Physicochemical Properties
| Molecular Formula | C5H11LINO5P |
| Molecular Weight | 203.06 |
| CAS # | 125229-62-1 |
| Related CAS # | D-AP5;79055-68-8;DL-AP5;76326-31-3;DL-AP5 sodium;1303993-72-7;L-AP5 |
| PubChem CID | 16218948 |
| Appearance | Typically exists as solids at room temperature |
| LogP | 0 |
| Hydrogen Bond Donor Count | 4 |
| Hydrogen Bond Acceptor Count | 6 |
| Rotatable Bond Count | 5 |
| Heavy Atom Count | 13 |
| Complexity | 200 |
| Defined Atom Stereocenter Count | 0 |
| SMILES | [Li].C(CC(C(=O)O)N)CP(=O)(O)O |
| Synonyms | 2-APV lithium; DL-2-Amino-5-phosphonovaleric acid lithium |
| HS Tariff Code | 2934.99.9001 |
| 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) |
Biological Activity
| Targets | NMDA Receptor |
| ln Vitro | DL-AP5 (100 μM) partially prevents glutamate-induced increase in Arc/Arg3.1 protein levels[5]. DL-AP5 decreases the NMDA-induced Arc/Arg3.1 upregulation[5]. |
| ln Vivo | DL-AP5 (0-10 μg/rat, Intra-CA1) significantly decreases the effect of NMDA[3]. DL-AP5 (0-10 nmol, Intracerebroventricular injection) causes a dose-dependent increase in food consumption[4]. DL-AP5 (5 nmol, Intracerebroventricular injection) attenuates the decreased food consumption induced by the intracerebroventricular injection of ghrelin[4]. |
| Animal Protocol |
Animal/Disease Models: Male Wistar rats (180-230 g)[3] Doses: 1, 3.2 and 10 μg/rat Route of Administration: Injected into the intra-dorsal hippocampal (intra-CA1) immediately after shock administration, once Experimental Results: Significantly decreased the effect of NMDA (10-2 μg/rat, intra-CA1) with significant interaction. Animal/Disease Models: Broilers cockerels (3-h fooddeprived (FD3), n=8 for each group)[4] Doses: 0, 2.5, 5, and 10 nmol; in a volume of 10 μL Route of Administration: Intracerebroventricular injection Experimental Results: Caused a dose-dependent increase in food consumption which was significant for 5 and 10 nmol doses. Animal/Disease Models: Broilers cockerels (3-h fooddeprived (FD3), n=8 for each group)[4] Doses: 5 nmol Route of Administration: Intracerebroventricular injection, followed by ghrelin (0.6 nmol) Experimental Results: Attenuated the decreased food consumption induced by the intracerebroventricular injection of ghrelin. |
| References |
[1]. Neurokinin and NMDA antagonists (but not a kainic acid antagonist) are antinociceptive in the mouse formalin model. Pain. 1991;44(2):179-185. [2]. 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]. 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]. 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. |
Solubility Data
| Solubility (In Vitro) | May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples |
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples. Injection Formulations (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] *Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.9247 mL | 24.6233 mL | 49.2465 mL | |
| 5 mM | 0.9849 mL | 4.9247 mL | 9.8493 mL | |
| 10 mM | 0.4925 mL | 2.4623 mL | 4.9247 mL |