LY456066
Based on 1 Customer Validation
LY456066 is a selective non-competitive metabotropic glutamate receptors (mGluR1) antagonist with an IC50 value of 52.0 nM. LY456066 is effective in rodent models of anxiolysis and nociception. LY456066 reduces hyperalgesia and the amount of licking and flinching following formalin injection, which is promising for research of analgesics for chronic pain.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.0%
- No. CAS: 338738-66-2
- Fòrmula: C19H23N3OS
- Peso molecular:341.47
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Almacenamiento:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
>9100 nM
Compound: 4; LY456066
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Negative allosteric modulation activity at recombinant human mGluR5a expressed in CHO cells assessed as inhibition of L-glutamate-induced intracellular Ca2+ mobilization
Negative allosteric modulation activity at recombinant human mGluR5a expressed in CHO cells assessed as inhibition of L-glutamate-induced intracellular Ca2+ mobilization
|
[PMID: 26988308] |
| CHO | IC50 |
28 nM
Compound: 4; LY456066
|
Negative allosteric modulation activity at recombinant human mGluR1a expressed in CHO cells assessed as inhibition of L-glutamate-induced intracellular Ca2+ mobilization
Negative allosteric modulation activity at recombinant human mGluR1a expressed in CHO cells assessed as inhibition of L-glutamate-induced intracellular Ca2+ mobilization
|
[PMID: 26988308] |
Chemical Information
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No. CAS 338738-66-2
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Appearance Solid
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Peso molecular 341.47
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Fòrmula C19H23N3OS
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Color White to off-white
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SMILES
OCCSC1=NC(NC2CC3=C(C2)C=CC=C3)=C4CCCCC4=N1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Pureza y Documentación
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Ficha de datos (269 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. El-Kouhen O, et al. Blockade of mGluR1 receptor results in analgesia and disruption of motor and cognitive performances: effects of A-841720, a novel non-competitive mGluR1 receptor antagonist. Br J Pharmacol. 2006 Nov;149(6):761-74. [Content Brief]
[2]. Varty GB, et al. The antinociceptive and anxiolytic-like effects of the metabotropic glutamate receptor 5 (mGluR5) antagonists, MPEP and MTEP, and the mGluR1 antagonist, LY456236, in rodents: a comparison of efficacy and side-effect profiles. Psychopharmacology (Berl). 2005 Apr;179(1):207-17. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)