| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
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| Targets |
CPPG targets metabotropic glutamate receptors (mGluRs), specifically group II (mGluR-2, mGluR-3) and group III (mGluR-4, mGluR-6, mGluR-7, mGluR-8) receptors. It is a competitive antagonist that binds to the glutamate binding site on these receptors. It effectively reverses the inhibition of forskolin-stimulated cAMP accumulation mediated by L-AP4 (IC50=2.2 nM) and L-CCG-I (IC50=46.2 nM).
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| ln Vitro |
In adult rat cortical slices, CPPG ((RS)-CPPG) potently reverses the inhibition of forskolin-stimulated cyclic AMP buildup mediated by L-AP4 (IC50=2.2 nM) and L-CCG-I (IC50=46.2 nM). In the brain of adult rats, CPPG is a strong antagonist of group II/III mGlu receptors and shows a modest degree of selectivity for group III mGlu receptors. On the other hand, in cultured cerebellar granule cells and newborn rat cortex, CPPG has a negligible impact on class I mGlu receptors [1].
CPPG exhibits potent in vitro activity as a group II/III mGlu receptor antagonist. It has IC50 values of 46.2 nM for group II and 2.2 nM for group III receptors. Its selectivity for group III over group II is approximately 20-fold. It reverses L-AP4-induced inhibition of cAMP accumulation with an IC50 of 2.2 nM. These in vitro activities confirm its utility as a pharmacological tool for studying mGlu receptor function. |
| ln Vivo |
In vivo, CPPG is used in neuropharmacological research to study the role of group II and III mGlu receptors in various physiological and pathological processes. As a competitive antagonist, it can be used to block mGlu receptor-mediated effects in animal models. Its ability to cross the blood-brain barrier is not extensively documented. Its in vivo effects are primarily studied in the context of synaptic transmission and neurological disorders.
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| Enzyme Assay |
In vitro receptor binding assays for CPPG involve measuring its affinity for group II and III mGlu receptors. These assays use membrane preparations from rat brain or cells expressing recombinant mGlu receptors and radiolabeled ligands. Functional assays measuring cAMP accumulation are used to determine antagonist activity. The IC50 values are determined from dose-response curves (46.2 nM for group II, 2.2 nM for group III).
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| Cell Assay |
In vitro cellular assays for CPPG are conducted in cells expressing group II or III mGlu receptors. Cells are treated with the compound at various concentrations, and agonist-induced inhibition of cAMP accumulation is measured. The compound's ability to reverse agonist effects is assessed. These assays characterize the compound's activity as a potent mGlu receptor antagonist.
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| Animal Protocol |
In vivo animal experiments with CPPG are conducted in rodent models of neurological disorders. The compound is administered via intracerebroventricular (ICV) injection or systemic administration. Behavioral assays, electrophysiological recordings, and biochemical measurements are performed to assess the effects of mGlu receptor antagonism. These studies help elucidate the role of group II and III mGlu receptors in brain function and disease.
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| ADME/Pharmacokinetics |
CPPG has a molecular weight of 271.21 and a molecular formula of C11H14NO5P. It is soluble in 1 equivalent of NaOH at 27.12 mg/mL. The compound is typically stored as a powder at -20°C (3 years) or 4°C (2 years), and in solution at -80°C (6 months) or -20°C (1 month). Its half-life and bioavailability have not been extensively characterized.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for CPPG are limited. The compound is intended for research use only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling this compound. Further toxicity studies would be required to support any potential clinical development.
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| References | |
| Additional Infomation |
2-Amino-2-cyclopropyl-2-(4-phosphonophenyl)acetic acid is an α-amino acid.
CPPG ((RS)-CPPG) is a potent, competitive antagonist at group II and III metabotropic glutamate receptors (mGluRs). It has IC50 values of 46.2 nM for group II and 2.2 nM for group III receptors, with approximately 20-fold selectivity for group III. It reverses L-AP4 and L-CCG-I-induced inhibition of cAMP accumulation. CPPG is used in neuropharmacological research to study mGlu receptor function. |
| Molecular Formula |
C11H14NO5P
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|---|---|
| Molecular Weight |
271.20636
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| Exact Mass |
271.061
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| CAS # |
183364-82-1
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| PubChem CID |
2878
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| Appearance |
White to off-white solid powder
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| LogP |
0.838
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
18
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| Complexity |
383
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
IGODGTDUQSMDQU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H14NO5P/c12-11(10(13)14,7-1-2-7)8-3-5-9(6-4-8)18(15,16)17/h3-7H,1-2,12H2,(H,13,14)(H2,15,16,17)
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| Chemical Name |
2-amino-2-cyclopropyl-2-(4-phosphonophenyl)acetic acid
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| HS Tariff Code |
2934.99.9001
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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) |
1M NaOH : 50 mg/mL (~184.36 mM)
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| 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 | 3.6872 mL | 18.4359 mL | 36.8718 mL | |
| 5 mM | 0.7374 mL | 3.6872 mL | 7.3744 mL | |
| 10 mM | 0.3687 mL | 1.8436 mL | 3.6872 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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