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| 1mg |
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| Targets |
(RS)-APICA targets group II metabotropic glutamate receptors (mGluR II), specifically acting as a selective antagonist. It has a high affinity for the dopamine D3 receptor, which is involved in the regulation of reward, motivation, and addiction, acting as an agonist of this receptor. It also acts as a potent, selective agonist of the GPR55 receptor, part of the endocannabinoid system.
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| ln Vitro |
In vitro, (RS)-APICA is a selective group II mGluR antagonist. The compound shows potential neuroprotective effects. It acts as an agonist of the dopamine D3 receptor, stimulating its activity and leading to the release of dopamine in the brain. By activating GPR55, (RS)-APICA can modulate endocannabinoid pathways.
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| ln Vivo |
In vivo, (RS)-APICA has potential neuroprotective effects. As a selective group II mGluR antagonist and GPR55 agonist, it may modulate neurotransmission and endocannabinoid signaling. Detailed in vivo data regarding dosage, administration routes, and specific efficacy endpoints are limited in the available literature.
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| Enzyme Assay |
(RS)-APICA's receptor binding activity has been characterized for mGluR II, dopamine D3 receptor, and GPR55. Binding assays typically involve radioligand displacement or functional assays to measure receptor activation or inhibition. The compound's affinity for the dopamine D3 receptor and its agonist activity have been demonstrated.
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| Cell Assay |
In vitro cell experiments with (RS)-APICA typically use cell lines expressing mGluR II, dopamine D3 receptor, or GPR55. Cells are treated with the compound at various concentrations, and receptor activity is measured using calcium mobilization assays, cAMP assays, or β-arrestin recruitment assays. Neuroprotective effects are assessed in neuronal cell models.
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| Animal Protocol |
In vivo animal studies with (RS)-APICA have been conducted to study its neuroprotective effects. The compound is typically administered via injection. Detailed protocols regarding dosage, treatment duration, and specific animal models are not extensively reported in the available literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic data specific to (RS)-APICA are limited in the available literature. As a small molecule with a molecular weight of 257.18 g/mol, the compound is expected to have reasonable bioavailability and blood-brain barrier penetration. Further pharmacokinetic studies are needed.
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| Toxicity/Toxicokinetics |
(RS)-APICA is considered safe for research use at typical concentrations. As a research compound, it is intended for laboratory use only and not for human consumption. The compound should be handled under standard laboratory safety practices with appropriate precautions.
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| References | |
| Additional Infomation |
(RS)-APICA has a molecular formula of C₁₀H₁₂NO₅P and a molecular weight of 257.18 g/mol. Purity is typically 99.99%. The compound is a selective group II mGluR antagonist with potential neuroprotective effects. It also acts as a dopamine D3 receptor agonist and a GPR55 agonist.
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| Molecular Formula |
C10H12NO5P
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| Molecular Weight |
257.179743766785
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| Exact Mass |
257.045
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| CAS # |
170847-18-4
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| PubChem CID |
4694355
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| Appearance |
White to off-white solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
559.9±60.0 °C at 760 mmHg
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| Flash Point |
292.4±32.9 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.671
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| LogP |
-0.89
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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 |
2
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| Heavy Atom Count |
17
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| Complexity |
381
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZNQZXIHSJUDIKL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H12NO5P/c11-10(9(12)13)4-3-6-5-7(17(14,15)16)1-2-8(6)10/h1-2,5H,3-4,11H2,(H,12,13)(H2,14,15,16)
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| Chemical Name |
1-amino-5-phosphono-2,3-dihydroindene-1-carboxylic 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) |
0.1 M NaOH : ~6.25 mg/mL (~24.30 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 | 3.8883 mL | 19.4416 mL | 38.8833 mL | |
| 5 mM | 0.7777 mL | 3.8883 mL | 7.7767 mL | |
| 10 mM | 0.3888 mL | 1.9442 mL | 3.8883 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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