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LY 354740 - ≥98%, high purity , CAS No.176199-48-7, Agonist of mGlu 2 receptor;Agonist of mGlu 3 receptor;Agonist of mGlu 6 receptor;Agonist of mGlu 8 receptor

  • Moligand™
  • ≥98%
Item Number
L275282
Grouped product items
SKUSizeAvailabilityPrice Qty
L275282-10mg
10mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$155.90
L275282-50mg
50mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$652.90

Group II mGlu agonist. Systemically active.

Basic Description

SynonymsEglumegad|176199-48-7|Eglumetad|(1S,2S,5R,6S)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid|LY354740|LY 354740|LY-354740|(rel)-Eglumegad|LY 354740 Hydrate|Eglumetad anhydrous|(1S,2S,5R,6S)-2-Aminobicyclo(3.1.0)hexane-2,6-dicarboxylic acid|CHEMBL8759|O
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsHighly potent and selective agonist at mGlu 2 and mGlu 3 receptors (EC 50 values are 5.1 and 24.3 nM, respectively). Displays no agonist or antagonist activity at mGlu 1 a, mGlu 5a , mGlu 4 or mGlu 7 receptors at concentrations up to 100 μM.
Storage TempStore at 2-8°C,Desiccated
Shipped InWet ice
GradeMoligand™
Action TypeAGONIST
Mechanism of actionAgonist of mGlu 2 receptor;Agonist of mGlu 3 receptor;Agonist of mGlu 6 receptor;Agonist of mGlu 8 receptor
NoteWherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

Store at +4°C. Store under desiccating conditions. The product can be stored for up to 12 months.

Associated Targets

CX3CR1 Tchem CX3C chemokine receptor 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GPR35 Tchem G-protein coupled receptor 35 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BRD4 Tchem Bromodomain-containing protein 4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK2 Tchem Cyclin-dependent kinase 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FFAR4 Tchem Free fatty acid receptor 4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HDAC6 Tclin Histone deacetylase 6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FPR2 Tchem N-formyl peptide receptor 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FGFR3 Tclin Fibroblast growth factor receptor 3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CSNK1D Tchem Casein kinase I isoform delta 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

S1PR1 Tclin Sphingosine 1-phosphate receptor 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TRIM24 Tchem Transcription intermediary factor 1-alpha 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

C5AR1 Tclin C5a anaphylatoxin chemotactic receptor 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BRPF1 Tchem Peregrin 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AURKA Tchem Aurora kinase A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADRB2 Tclin Beta-2 adrenergic receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

APLNR Tchem Apelin receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ABL1 Tclin Tyrosine-protein kinase ABL1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADRA2A Tclin Alpha-2A adrenergic receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADGRF1 Tbio Adhesion G-protein coupled receptor F1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AGTR1 Tclin Type-1 angiotensin II receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GRM1 Tchem Metabotropic glutamate receptor 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GSK3B Tclin Glycogen synthase kinase-3 beta 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GRIA3 Tclin Glutamate receptor 3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GRIK2 Tclin Glutamate receptor ionotropic, kainate 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GRM2 Tchem Metabotropic glutamate receptor 2 19 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GRM4 Tchem Metabotropic glutamate receptor 4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GRM5 Tchem Metabotropic glutamate receptor 5 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GRM7 Tchem Metabotropic glutamate receptor 7 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GRM8 Tchem Metabotropic glutamate receptor 8 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GPR119 Tclin Glucose-dependent insulinotropic receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GRM3 Tchem Metabotropic glutamate receptor 3 14 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GRM6 Tchem Metabotropic glutamate receptor 6 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GLP1R Tclin Glucagon-like peptide 1 receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GRIN3A Tclin Glutamate receptor ionotropic, NMDA 3A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAPK1 Tchem Mitogen-activated protein kinase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name (1S,2S,5R,6S)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid
INCHI InChI=1S/C8H11NO4/c9-8(7(12)13)2-1-3-4(5(3)8)6(10)11/h3-5H,1-2,9H2,(H,10,11)(H,12,13)/t3-,4-,5-,8-/m0/s1
InChi Key VTAARTQTOOYTES-RGDLXGNYSA-N
Canonical SMILES C1CC(C2C1C2C(=O)O)(C(=O)O)N
Isomeric SMILES C1C[C@]([C@H]2[C@@H]1[C@@H]2C(=O)O)(C(=O)O)N
Alternate CAS 176199-48-7
PubChem CID 213056
MeSH Entry Terms (+)-(1S,2S,5R,6S)-2-aminobicyclo(3.1.0)hexane-2,6-dicarboxylic acid;2-aminobicyclo(3.1.0)hexane-2,6-dicarboxylic acid;eglumetad;LY 314582;LY 354740;LY 366563;LY-314582;LY-354740;LY-366563;LY314582;LY354740;LY366563
Molecular Weight 185.18

Certificates

Certificate of Analysis(COA)

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Chemical and Physical Properties

SolubilitySoluble in 1 eq. NaOH to 100 mM

Related Documents

References

1. Kłodzińska A, Chojnacka-Wójcik E, Pałucha A, Brański P, Popik P, Pilc A.  (1999)  Potential anti-anxiety, anti-addictive effects of LY 354740, a selective group II glutamate metabotropic receptors agonist in animal models..  Neuropharmacology,  38  (12): (1831-9).  [PMID:10608278]
2. Pilc A.  (2003)  LY-354740 (Eli Lilly)..  IDrugs,  (1): (66-71).  [PMID:12789623]
3. Dunayevich E, Erickson J, Levine L, Landbloom R, Schoepp DD, Tollefson GD.  (2008)  Efficacy and tolerability of an mGlu2/3 agonist in the treatment of generalized anxiety disorder..  Neuropsychopharmacology,  33  (7): (1603-10).  [PMID:17712352]
4. Schoepp DD, Johnson BG, Wright RA, Salhoff CR, Mayne NG, Wu S, Cockerman SL, Burnett JP, Belegaje R, Bleakman D et al..  (1997)  LY354740 is a potent and highly selective group II metabotropic glutamate receptor agonist in cells expressing human glutamate receptors..  Neuropharmacology,  36  (1): (1-11).  [PMID:9144636]
5. Bond A, Monn JA, Lodge D.  (1997)  A novel orally active group 2 metabotropic glutamate receptor agonist: LY354740..  Neuroreport,  (6): (1463-6).  [PMID:9172154]
6. Procaccini C et al..  (2013)  Reversal of novelty-induced hyperlocomotion and hippocampal c-Fos expression in GluA1 knockout male mice by the mGluR2/3 agonist LY354740..  Neuroscience,  250  (189-200).  [PMID:23867766]

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