CJ 033466Selective 5-HT4 partial agonist CAS# 519148-48-2 |
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Quality Control & MSDS
3D structure
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| Cas No. | 519148-48-2 | SDF | Download SDF |
| PubChem ID | 10429706 | Appearance | Powder |
| Formula | C19H28ClN5O | M.Wt | 377.91 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in DMSO and to 100 mM in ethanol | ||
| Chemical Name | 5-amino-6-chloro-2-methyl-N-[[1-(2-methylpropyl)piperidin-4-yl]methyl]imidazo[1,2-a]pyridine-8-carboxamide | ||
| SMILES | CC1=CN2C(=C(C=C(C2=N1)C(=O)NCC3CCN(CC3)CC(C)C)Cl)N | ||
| Standard InChIKey | ISKHMDNIWXPUGR-UHFFFAOYSA-N | ||
| Standard InChI | 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) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Potent and selective 5-HT4 partial agonist (EC50= 0.927 nM). Displays > 1000-fold selectivity for 5-HT4 over other 5-HT and D2 receptors. Exhibits gastroprokinetic effects in vivo following oral administration. Weakly blocks hERG (IC50 = 2.6 μM). |
CJ 033466 Dilution Calculator
CJ 033466 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.6461 mL | 13.2307 mL | 26.4613 mL | 52.9227 mL | 66.1533 mL |
| 5 mM | 0.5292 mL | 2.6461 mL | 5.2923 mL | 10.5845 mL | 13.2307 mL |
| 10 mM | 0.2646 mL | 1.3231 mL | 2.6461 mL | 5.2923 mL | 6.6153 mL |
| 50 mM | 0.0529 mL | 0.2646 mL | 0.5292 mL | 1.0585 mL | 1.3231 mL |
| 100 mM | 0.0265 mL | 0.1323 mL | 0.2646 mL | 0.5292 mL | 0.6615 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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The 5-HT(4) agonists cisapride, mosapride, and CJ-033466, a Novel potent compound, exhibit different human ether-a-go-go-related gene (hERG)-blocking activities.[Pubmed:17928736]
J Pharmacol Sci. 2007 Oct;105(2):207-10. Epub 2007 Oct 6.
The blocking effect of three 5-HT(4) agonists, cisapride, mosapride, and the newly discovered CJ-033466 on the human ether-a-go-go-related gene (hERG) channel was studied using a whole cell patch-clamp technique in HEK293 cells. Cisapride was found to be the most potent of the hERG blockers. CJ-033466 had the widest safety margin between its hERG blocking activity and 5-HT(4) agonism among the tested compounds. This suggests a lower clinical risk of cardiac arrhythmia in CJ-033466 compared with the other 2 agonists. Therefore, CJ-033466 has the potential to be a drug with higher therapeutic efficacy and less cardiac risk than both cisapride and mosapride.
5-Amino-6-chloro-N-[(1-isobutylpiperidin-4-yl)methyl]-2-methylimidazo[1,2-alpha]p yridine-8-carboxamide (CJ-033,466), a novel and selective 5-hydroxytryptamine4 receptor partial agonist: pharmacological profile in vitro and gastroprokinetic effect in conscious dogs.[Pubmed:18198343]
J Pharmacol Exp Ther. 2008 Apr;325(1):190-9.
5-Hydroxytryptamine (5-HT) receptors and dopamine(2) (D(2)) receptor modulate gastrointestinal motility. Gastroprokinetic agents that act on several 5-HT receptor subtypes and/or D(2) receptors are used clinically. Although the 5-HT(4) receptor is known to mediate the gastroprokinetic effects of these agents, the absence of highly selective 5-HT(4) receptor agonists has made it difficult to confirm the physiological consequences of selective 5-HT(4) receptor stimulation. In this study, we report the in vitro pharmacological profiles and the in vivo gastroprokinetic effects of 5-amino-6-chloro-N-[(1-isobutylpiperidin-4-yl)methyl]-2-methylimidazo[1,2-alpha]p yridine-8-carboxamide (CJ-033,466), a novel, potent, and selective 5-HT(4) partial agonist. Compared with preceding 5-HT(4) agonists such as cisapride, mosapride, and tegaserod, CJ-033,466 had a superior in vitro profile, with nanomolar agonistic activities for the 5-HT(4) receptor and 1000-fold greater selectivity for the 5-HT(4) receptor over other 5-HT and D(2) receptors. In vivo studies in conscious dogs showed that CJ-033,466 dose-dependently stimulated gastric antral motility in both the fasted and postprandial states at the same dose range and that it was 30 times more potent than cisapride. Furthermore, CJ-033,466 accelerated the gastric emptying rate in a gastroparesis dog model at the minimally effective dose established in the gastric motility study. In conclusion, CJ-033,466 is a potent and highly selective 5-HT(4) agonist that stimulates physiologically coordinated gastric motility, and it has no activity on other 5-HT receptor subtypes and D(2) receptors. Therefore, CJ-033,466 could be used to treat gastroparesis, providing better gastroprokinetics and reduced side effects mediated by the other receptors.
