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| Targets |
CJ-033466 targets the 5-hydroxytryptamine 4 (5-HT4) receptor, a G protein-coupled receptor (GPCR) that plays important roles in gastrointestinal motility, cognition, and other physiological functions. It acts as a partial agonist at this receptor with an EC50 of 9 nM. The compound exhibits high selectivity for 5-HT4 receptors over 5-HT and D2 receptors. Its agonism at the 5-HT4 receptor leads to increased gastrointestinal motility, making it useful for studying gastric motility disorders.
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| ln Vitro |
CJ-033466 demonstrates potent agonism at the 5-HT4 receptor with an EC50 of 9 nM. It shows high selectivity for 5-HT4 receptors compared to 5-HT and D2 receptors. The compound exhibits weak hERG channel blocking activity (IC50 = 2570.4 nM), suggesting a favorable cardiac safety profile. It also demonstrates significant antiviral properties against SARS-CoV-2, with 98.61% inhibition of the SARS-CoV-2 3CL-Pro protease at 20 μM in a FRET-based assay. CJ-033466 displays gastroprokinetic effects upon oral administration.
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| ln Vivo |
CJ-033466 displays gastroprokinetic effects upon oral administration. The compound's agonism at the 5-HT4 receptor promotes gastrointestinal motility, which has been demonstrated in animal models. It has been studied for its potential in treating gastrointestinal motility disorders. The compound also shows diverse biological activities and has been investigated for antiviral properties against SARS-CoV-2. CJ-033466 has been evaluated for its effects on gastric emptying and intestinal transit in preclinical models.
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| Enzyme Assay |
The in vitro receptor binding assay for CJ-033466 typically involves measuring its affinity for the 5-HT4 receptor using radioligand binding or functional assays. For binding studies, membrane preparations from cells expressing the 5-HT4 receptor are incubated with varying concentrations of CJ-033466 (typically 0.001-100 μM) and a radiolabeled ligand (such as [3H]GR113808). The binding affinity (Ki) is determined by competition binding analysis. For functional assays, cells expressing the 5-HT4 receptor are treated with CJ-033466 and the production of cAMP is measured using ELISA or HTRF-based assays.
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| Cell Assay |
In vitro cellular assays for CJ-033466 typically involve treating cells expressing the 5-HT4 receptor (such as HEK-293 or CHO cells) with the compound at concentrations ranging from 0.001 to 10 μM. cAMP production is measured using ELISA or HTRF-based assays to assess receptor activation. Cellular viability and proliferation are evaluated using standard assays. The compound is dissolved in DMSO as a stock solution and diluted in cell culture medium, with DMSO-only treated cells serving as controls. The compound's selectivity over other serotonin receptors and D2 receptors can be assessed in parallel assays.
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| Animal Protocol |
In vivo animal studies for CJ-033466 typically involve oral administration to mice, rats, or guinea pigs at doses ranging from 0.1 to 10 mg/kg. Gastrointestinal motility is assessed by measuring gastric emptying, intestinal transit, or colonic motility using standard methods. Blood and tissue samples are collected for pharmacokinetic analysis. The compound's effects on gastrointestinal motility are evaluated in models of postoperative ileus or other motility disorders. The compound is formulated in appropriate vehicles for oral administration.
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| ADME/Pharmacokinetics |
CJ-033466 has a molecular weight of 377.91 g/mol and formula C19H28ClN5O. The compound shows weak hERG channel blocking activity with an IC50 of 2570.4 nM, suggesting a favorable cardiac safety profile. Recommended storage is at +4°C for powder. The compound is soluble in DMSO and other organic solvents. Detailed PK parameters such as half-life, Cmax, AUC, and bioavailability would require experimental determination, but the compound's oral bioavailability is indicated by its gastroprokinetic effects upon oral administration.
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| Toxicity/Toxicokinetics |
Toxicity data for CJ-033466 are not extensively reported. The compound shows weak hERG channel blocking activity (IC50 = 2570.4 nM), suggesting a favorable cardiac safety profile. The compound is intended for research use only and is not approved for human therapeutic applications. Standard preclinical toxicity assessments would include acute toxicity studies in rodents, repeated-dose toxicity studies, and assessment of off-target effects. The compound's high selectivity for 5-HT4 receptors may contribute to a favorable safety profile.
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| Additional Infomation |
CJ-033466 (CAS 519148-48-2) is a potent and selective partial agonist of the 5-HT4 receptor with an EC50 of 9 nM. It has a molecular weight of 377.91 g/mol and formula C19H28ClN5O. The compound exhibits high selectivity for 5-HT4 receptors over 5-HT and D2 receptors and displays gastroprokinetic effects upon oral administration. It shows weak hERG channel blocking activity (IC50 = 2570.4 nM). The compound is also known as 5-amino-6-chloro-2-methyl-N-((1-(2-methylpropyl)-4-piperidinyl)methyl)imidazo(1,2-a)pyridine-8-carboxamide. It is not approved for clinical use.
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| Molecular Formula |
C19H28CLN5O
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| Molecular Weight |
377.91200
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| Exact Mass |
377.198
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| CAS # |
519148-48-2
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| PubChem CID |
10429706
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| Appearance |
Light yellow to light brown solid powder
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| LogP |
3.886
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
26
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| Complexity |
483
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C)CN1CCC(CNC(C2C3=NC(C)=CN3C(N)=C(Cl)C=2)=O)CC1
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| InChi Key |
ISKHMDNIWXPUGR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H28ClN5O/c1-12(2)10-24-6-4-14(5-7-24)9-22-19(26)15-8-16(20)17(21)25-11-13(3)23-18(15)25/h8,11-12,14H,4-7,9-10,21H2,1-3H3,(H,22,26)
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| Chemical Name |
5-amino-6-chloro-2-methyl-N-[[1-(2-methylpropyl)piperidin-4-yl]methyl]imidazo[1,2-a]pyridine-8-carboxamide
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
DMSO : ~50 mg/mL (~132.31 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 | 2.6461 mL | 13.2307 mL | 26.4613 mL | |
| 5 mM | 0.5292 mL | 2.6461 mL | 5.2923 mL | |
| 10 mM | 0.2646 mL | 1.3231 mL | 2.6461 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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