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Signaling Pathway

LY341495

HY-70059

(LY 341495; LY-341495)

LY341495

LY341495 Chemical Structure

LY341495 is a highly potent and selective group II metabotropic glutamate receptor antagonist. (Ki/IC50 values are 2.3, 1.3, 173, 990, 6800, 8200 and 22000 nM for human mGlu2, mGlu3, mGlu8 , mGlu7a, mGlu1a, mGlu5a and mGlu4a receptors respectively).

Size Price Stock Quantity
10 mM * 1 mL in DMSO $85 In-stock
5 mg $77 In-stock
10 mg $132 In-stock
50 mg $495 In-stock
100 mg Get quote
200 mg Get quote
Size Price Stock Quantity
10 mM * 1 mL in DMSO €83 In-stock
5 mg €75 In-stock
10 mg €129 In-stock
50 mg €485 In-stock
100 mg Get quote
200 mg Get quote

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Product name: LY341495
Cat. No.: HY-70059

LY341495 Data Sheet

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    Purity: 99.50%

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    DataSheet

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    MSDS

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    COA

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Biological Activity of LY341495

LY341495 is a highly potent and selective group II metabotropic glutamate receptor antagonist. (Ki/IC50 values are 2.3, 1.3, 173, 990, 6800, 8200 and 22000 nM for human mGlu2, mGlu3, mGlu8 , mGlu7a, mGlu1a, mGlu5a and mGlu4a receptors respectively).
IC50 Value: 2.9 nM (for  mGluR-2, human); 10 nM (for mGluR-3, human); 170 nM (for mGluR-8, huma)[1]
Target: mGluR
in vitro: LY341495 was micromolar potent in antagonizing quisqualate-induced phosphoinositide (PI) hydrolysis, with IC50 values of 7.8 and 8.2 microM for mGlu1a and mGlu5a receptors, respectively. Among the human group III mGlu receptors, the most potent inhibition of L-2-amino-4-phosphonobutyric acid (L-AP4) responses was seen for LY341495 at mGlu8, with an IC50 of 0.17 microM. LY341495 was less potent at mGlu7 (IC50 = 0.99 microM) and least potent at mGlu4 (IC50 = 22 microM).  LY341495 competitively antagonised DHPG-stimulated PI hydrolysis in AV12-664 cells expressing either human mGlu1 or mGlu5 receptors with Ki-values of 7.0 and 7.6 microM, respectively.
in vivo: LY341495 (3 mg/kg, i.p., 2.5 h) -induced c-Fos expression was not altered in either KO brain. However, in mGluR3-KO mice, LY341495 was almost inactive in the central extended amygdala [central nucleus of the amygdala, lateral (CeL) and bed nucleus of the stria terminalis, laterodorsal (BSTLD)].
 

Protocol (Extracted from published papers and Only for reference)

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Chemical Information

M.Wt 353.37 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C20H19NO5
CAS No 201943-63-7
Solvent & Solubility

10 mM in DMSO

Preparing Stock Solutions

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

References on LY341495

Inhibitor Kit

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