| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
NMDA Receptor
|
|---|---|
| ln Vitro |
The separate optical enantiomers of 2-amino-5-phosphonovalerate (APV) and 2-amino-4-phosphonobutyrate (APB) have been tested for their ability to modify amino acid-induced and synaptic excitation of cat spinal neurones. D-(-)-APV was a highly potent and selective antagonist of amino acid-induced and synaptic excitation. Polysynaptic excitation was more susceptible to antagonism by D-APV than was monosynaptic excitation. It was considered likely that the depression of synaptic excitation by D-APV was due to the blockade of an excitatory amino acid transmitter acting at N-methyl-D-aspartate (NMDA) receptors. L-(+)-APV showed a relatively weak amino acid and synaptic blocking activity, which was similar in character to that of D-APV, and which may have been due to a slight residuum of the D isomer in the sample of the L form used. D-(-)-APB was a weak and relatively non-selective antagonist of amino acid-induced responses. In contrast, L-(+)-APB either had no effect or, at higher concentrations, enhanced these responses. Both isomers depressed synaptic responses in a proportion of the cells tested, the L form being the more potent isomer in producing this effect. Monosynaptic and polysynaptic excitations were both susceptible to this type of action. The depression of synaptic excitation by D-APB may have been due in some cases to the blockade of an excitatory amino acid transmitter. However, it is unlikely that the synaptic depressant action of L-APB is due to this mechanism.[1]
|
| References |
| Molecular Formula |
C5H12NO5P
|
|---|---|
| Molecular Weight |
197.126242637634
|
| Exact Mass |
197.045
|
| CAS # |
79055-67-7
|
| Related CAS # |
DL-AP5;76326-31-3;D-AP5;79055-68-8
|
| PubChem CID |
1617110
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.5±0.1 g/cm3
|
| Boiling Point |
482.1±55.0 °C at 760 mmHg
|
| Flash Point |
245.4±31.5 °C
|
| Vapour Pressure |
0.0±2.6 mmHg at 25°C
|
| Index of Refraction |
1.536
|
| LogP |
-2.32
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
12
|
| Complexity |
200
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
C(CP(O)(O)=O)C[C@H](N)C(=O)O
|
| InChi Key |
VOROEQBFPPIACJ-BYPYZUCNSA-N
|
| InChi Code |
InChI=1S/C5H12NO5P/c6-4(5(7)8)2-1-3-12(9,10)11/h4H,1-3,6H2,(H,7,8)(H2,9,10,11)/t4-/m0/s1
|
| Chemical Name |
(2S)-2-amino-5-phosphonopentanoic acid
|
| Synonyms |
L-AP5; 79055-67-7; (S)-2-amino-5-phosphonopentanoic acid; 5-phosphono-L-norvaline; (2S)-2-amino-5-phosphonopentanoic acid; CHEMBL71898; (S)-2-amino-5-phosphonopentanoicacid; L(+)-2-Amino-5-phosphonovaleric acid;
|
| 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)
|
| 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
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] 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). View More
Oral Formulation 3: Dissolved in PEG400 (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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