| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Target: CP-409092 targets the gamma-aminobutyric acid type A (GABAA) receptor, a major inhibitory neurotransmitter receptor in the central nervous system. As a partial agonist, it binds to the GABAA receptor and modulates chloride ion flux, producing anxiolytic effects without full receptor activation. The partial agonist profile may offer advantages over full agonists in terms of reduced side effects and lower risk of tolerance development. The compound interferes with or suppresses the transmission of signals between neurons in the nervous system.
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| ln Vitro |
In Vitro Activity: CP-409092 demonstrates partial agonist activity at the GABAA receptor in vitro. At equivalent molar concentrations, both the salt and free forms of the compound exhibit comparable biological activity. The compound's aqueous solubility (50 mg/mL) enables consistent binding assays and water-based dosing in experimental settings. Detailed electrophysiological data, including EC50 values for chloride current potentiation, are available in the primary scientific literature. The compound serves as a valuable probe for studying GABAA receptor pharmacology and partial agonism.
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| ln Vivo |
In Vivo Activity: In rat models, CP-409092 has been characterized for its pharmacokinetic profile and metabolic pathways. The compound has been studied in drug discovery efforts aimed at identifying novel therapeutic agents for neurological and psychiatric disorders. While detailed behavioral efficacy data in anxiety models are not extensively published, the compound's GABAA partial agonist activity suggests potential anxiolytic effects. It has been used as a research tool to study high-clearance, low-bioavailability GABAA partial agonists, distinct from clinically used anxiolytics.
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| Enzyme Assay |
In Vitro Enzyme/Receptor Binding Protocol: GABAA receptor binding assays typically involve radioligand binding using [3H]muscimol or [3H]flunitrazepam to membrane preparations from rat brain cortex or cells expressing recombinant GABAA receptors. Competition binding experiments with varying concentrations of CP-409092 determine receptor affinity and binding characteristics. For functional characterization, electrophysiological recordings using patch-clamp or two-electrode voltage-clamp techniques on GABAA receptor-expressing cells measure chloride currents in response to GABA alone or in combination with CP-409092.
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| Cell Assay |
In Vitro Cell-Based Assay Protocol: Cells expressing GABAA receptors (such as HEK293 or CHO cells transfected with relevant subunits) are cultured and treated with CP-409092 at various concentrations. Receptor activation is assessed by measuring chloride flux using fluorescent indicators or electrophysiological techniques. Cell viability and cytotoxicity are evaluated using standard assays such as MTT or LDH release. The compound's aqueous solubility facilitates preparation of stock solutions in water or DMSO for cell-based experiments.
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| Animal Protocol |
In Vivo Animal Assay Protocol: Rodent models are used to study CP-409092 pharmacokinetics and metabolism. In a published study, [14C]CP-409,092 was administered orally at 100 mg/kg to rats, and total recovery was 89.1%±3.2% for male rats and 89.3%±0.58% for female rats. The compound is formulated in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% saline for in vivo administration. Behavioral tests such as elevated plus maze may be used to assess anxiolytic activity.
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| ADME/Pharmacokinetics |
Pharmacokinetics: Following single intravenous and oral doses of 4 and 15 mg/kg respectively, CP-409092 exhibits high clearance of 169±18 mL/min/kg and a volume of distribution of 8.99±1.46 L/kg. Oral bioavailability is very low at 2.9%±3%. After oral administration of 100 mg/kg [14C]CP-409,092, total recovery was approximately 89% in rats. The compound undergoes oxidative deamination of the benzylic amine, serving as a probe for MAO-mediated clearance mechanisms. Its distinct pharmacokinetic signature makes it a poor surrogate for drugs with more favorable oral exposure profiles.
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| Toxicity/Toxicokinetics |
Toxicity: No detailed toxicity data are publicly available for CP-409092 HCl. As a research compound not intended for human use, comprehensive toxicological profiling has not been extensively published. The compound is for research use only and has not been approved by any regulatory agency for therapeutic applications. Standard preclinical safety assessments including acute and chronic toxicity studies would be required before any clinical development.
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| References | |
| Additional Infomation |
Additional Information: CP-409092 HCl has CAS number 225240-86-8, molecular formula C17H20ClN3O2, and molecular weight 333.81. It is also known as CP-409092, CP409092, CP 409092, and UNII-420WLS764W. The related free base has CAS number 194098-25-4. The compound is a GABAA receptor partial agonist with potential anti-anxiety activity. The hydrochloride salt form overcomes the aqueous insolubility limitations of the free base, enabling water-based dosing and reproducible binding assays. For research use only, not for human therapy.
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| Molecular Formula |
C17H20CLN3O2
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|---|---|
| Molecular Weight |
333.8126
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| Exact Mass |
333.124
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| CAS # |
225240-86-8
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| Related CAS # |
CP-409092;194098-25-4
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| PubChem CID |
139035003
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
23
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| Complexity |
418
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl[H].O=C1C([H])([H])C([H])([H])C([H])([H])C2=C1C(C(N([H])C1C([H])=C([H])C(C([H])([H])N([H])C([H])([H])[H])=C([H])C=1[H])=O)=C([H])N2[H]
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| InChi Key |
XFJIYNUISLDNLP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H19N3O2/c1-18-9-11-5-7-12(8-6-11)20-17(22)13-10-19-14-3-2-4-15(21)16(13)14/h5-8,10,18-19H,2-4,9H2,1H3,(H,20,22)
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| Chemical Name |
1H-Indole-3-carboxamide, 4,5,6,7-tetrahydro-N-(4-((methylamino)methyl)phenyl)-4-oxo-
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| Synonyms |
CP-409092; CP409092; CP 409092; UNII-420WLS764W.
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~50 mg/mL (~149.79 mM)
DMSO : ~41.67 mg/mL (~124.83 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.23 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.23 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.23 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 25 mg/mL (74.89 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9957 mL | 14.9786 mL | 29.9572 mL | |
| 5 mM | 0.5991 mL | 2.9957 mL | 5.9914 mL | |
| 10 mM | 0.2996 mL | 1.4979 mL | 2.9957 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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