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NP10679 is an orally available, selective, brain-penetrating, potent, and pH-sensitive N-methyl-D-aspartate (NMDA) receptor inhibitor of the GluN2B subunit.NP10679 inhibits histamine H1, hERG channels, and CYP enzymes, and may be useful in the study of epilepsy and ischemic stroke.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $293 | In Stock | |
5 mg | $722 | In Stock | |
10 mg | $987 | In Stock | |
25 mg | $1,520 | In Stock | |
50 mg | $1,980 | In Stock | |
100 mg | $2,500 | In Stock |
Description | NP10679 is an orally available, selective, brain-penetrating, potent, and pH-sensitive N-methyl-D-aspartate (NMDA) receptor inhibitor of the GluN2B subunit.NP10679 inhibits histamine H1, hERG channels, and CYP enzymes, and may be useful in the study of epilepsy and ischemic stroke. |
Targets&IC50 | H1 Receptor:0.04 μM (Ki), H1 Receptor:0.073 μM, α1B-adrenoceptor:1.92 μM (Ki), α2C-adrenoceptor:3.09 μM (Ki), α1A-adrenoceptor:0.603 μM (Ki), α1A-adrenoceptor:0.154 μM, α1D-adrenoceptor:0.495 μM (Ki) |
In vitro | NP10679 is an NMDA receptor inhibitor containing GluN2B that is more effective than physiological pH. It exhibits inhibitory effects on 5-HT2A, α1A adrenergic receptor, H1 histamine receptor, and hERG channels[2]. |
In vivo | In the Male C57BL/6 middle cerebral artery occlusion (MCAo) model of transient ischemia mice, NP10679 (2, 5, and 10 mg/kg; intraperitoneal injection; administered 15 minutes prior to transient ischemia) dose-dependently reduces infarct volumes, with an ED50 of 1 mg/kg[2]. |
Molecular Weight | 449.47 |
Formula | C23H26F3N3O3 |
Cas No. | 2914889-88-4 |
Smiles | O(C[C@@H](CN1CCN(CC1)C2=CC=C(C(F)(F)F)C=C2)O)C=3C=C4C(=CC3)NC(=O)CC4 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 80 mg/mL (177.99 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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