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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
AP-5 (AP5) is a novel, selective and potent NMDA (N-methyl-D-aspartate) receptor antagonist with anticonvulsant activity. It actis by competitively inhibiting the ligand (glutamate) binding site of NMDA receptors.
| ln Vitro |
The glutamate-induced increase in Arc/Arg3.1 protein levels is partially inhibited by DL-AP5 (100 μM) [5]. Arc/Arg3.1's NMDA-induced upregulation is reduced by DL-AP5 [5].
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| ln Vivo |
DL-AP5 (0-10 μg/rat, Intra-CA1) greatly diminishes the effect of NMDA [3]. DL-AP5 (0-10 nmol, intracerebroventricular injection) promotes a dose-dependent increase in food consumption [4]. DL-AP5 (5 nmol, intracerebroventricular injection) attenuates the reduction in food consumption generated by intracerebroventricular injection of ghrelin [4].
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| Animal Protocol |
Animal/Disease Models: Male Wistar rat (180-230 g) [3]
Doses: 1, 3.2 and 10 μg/rat Route of Administration: Inject into the dorsal hippocampus (within CA1) immediately after electric shock, one time Experimental Results:Significant reduction There was a significant interaction effect of NMDA (10-2 μg/rat, within CA1). Animal/Disease Models: Broiler chicken (FD3) (3 hrs (hrs (hours)) fast, n=8 per group) [4] Doses: 0, 2.5, 5 and 10 nmol; volume of 10 µL Route of Administration: intracerebroventricular injection Experimental Results: dose causing food consumption The dependence increased, being significant for the 5 and 10 nmol doses. Animal/Disease Models: broiler rooster (fasted for 3 hrs (hrs (hours)) (FD3), n=8 per group) [4] Doses: 5 nmol Route of Administration: intracerebroventricular injection, followed by ghrelin (0.6 nmol) Experimental Results: Attenuated by Intracerebroventricular injection of ghrelin. |
| References |
[1]. Murray CW, et al. Neurokinin and NMDA antagonists (but not a kainic acid antagonist) are antinociceptive in the mouse formalin model. Pain. 1991;44(2):179-185.
[2]. Massey SC, et al. N-methyl-D-aspartate receptors of ganglion cells in rabbit retina. J Neurophysiol. 1990;63(1):16-30. [3]. Jafari-Sabet M. NMDA receptor blockers prevents the facilitatory effects of post-training intra-dorsal hippocampal NMDA and physostigmine on memory retention of passive avoidance learning in rats. Behav Brain Res. 2006 Apr 25;169(1):120-7. [4]. Taati M, et al. The effects of DL-AP5 and glutamate on ghrelin-induced feeding behavior in 3-h food-deprived broiler cockerels. J Physiol Biochem. 2011 Jun;67(2):217-23. [5]. Chen T, et al. Glutamate-induced rapid induction of Arc/Arg3.1 requires NMDA receptor-mediated phosphorylation of ERK and CREB. Neurosci Lett. 2017 Nov 20;661:23-28. |
| Molecular Formula |
C5H12NO5P
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|---|---|
| Molecular Weight |
197.1262
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| CAS # |
76326-31-3
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| Related CAS # |
D-AP5;79055-68-8;L-AP5;79055-67-7
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| SMILES |
P(C([H])([H])C([H])([H])C([H])([H])C([H])(C(=O)O[H])N([H])[H])(=O)(O[H])O[H]
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~33.33 mg/mL (~169.08 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (253.64 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.0728 mL | 25.3640 mL | 50.7279 mL | |
| 5 mM | 1.0146 mL | 5.0728 mL | 10.1456 mL | |
| 10 mM | 0.5073 mL | 2.5364 mL | 5.0728 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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