LY404039
Based on 2 publication(s) in Google Scholar
LY404039 is a potent, selective and orally active mGluR2 and mGluR3 agonist with Kis of 149 nM and 92 nM for recombinant human mGluR2 and mGluR3, respectively. LY404039 shows >100-fold selectivity for mGluR2/3 over other receptors/transproters. LY404039 has antipsychotic and anxiolytic effects.
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- Purity: 98.0%
- CAS No.: 635318-11-5
- 화학식: C7H9NO6S
- 분자량:235.21
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) LY404039
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Biological Activity
제품 설명
IC50 & Target
[1]|
mGlu2 Receptor 149 nM (Ki, Recombinant human mGluR2) |
hmGluR3 92 nM (Ki) |
In Vitro
LY404039 is a nanomolar potent agonist in rat neurons expressing native mGlu2/3 receptors (Ki = 88 nM)[1].
Functionally, LY404039 potently inhibits Forskolin-stimulated cAMP formation in cells expressing human mGlu2 (EC50 = 23 nM) and mGlu3 receptors (EC50 = 48 nM)[1].
Electrophysiological studies indicate that LY404039 suppresses electrically evoked excitatory activity in the striatum, and serotonin-induced L-glutamate release in the prefrontal cortex. LY404039 suppresses the frequency of 5-HT-induced excitatory postsynaptic currents (EPSCs) with an EC50 of 82.3 nM and with a near maximal suppression of 85.6% at 1 μM[1].
LY404039 inhibits the binding of the D2-specific antagonist, [3H]domperidone, to the human cloned D2 receptor with dissociation constants of 8.2 nM at D2High and 1640 nM at D2Low. Using rat striatal tissue, LY404039 has dissociation constants of 12.6 nM at D2High and 2100 nM at D2Low[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Following oral administration of LY404039 to fasted rats at doses of 1, 3, or 10 mg/kg, exposure increased proportionally with dose. LY404039 (10 mg/kg; p.o.) treatment shows the Cmax is 1528.5 ng/mL and Tmax is 2 hours in rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 635318-11-5
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Appearance Solid
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분자량 235.21
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화학식 C7H9NO6S
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Color White to gray
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SMILES
O=C([C@]1(N)CS([C@@]2([H])[C@H](C(O)=O)[C@@]12[H])(=O)=O)O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Pharmacol Biochem Behav
Anxiolytic-like effects of an mGluR 5 antagonist and a mGluR 2/3 agonist, and antidepressant-like effects of an mGluR 7 agonist in the chick social separation stress test, a dual-drug screening model of treatment-resistant depression. [Abstract]2023 Jun:227-228:173588. PMID: 37348610 -
용액&용해도
In Vitro:
0.5 M NaOH : 50 mg/mL (212.58 mM; ultrasonic and warming and heat to 60°C)
H2O : 5.2 mg/mL (22.11 mM; ultrasonic and adjust pH to 6 with NaOH)
DMSO : 3.84 mg/mL (16.33 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.
Add each solvent one by one: PBS
Solubility: 2 mg/mL (8.50 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
순도&문서
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Data Sheet (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Linda M Rorick-Kehn, et al. Pharmacological and pharmacokinetic properties of a structurally novel, potent, and selective metabotropic glutamate 2/3 receptor agonist: in vitro characterization of agonist (-)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3.1.0]-hexane-4,6-dicarboxylic acid (LY404039). J Pharmacol Exp Ther. 2007 Apr;321(1):308-17. [Content Brief]
[2]. Seeman P. An agonist at glutamate and dopamine D2 receptors, LY404039. Neuropharmacology. 2013 Mar;66:87-8. [Content Brief]
[3]. Rorick-Kehn LM, et al. In vivo pharmacological characterization of the structurally novel, potent, selective mGlu2/3 receptor agonistLY404039 in animal models of psychiatric disorders. Psychopharmacology (Berl). 2007 Jul;193(1):121-36. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O / 0.5 M NaOH | 1 mM | 4.2515 mL | 21.2576 mL | 42.5152 mL | 106.2880 mL |
| 5 mM | 0.8503 mL | 4.2515 mL | 8.5030 mL | 21.2576 mL | |
| 10 mM | 0.4252 mL | 2.1258 mL | 4.2515 mL | 10.6288 mL | |
| 15 mM | 0.2834 mL | 1.4172 mL | 2.8343 mL | 7.0859 mL | |
| H2O / 0.5 M NaOH | 20 mM | 0.2126 mL | 1.0629 mL | 2.1258 mL | 5.3144 mL |
| 0.5 M NaOH | 25 mM | 0.1701 mL | 0.8503 mL | 1.7006 mL | 4.2515 mL |
| 30 mM | 0.1417 mL | 0.7086 mL | 1.4172 mL | 3.5429 mL | |
| 40 mM | 0.1063 mL | 0.5314 mL | 1.0629 mL | 2.6572 mL | |
| 50 mM | 0.0850 mL | 0.4252 mL | 0.8503 mL | 2.1258 mL | |
| 60 mM | 0.0709 mL | 0.3543 mL | 0.7086 mL | 1.7715 mL | |
| 80 mM | 0.0531 mL | 0.2657 mL | 0.5314 mL | 1.3286 mL | |
| 100 mM | 0.0425 mL | 0.2126 mL | 0.4252 mL | 1.0629 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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