AM-1488
Based on 1 Customer Validation
AM-1488 is a potent, orally active glycine receptor (GlyR) potentiator (hGlyRα3 EC50=0.45 μM).
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.87%
- CAS No.: 2079895-60-4
- Formule: C19H17N3O4S
- Masse moléculaire:383.42
-
Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
-
Solvant et solubilité
- Pureté et documentation
- Références
-
Help & FAQs
Activité biologique
Description
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | EC50 |
0.45 μM
Compound: 20-AM-1488
|
Positive allosteric modulation of human glycine alpha3 receptor expressed in HEK293T cells assessed as potentiation of glycine-induced increase in chloride ion flux after 4 mins by membrane potential blue dye based FLIPR assay
Positive allosteric modulation of human glycine alpha3 receptor expressed in HEK293T cells assessed as potentiation of glycine-induced increase in chloride ion flux after 4 mins by membrane potential blue dye based FLIPR assay
|
[PMID: 28001399] |
In Vitro
AM-1488 also potentiates native GlyRs in mouse spinal-cord neurons, which express mostly GlyRα1(β) and GlyRα3(β)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
-
Cell Line:Mouse spinal-cord neuron
-
Concentration:0.5 μM
-
Incubation Time:10 min
-
Result:Increased the peak current evoked by a puff of 20 µM glycine in five out of five cells, from an average of 50.8 pA to an average of 222.2 pA.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Mouse model of spared nerve injury (SNI)[1]
-
Dosage:20 mg/kg
-
Administration:Oral gavage; 20 mg/kg; once
-
Result:Produced a significant 94% reversal of tactile allodynia, and the unbound brain concentration was 2.8- and 1.6-fold higher than the mouse GlyRα1 and GlyRα3 EC50 values, respectively.
-
Animal Model:Naive mice[1]
-
Dosage:20 mg/kg
-
Administration:Oral gavage; 20 mg/kg; once
-
Result:Showed not significantly different from mice treated with vehicle.
Chemical Information
-
CAS No. 2079895-60-4
-
Appearance Solid
-
Masse moléculaire 383.42
-
Formule C19H17N3O4S
-
Color White to off-white
-
SMILES
O=C1[C@@]2([H])[C@@](CN(C2)S(=O)(C3=CC=C(OC=C4)C4=C3)=O)([H])C5=CN=CC=C5N1C
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 15 mg/mL (39.12 mM; Need ultrasonic; 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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
-
Fiche technique (280 KB)
-
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
-
Instruction de manipulation (2659 KB)
Références
[1]. Xin Huang, et al. Crystal structures of human glycine receptor α3 bound to a novel class of analgesic potentiators. Nat Struct Mol Biol. 2017 Feb;24(2):108-113. [Content Brief]
[2]. Howard Bregman, et al. The Discovery and Hit-to-Lead Optimization of Tricyclic Sulfonamides as Potent and Efficacious Potentiators of Glycine Receptors. J Med Chem. 2017 Feb 9;60(3):1105-1125. [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 | 1 mM | 2.6081 mL | 13.0405 mL | 26.0811 mL | 65.2026 mL |
| 5 mM | 0.5216 mL | 2.6081 mL | 5.2162 mL | 13.0405 mL | |
| 10 mM | 0.2608 mL | 1.3041 mL | 2.6081 mL | 6.5203 mL | |
| 15 mM | 0.1739 mL | 0.8694 mL | 1.7387 mL | 4.3468 mL | |
| 20 mM | 0.1304 mL | 0.6520 mL | 1.3041 mL | 3.2601 mL | |
| 25 mM | 0.1043 mL | 0.5216 mL | 1.0432 mL | 2.6081 mL | |
| 30 mM | 0.0869 mL | 0.4347 mL | 0.8694 mL | 2.1734 mL |
AM-1488 Related Classifications
HY-147367 Related Classifications
Powered by Bioz