rel-ACPT-I
Based on 1 Customer Validation
rel-ACPT-I is an agonist of group III mGluRs with diverse biological activities including neuroprotective, anticonvulsant, and anxiolytic-like effects.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.0%
- CAS. Nr.: 194918-76-8
- Formel: C8H11NO6
- Molecular Weight:217.18
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Speicherung:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
<100 μM
Compound: 6
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Stimulation of [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells; Active
Stimulation of [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells; Active
|
[PMID: 15801843] |
| HEK293 | EC50 |
>1000 μM
Compound: ACPT-I
|
Activity at rat mGluR5 receptor measured as intracellular calcium concentration in HEK293 cells
Activity at rat mGluR5 receptor measured as intracellular calcium concentration in HEK293 cells
|
[PMID: 16828551] |
| HEK293 | EC50 |
10.1 μM
Compound: ACPT-I
|
Activity at rat mGluR8 receptor measured as intracellular calcium concentration in HEK293 cells
Activity at rat mGluR8 receptor measured as intracellular calcium concentration in HEK293 cells
|
[PMID: 16828551] |
| HEK293 | EC50 |
1200 μM
Compound: ACPT-I
|
Activity at rat mGluR7 receptor measured as intracellular calcium concentration in HEK293 cells
Activity at rat mGluR7 receptor measured as intracellular calcium concentration in HEK293 cells
|
[PMID: 16828551] |
| HEK293 | EC50 |
18.4 μM
Compound: ACPT-I
|
Activity at rat mGluR6 receptor measured as intracellular calcium concentration in HEK293 cells
Activity at rat mGluR6 receptor measured as intracellular calcium concentration in HEK293 cells
|
[PMID: 16828551] |
| HEK293 | EC50 |
7.2 μM
Compound: ACPT-I
|
Activity at rat mGluR4 receptor measured as intracellular calcium concentration in HEK293 cells
Activity at rat mGluR4 receptor measured as intracellular calcium concentration in HEK293 cells
|
[PMID: 16828551] |
| HEK293 | EC50 |
>1000 μM
Compound: ACPT-I
|
Activity at rat mGluR2 receptor measured as intracellular calcium concentration in HEK293 cells
Activity at rat mGluR2 receptor measured as intracellular calcium concentration in HEK293 cells
|
[PMID: 16828551] |
| HEK293 | EC50 |
1.74 μM
Compound: ACPT-I
|
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
|
[PMID: 20218620] |
| HEK293 | EC50 |
10.6 μM
Compound: ACPT-I
|
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
|
[PMID: 20218620] |
| HEK293 | EC50 |
280 μM
Compound: ACPT-I
|
Agonist activity at rat mGlu7 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
Agonist activity at rat mGlu7 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
|
[PMID: 20218620] |
| HEK293 | EC50 |
5.1 μM
Compound: ACPT-I
|
Agonist activity at rat mGlu8 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
Agonist activity at rat mGlu8 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
|
[PMID: 20218620] |
| HEK293 | EC50 |
7.2 μM
Compound: 18 ACPT-I
|
Agonist activity against Metabotropic glutamate receptor 4 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation
Agonist activity against Metabotropic glutamate receptor 4 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation
|
[PMID: 9301676] |
Chemical Information
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CAS. Nr. 194918-76-8
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Appearance Solid
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Molecular Weight 217.18
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Formel C8H11NO6
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Color White to off-white
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SMILES
OC([C@]1(C[C@H]([C@H](C1)C(O)=O)C(O)=O)N)=O
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Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
H2O : 2 mg/mL (9.21 mM; Need ultrasonic and warming)
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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (276 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)
Verweise
[1]. Acher FC, et al. Synthesis and pharmacological characterization of aminocyclopentanetricarboxylic acids: new tools to discriminate between metabotropic glutamate receptor subtypes. J Med Chem. 1997 Sep 12;40(19):3119-29. [Content Brief]
[2]. Domin H, et al. Neuroprotective potential of the group III mGlu receptor agonist ACPT-I in animal models of ischemic stroke: In vitro and in vivo studies. Neuropharmacology. 2016 Mar;102:276-94. [Content Brief]
[3]. Domin H, et al. Group III mGlu receptor agonist, ACPT-I, exerts potential neuroprotective effects in vitro and in vivo. Neurotox Res. 2014 Jul;26(1):99-113. [Content Brief]
[4]. Chapman AG, et al. Anticonvulsant activity of a mGlu(4alpha) receptor selective agonist, (1S,3R,4S)-1-aminocyclopentane-1,2,4-tricarboxylic acid. Eur J Pharmacol. 2001 Jul 20;424(2):107-13. [Content Brief]
[5]. Stachowicz K, et al. The group III mGlu receptor agonist ACPT-I exerts anxiolytic-like but not antidepressant-like effects, mediated by the serotonergic and GABA-ergic systems. Neuropharmacology. 2009 Sep;57(3):227-34. [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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O | 1 mM | 4.6045 mL | 23.0224 mL | 46.0448 mL | 115.1119 mL |
| 5 mM | 0.9209 mL | 4.6045 mL | 9.2090 mL | 23.0224 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.