LY341495

Name: LY341495
Brand: MedChemExpress
SKU: HY-70059
Rating: 5.0 (14 reviews)

製品番号: HY-70059 純度: 99.17%: Data Sheet SDS COA 取扱説明書
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LY341495 is a metabotropic glutamate receptor (mGluR) antagonist with IC₅₀s of 21 nM, 14 nM, 7.8 μM, 8.2 μM, 170 nM, 990 nM, 22 μM for mGlu2, mGlu3, mGlu1a, mGlu5a, mGlu8, mGlu7, and mGlu4 receptors, respectively.

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CAS 番号 : 201943-63-7

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 121	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 121	在庫あり	Estimated Time of Arrival: December 31
Solid
1 mg	$45	在庫あり	Estimated Time of Arrival: December 31
5 mg	$110	在庫あり	Estimated Time of Arrival: December 31
10 mg	$170	在庫あり	Estimated Time of Arrival: December 31
25 mg	$352	在庫あり	Estimated Time of Arrival: December 31
50 mg	$600	在庫あり	Estimated Time of Arrival: December 31
100 mg	$960	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 14 publication(s) in Google Scholar

Other Forms of LY341495:

(Rac)-LY341495 在庫あり

顧客検証

In Vivo Efficacy Study

IHC

: LY341495 purchased from MedChemExpress. Usage Cited in: Cell Res. 2025 Mar;35(3):165-185. [Abstract]; Representative western blot and quantification of AKT signal in GT1-7 cells treated with 10 ng/ml Raptin and GRM3 agonists (LY354740, LY2794193, LY379268), inhibitors (LY341495) or allosteric agents (VU0650786).

: LY341495 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2020 Feb 28;11:183. [Abstract]; LY341495 (1 mg/kg; IP; 30 min prior to MPTP injection (30 mg/kg/d) once a day for 7 days consecutively) significantly decreased compared with the normal + saline group and a significant longer time-down (TLA) was spent by the MPTP + saline group and MPTP + LY341495 group compared with the normal + saline group (both p < 0.01) and LY354740 + saline group (both p < 0.05).

: LY341495 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2020 Feb 28;11:183. [Abstract]; LY341495 (1 mg/kg; IP; for four times (30 min before each MPTP injection); once a day for 6 days consecutively) showed that latency times in acute MPTP-mice treated with LY341495 (1 mg/kg) significantly decreased, both MPTP + saline group and MPTP + LY341495 group exhibited longer times (Turn) than normal + saline group and MPTP + LY354740 (4 mg/kg) group.

: LY341495 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2020 Feb 28;11:183. [Abstract]; (A, B) Immunohistochemical images and corresponding TH positive cell counts in SN from each group.LY341495 (1 mg/kg; IP; 30 min prior to MPTP injection (30 mg/kg/d) once a day for 7 days consecutively) counted fewer TH-positive cells in sub-acute MPTP-mice treated.

: LY341495 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2020 Feb 28;11:183. [Abstract]; LY341495 (1 mg/kg; IP; 30 min prior to MPTP injection (30 mg/kg/d) once a day for 7 days consecutively) exhibited much higher expressions of p-Fyn Tyr416.

: LY341495 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2020 Feb 28;11:183. [Abstract]; LY341495 (1 mg/kg; IP; 30 min prior to MPTP injection (30 mg/kg/d) once a day for 7 days consecutively) showed an elevation of the number of PLK2 positive cells, indicating increased expression of PLK2. Immunofluorescence of PLK2 positive cell counts in SN.

: LY341495 purchased from MedChemExpress. Usage Cited in: Pain. 2016 Aug;157(8):1711-23. [Abstract]; LY341495 and Sulfasalazine mildly suppress the effects of chronic constrictive injury (CCI)-induced mechanical allodynia and matrix metalloproteinase-9 activity by N-acetyl-cysteine (NAC).

mGluR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

mGluR1 mGluR2 mGluR3 mGluR4 mGluR5 mGluR6 mGluR7 mGluR8 mGluR

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製品説明

IC₅₀ & Target^[5]

mGluR1a

7.8 μM (IC₅₀)

mGluR2

21 nM (IC₅₀)

mGluR3

14 nM (IC₅₀)

mGluR4

22 μM (IC₅₀)

mGluR5a

8.2 μM (IC₅₀)

mGluR7

990 nM (IC₅₀)

mGluR8

170 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	> 100000 1 Compound: 9	Effective concentration for agonistic activity towards metabotropic glutamate receptor 1 of rat expressed in CHO cells Effective concentration for agonistic activity towards metabotropic glutamate receptor 1 of rat expressed in CHO cells	[PMID: 15317467]
CHO	EC₅₀	>100 3 Compound: 9	Effective concentration for agonistic activity towards metabotropic glutamate receptor 1 of rat expressed in CHO cells Effective concentration for agonistic activity towards metabotropic glutamate receptor 1 of rat expressed in CHO cells	[PMID: 15317467]
CHO	IC₅₀	0.2 3 Compound: 7	Antagonistic activity against stimulation of GTP (gamma) 35 S binding by glutamate in membranes from CHO cells expressing human mGluR2 Antagonistic activity against stimulation of GTP (gamma) 35 S binding by glutamate in membranes from CHO cells expressing human mGluR2	[PMID: 11720869]
CHO	EC₅₀	> 100000 1 Compound: 9	Effective concentration for agonistic activity towards metabotropic glutamate receptor 2 of rat expressed in CHO cells Effective concentration for agonistic activity towards metabotropic glutamate receptor 2 of rat expressed in CHO cells	[PMID: 15317467]
CHO	IC₅₀	0.2 3 Compound: 7	Antagonistic activity against stimulation of GTP (gamma) 35 S binding by glutamate in membranes from CHO cells expressing human mGluR2 Antagonistic activity against stimulation of GTP (gamma) 35 S binding by glutamate in membranes from CHO cells expressing human mGluR2	[PMID: 11720869]
CHO	EC₅₀	> 100000 1 Compound: 9	Effective concentration for agonistic activity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells Effective concentration for agonistic activity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells	[PMID: 15317467]
CHO	IC₅₀	2.9 1 Compound: 1, LY-341495	Displacement of [3H]-MGS0008 from mGluR2 expressed in CHO cells Displacement of [3H]-MGS0008 from mGluR2 expressed in CHO cells	[PMID: 18348906]
CHO	EC₅₀	> 100000 1 Compound: 9	Effective concentration for agonistic activity towards metabotropic glutamate receptor 5 of rat expressed in CHO cells Effective concentration for agonistic activity towards metabotropic glutamate receptor 5 of rat expressed in CHO cells	[PMID: 15317467]
HEK293	IC₅₀	0.016 3 Compound: 7	Compound was evaluated for the inhibition of binding of [3H]glutamate against rat recombinant mGluR3 receptors expressed in HEK293 cells Compound was evaluated for the inhibition of binding of [3H]glutamate against rat recombinant mGluR3 receptors expressed in HEK293 cells	[PMID: 11720869]
CHO	EC₅₀	> 100000 1 Compound: 9	Effective concentration for agonistic activity towards metabotropic glutamate receptor 6 of rat expressed in CHO cells Effective concentration for agonistic activity towards metabotropic glutamate receptor 6 of rat expressed in CHO cells	[PMID: 15317467]
CHO	IC₅₀	14.2 1 Compound: 9	Concentration required to inhibit metabotropic glutamate receptor 3 activity of rat expressed in CHO cells Concentration required to inhibit metabotropic glutamate receptor 3 activity of rat expressed in CHO cells	[PMID: 15317467]
CHO	IC₅₀	0.2 3 Compound: 7	Antagonistic activity against stimulation of GTP (gamma) 35 S binding by glutamate in membranes from CHO cells expressing human mGluR2 Antagonistic activity against stimulation of GTP (gamma) 35 S binding by glutamate in membranes from CHO cells expressing human mGluR2	[PMID: 11720869]
CHO	IC₅₀	23.2 1 Compound: 9	Concentration required to inhibit metabotropic glutamate receptor 2 activity of rat expressed in CHO cells Concentration required to inhibit metabotropic glutamate receptor 2 activity of rat expressed in CHO cells	[PMID: 15317467]
CHO	IC₅₀	1140 1 Compound: 9	Concentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cells Concentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cells	[PMID: 15317467]
CHO	IC₅₀	1140 1 Compound: 9	Concentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cells Concentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cells	[PMID: 15317467]
CHO	IC₅₀	11400 1 Compound: 9	Concentration required to inhibit metabotropic glutamate receptor 5 activity of rat expressed in CHO cells Concentration required to inhibit metabotropic glutamate receptor 5 activity of rat expressed in CHO cells	[PMID: 15317467]
CHO	IC₅₀	2650 1 Compound: 9	Concentration required to inhibit metabotropic glutamate receptor 4 activity of rat expressed in CHO cells Concentration required to inhibit metabotropic glutamate receptor 4 activity of rat expressed in CHO cells	[PMID: 15317467]
CHO	IC₅₀	8990 1 Compound: 9	Concentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cells Concentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cells	[PMID: 15317467]
CHO	IC₅₀	14.2 1 Compound: 9	Concentration required to inhibit metabotropic glutamate receptor 3 activity of rat expressed in CHO cells Concentration required to inhibit metabotropic glutamate receptor 3 activity of rat expressed in CHO cells	[PMID: 15317467]
CHO	IC₅₀	11400 1 Compound: 9	Concentration required to inhibit metabotropic glutamate receptor 5 activity of rat expressed in CHO cells Concentration required to inhibit metabotropic glutamate receptor 5 activity of rat expressed in CHO cells	[PMID: 15317467]
CHO	IC₅₀	2.9 1 Compound: 1, LY-341495	Displacement of [3H]-MGS0008 from mGluR2 expressed in CHO cells Displacement of [3H]-MGS0008 from mGluR2 expressed in CHO cells	[PMID: 18348906]
CHO	IC₅₀	23.2 1 Compound: 9	Concentration required to inhibit metabotropic glutamate receptor 2 activity of rat expressed in CHO cells Concentration required to inhibit metabotropic glutamate receptor 2 activity of rat expressed in CHO cells	[PMID: 15317467]
CHO	IC₅₀	2650 1 Compound: 9	Concentration required to inhibit metabotropic glutamate receptor 4 activity of rat expressed in CHO cells Concentration required to inhibit metabotropic glutamate receptor 4 activity of rat expressed in CHO cells	[PMID: 15317467]
CHO	IC₅₀	8990 1 Compound: 9	Concentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cells Concentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cells	[PMID: 15317467]
HEK293	IC₅₀	0.016 3 Compound: 7	Compound was evaluated for the inhibition of binding of [3H]glutamate against rat recombinant mGluR3 receptors expressed in HEK293 cells Compound was evaluated for the inhibition of binding of [3H]glutamate against rat recombinant mGluR3 receptors expressed in HEK293 cells	[PMID: 11720869]

体内実験

LY341495 (0.3, 1, and 3 mg/kg, i.p.) displays a lower level of discrimination in rats^[1]. LY341495 (3.0 mg/kg) decreases Dvl-2, pGSK-3α/β and β-catenin protein levels but Dvl-1, Dvl-3 and GSK-3α/β are unaffected in both the PFC and STR. LY341495 has the generally the opposite effect following acute and chronic administration compared to mGlu2/3 agonist, LY379268^[2]. LY341495 (3 mg/kg, i.p., 2.5 h) -induced c-Fos expression is not altered in either KO brain. LY341495 is almost inactive in the central extended amygdala [central nucleus of the amygdala, lateral (CeL) and bed nucleus of the stria terminalis, laterodorsal (BSTLD)] in mGluR3-KO mice^[3].

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

分子量

353.37

分子式

C₂₀H₁₉NO₅

CAS 番号

201943-63-7

Appearance

Solid

Color

White to off-white

SMILES

O=C(O)[C@@H]1[C@H](C1)[C@@](N)(CC2C3=C(C=CC=C3)OC4=C2C=CC=C4)C(O)=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

DMSO : 6 mg/mL (16.98 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	2.8299 mL	14.1495 mL	28.2990 mL
5 mM	0.5660 mL	2.8299 mL	5.6598 mL
10 mM	0.2830 mL	1.4149 mL	2.8299 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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 90% Corn Oil
Solubility: ≥ 0.6 mg/mL (1.70 mM); Clear solution

This protocol yields a clear solution of ≥ 0.6 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 (6.0 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).

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.

純度とドキュメンテーション

純度: 99.96%

Select Batch:

データシート (281 KB) SDS (393 KB)

COA (255 KB) RP-HPLC (248 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Pitsikas N, et al. The metabotropic glutamate 2/3 receptor antagonist LY341495 differentially affects recognition memory in rats. Behav Brain Res. 2012 May 1;230(2):374-9. [Content Brief]

[2]. Sutton LP, et al. Regulation of Akt and Wnt signaling by the group II metabotropic glutamate receptor antagonist LY341495 and agonist LY379268.J Neurochem. 2011 Jun;117(6):973-83. [Content Brief]

[3]. Linden AM, et al. Use of MGLUR2 and MGLUR3 knockout mice to explore in vivo receptor specificity of the MGLUR2/3 selective antagonist LY341495. Neuropharmacology. 2009 Aug;57(2):172-82. Epub 2009 May 27. [Content Brief]

[4]. Li J, et al. N-acetyl-cysteine attenuates neuropathic pain by suppressing matrix metalloproteinases. Pain. 2016 Aug;157(8):1711-23. [Content Brief]

[5]. A E Kingston, et al. LY341495 Is a Nanomolar Potent and Selective Antagonist of Group II Metabotropic Glutamate Receptors.Neuropharmacology. 1998;37(1):1-12. [Content Brief]

動物実験
^[1]

The rats are randomLy divided into six experimental groups (10 rats per group): vehicle and 0.05, 0.1, 0.3, 1, and 3 mg/kg LY341495. The LY341495 doses are selected on the basis of results from previous Published studies that evaluated the effects of this compound on cognition. The rats are subjected to a training session that consisted of two 2-min trials. The animals receive either vehicle or LY341495 immediately after T1. Using the 2-min trial duration, an ITI of 1 h is used because recognition memory is still intact in untreated control rats under these experimental conditions

MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。

参考文献

[1]. Pitsikas N, et al. The metabotropic glutamate 2/3 receptor antagonist LY341495 differentially affects recognition memory in rats. Behav Brain Res. 2012 May 1;230(2):374-9. [Content Brief]

[2]. Sutton LP, et al. Regulation of Akt and Wnt signaling by the group II metabotropic glutamate receptor antagonist LY341495 and agonist LY379268.J Neurochem. 2011 Jun;117(6):973-83. [Content Brief]

[3]. Linden AM, et al. Use of MGLUR2 and MGLUR3 knockout mice to explore in vivo receptor specificity of the MGLUR2/3 selective antagonist LY341495. Neuropharmacology. 2009 Aug;57(2):172-82. Epub 2009 May 27. [Content Brief]

[4]. Li J, et al. N-acetyl-cysteine attenuates neuropathic pain by suppressing matrix metalloproteinases. Pain. 2016 Aug;157(8):1711-23. [Content Brief]

[5]. A E Kingston, et al. LY341495 Is a Nanomolar Potent and Selective Antagonist of Group II Metabotropic Glutamate Receptors.Neuropharmacology. 1998;37(1):1-12. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.8299 mL	14.1495 mL	28.2990 mL	70.7474 mL
	5 mM	0.5660 mL	2.8299 mL	5.6598 mL	14.1495 mL
	10 mM	0.2830 mL	1.4149 mL	2.8299 mL	7.0747 mL
	15 mM	0.1887 mL	0.9433 mL	1.8866 mL	4.7165 mL

LY341495 Related Classifications

Neurological Disease

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

Help & FAQs

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.

Keywords:

LY341495201943-63-7LY 341495LY-341495mGluRMetabotropic glutamate receptorsInhibitorinhibitorinhibit

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LY341495

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参考文献

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Molarity Calculator

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Complete Stock Solution Preparation Table

LY341495 Related Classifications

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