5.04466

LY-404,039

• Synonym(s): LY-404,039, (1R,4S,5S,6S)-4-[[(2S)-2-Amino-4-(methylthio)-1-oxobutyl]amino]-2-thiabicyclo[3.1.0]hexane-4,6-dicarboxylic acid 2,2-dioxide
• Empirical Formula (Hill Notation): C₇H₉NO₆S
• CAS Number: 635318-55-7
• Molecular Weight: 235.21
• UNSPSC Code: 12352200

Properties

• assay: ≥98% (NMR)
• Quality Level: 100
• form: powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 0.25 mg/mL; dilute NaOH: 10 mg/mL
• storage temp.: −20°C
• InChI: 1S/C12H18N2O7S2/c1-22-3-2-5(13)9(15)14-12(11(18)19)4-23(20,21)8-6(7(8)12)10(16)17/h5-8H,2-4,13H2,1H3,(H,14,15)(H,16,17)(H,18,19)/t5-,6+,7+,8-,12+/m0/s1
• InChI key: VOYCNOJFAJAILW-OZFRBSTCSA-N

Description

General description

A highly selective and potent agonist for recombinant human mGlu₂ and mGlu₃ receptors (K_i = 149 nM and 92 nM, respectively) and for rat neurons mGlu_2/3 receptors (K_i = 88 nM). Negligible interactions with other mGlu receptors and ionotropic glutamate receptors, glutamate transporter subtypes, monoamine and other receptors. Widely used for investigating neuropsychiatric disorders in animal models and developing potential treatment for human mental disorders, such as schizophrenia.

Biochem/physiol Actions

Primary Target
mGlu₂ & mGlu₃

Target K_i: 149 nM and 92 nM for human mGlu₂ and mGlu₃, respectively.

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C. Stock solutions are stable for up to 3 months ta -20°C.

Other Notes

Seeman, P., 2013. Neuropharmacology.66, 87.
Rorick-Kehn, L., et al. 2007. J. Pharmacol. Exp. Ther.321, 308.
Fell, M., et al. 2008. J. Pharmacol. Exp. Ther.326, 209.
Rodd, Z., et al. 2006. Behav. Brain Res.171, 207.
Mezler, M., et al. 2010. Curr. Opi. In Investigational Drugs.11, 833.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable