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SML2269

LY404039

≥98% (HPLC)

Synonym(s):

(1R,4S,5S,6S)-4-Amino-2-thiabicyclo[3.1.0]hexane-4,6-dicarboxylic acid 2,2-dioxide, (–)-(1R,4S,5S,6S)-4-Amino-2-sulfonylbicyclo[3.1.0]hexane-4,6-dicarboxylic acid, LY 404039, LY-404,039, LY-404039

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Pack SizeSKUAvailabilityPrice
25 mg

Available to ship TODAYfromMILWAUKEE

$395.00

About This Item

Empirical Formula (Hill Notation):
C7H9NO6S
CAS Number:
635318-11-5
Molecular Weight:
235.21
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD11974011
Assay:
≥98% (HPLC)
Form:
powder

$395.00

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assay

≥98% (HPLC)

form

powder

optical activity

[α]/D -69 to -79°, c = 1.0 in 1 M NaOH

color

white to gray

solubility

DMSO: 2 mg/mL, clear (warmed)

storage temp.

−20°C

SMILES string

[H][C@]1([C@@](C(O)=O)(N)C2)[C@@]([C@@H]1C(O)=O)([H])S2(=O)=O

InChI

1S/C7H9NO6S/c8-7(6(11)12)1-15(13,14)4-2(3(4)7)5(9)10/h2-4H,1,8H2,(H,9,10)(H,11,12)/t2-,3-,4+,7+/m1/s1

InChI key

AVDUGNCTZRCAHH-MDASVERJSA-N

Biochem/physiol Actions

LY404039 is a potent and selective group II metabotropic glutamate receptors mGluR2/3 agonist (Ki = 15 nM against against [3H]LY341495 for binding rat neurons; Ki = 149 nM and 92 nM, respectively, using membrane from human mGluR2- or mGluR3-expressing cells) with >100-fold selectivity over 16 other receptors/transproters, including iGluRs and EAAT1/2/3. LY404039 inhibits forskolin-stimulated c-AMP production in RGT cells expressing human mGluR2 (EC50 = 23 nM) or mGluR3 (EC50 = 48 nM) with little or no potency toward mGluR1a/5a/4a/6/7a/8a-expressing cells (EC50 >10 μM). LY404039 is orally available (Cmax 1528.5 ng/mL, Tmax 2 h; 10 mg/kg p.o. in rats) and exhibits antipsychotic and anxiolytic efficacy in rats (3-30 mg/kg) in vivo.
Orally available, potent and selective metabotropic glutamate receptors mGluR2 & mGluR3 agonist with antipsychotic and anxiolytic efficacy in vivo.

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LY404039 ≥98% (HPLC)

Sigma-Aldrich

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LY-354740 hydrate ≥98% (HPLC)

Sigma-Aldrich

L1045

LY-354740 hydrate

Dorzolamide ≥98% (HPLC)

Sigma-Aldrich

SML0468

Dorzolamide

BI-2545 ≥98% (HPLC)

Sigma-Aldrich

SML2255

BI-2545

form

powder

form

solid

form

powder

form

powder

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

storage temp.

−20°C

storage temp.

room temp

storage temp.

room temp

storage temp.

2-8°C

solubility

DMSO: 2 mg/mL, clear (warmed)

solubility

deionized water: 8 mg/mL

solubility

DMSO: 5 mg/mL (clear solution, warmed)

solubility

DMSO: 2 mg/mL, clear

color

white to gray

color

-

color

white to beige

color

white to beige

optical activity

[α]/D -69 to -79°, c = 1.0 in 1 M NaOH

optical activity

-

optical activity

[α]/D -25 to -35°, c = 1 in methanol

optical activity

-

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000193031
0000193031
0000045211
0000045212
0000036700

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Shingo Suzuki et al.
Peptides, 89, 42-49 (2017-01-26)
Accumulating evidence suggests functional interaction between brain-derived neurotrophic factor (BDNF) and metabotropic glutamate receptor (mGluR) signaling pathways in the central nervous system (CNS). To date, eight subtypes of mGluRs, mGluR1-8, have been identified, and a previous study suggested that BDNF
Guy Griebel et al.
Scientific reports, 6, 35320-35320 (2016-10-14)
Normalization of altered glutamate neurotransmission through activation of the mGluR2 has emerged as a new approach to treat schizophrenia. These studies describe a potent brain penetrant mGluR2 positive allosteric modulator (PAM), SAR218645. The compound behaves as a selective PAM of
Linda M Rorick-Kehn et al.
Psychopharmacology, 193(1), 121-136 (2007-03-27)
Data from both preclinical and clinical studies have provided proof of concept that modulation of limbic and forebrain glutamate, via mGlu2/3 receptor agonists, might provide therapeutic benefits in many psychiatric disorders including schizophrenia and anxiety. The aim of this study
View All Related Papers

Global Trade Item Number

SKUGTIN
SML2269-5MG04061835255108
SML2269-25MG04061835255092

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