3 in antipsychotic-like effects, sleep-wake architecture and network oscillatory activity using novel Han Wistar rats lacking mGluR2 expression. Neuropharmacology. 2018 Sep 15;140:246-259. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5265 mL	12.6323 mL	25.2646 mL	63.1616 mL
	5 mM	0.5053 mL	2.5265 mL	5.0529 mL	12.6323 mL
	10 mM	0.2526 mL	1.2632 mL	2.5265 mL	6.3162 mL
	15 mM	0.1684 mL	0.8422 mL	1.6843 mL	4.2108 mL
	20 mM	0.1263 mL	0.6316 mL	1.2632 mL	3.1581 mL
	25 mM	0.1011 mL	0.5053 mL	1.0106 mL	2.5265 mL
	30 mM	0.0842 mL	0.4211 mL	0.8422 mL	2.1054 mL
	40 mM	0.0632 mL	0.3158 mL	0.6316 mL	1.5790 mL
	50 mM	0.0505 mL	0.2526 mL	0.5053 mL	1.2632 mL
	60 mM	0.0421 mL	0.2105 mL	0.4211 mL	1.0527 mL
	80 mM	0.0316 mL	0.1579 mL	0.3158 mL	0.7895 mL
	100 mM	0.0253 mL	0.1263 mL	0.2526 mL	0.6316 mL