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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Purity: ≥98%
Camicinal (also known as GSK962040) is a novel, potent and selective motilin receptor agonist with pEC50 of 7.9. It appears to work as a gastrointestinal motility stimulant in both humans and rabbits. In a clinical setting that is in need of novel agents, camicinal offers a fresh approach to treatment.
Targets |
Motilin Receptor ( pEC50 = 7.9 )
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ln Vitro |
Camicinal (GSK962040) did not exhibit any noteworthy effects at other receptors, ion channels, or enzymes, such as ghrelin. Camicinal (GSK962040) 300 nmol L 1-10 μmol L 1 prolongedly facilitated the amplitude of cholinergically mediated contractions in the rabbit gastric antrum, reaching a maximum of 248 ± 47% at 3 μmol L 1. Motilin, erythromycin, and Camicinal (GSK962040) had pEC50 values of 10.4 ± 0.01 (n = 770), 7.3 ± 0.29 (n = 4), and 7.9 ± 0.09 (n = 17), respectively [1]. Camicinal (GSK962040) compared with [Nle13]-motilin, activated the dog motilin receptor (pEC50 5.79; intrinsic activity 0.72)[2]. Camicinal (GSK962040) was the drug of choice because, at CYP3A4, its initial IC50 values were much higher than our recommended threshold of 10 μM [3].
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ln Vivo |
Camicinal (GSK962040) (5 mg free base kg 1) additionally caused a rise in total faecal weight (21.2 ± 4.5 g; P < 0.05) during the 2-hour postdose period[1]. Camicinal (GSK962040) caused dose-dependent phasic contractions, lasting 48 and 173 minutes for 3 and 6 mg kg1, respectively, and were triggered by mean plasma concentrations greater than 1.14 μmol L 1. Migration of the migrating motor complex (MMC) resumed after GSK962040's effects subsided. 3 mg kg 1 GSK962040 had no effect on the restoration of the migrating motor complex, but at 6 mg kg 1, MMCs returned 253 min after dosing, as opposed to 101 min after saline (n = 5 each)[2]. It was discovered that Camicinal (GSK962040) had an oral bioavailability (Fpo) of 48 (13%). When compared to the short-lived effect of [Nle13]motilin (T1/2 ) 11.4 ( 1.5 min at 0.3 μM), camecicinal (GSK962040) exhibits a long-lasting effect (T1/2 ) 46.9 ( 5.0 min at 3 μM) [3]. Only the fundus and small intestine showed reduced cholinergic activity when camicinal (GSK962040) was administered [4].
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References |
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Molecular Formula |
C25H33FN4O
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Molecular Weight |
424.55412
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Exact Mass |
424.26
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Elemental Analysis |
C, 70.73; H, 7.83; F, 4.47; N, 13.20; O, 3.77
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CAS # |
923565-21-3
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Related CAS # |
Camicinal hydrochloride; 923565-22-4
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Appearance |
Solid powder
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SMILES |
C[C@H]1CN(CCN1)CC2=CC=C(C=C2)CC(=O)N3CCC(CC3)NC4=CC(=CC=C4)F
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InChi Key |
RZKDEGZIFSJVNA-IBGZPJMESA-N
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InChi Code |
InChI=1S/C25H33FN4O/c1-19-17-29(14-11-27-19)18-21-7-5-20(6-8-21)15-25(31)30-12-9-23(10-13-30)28-24-4-2-3-22(26)16-24/h2-8,16,19,23,27-28H,9-15,17-18H2,1H3/t19-/m0/s1
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Chemical Name |
1-[4-(3-fluoroanilino)piperidin-1-yl]-2-[4-[[(3S)-3-methylpiperazin-1-yl]methyl]phenyl]ethanone
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Synonyms |
Camicinal; GSK-962040; GSK962040; GSK 962040
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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) |
DMSO: ~100 mg/mL (~235.5 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.89 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 25.0 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: ≥ 2.5 mg/mL (5.89 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 25.0 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: ≥ 2.5 mg/mL (5.89 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.3554 mL | 11.7772 mL | 23.5544 mL | |
5 mM | 0.4711 mL | 2.3554 mL | 4.7109 mL | |
10 mM | 0.2355 mL | 1.1777 mL | 2.3554 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.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT02210000 | Completed | Drug: Camicinal Drug: Placebo |
Gastroparesis | GlaxoSmithKline | August 27, 2014 | Phase 2 |
NCT01039974 | Completed | Drug: GSK962040 Drug: Ketoconazole |
Gastroparesis | GlaxoSmithKline | September 18, 2009 | Phase 1 |
NCT00733551 | Completed | Drug: GSK962040 Drug: Placebo |
Gastroparesis | GlaxoSmithKline | September 23, 2008 | Phase 1 |
NCT01039805 | Completed | Drug: GSK962040 (50 mg) Drug: GSK962040 (75 mg) |
Gastroparesis | GlaxoSmithKline | December 2009 | Phase 2 |
NCT00562848 | Completed | Drug: GSK962040 Drug: Placebo |
Gastroparesis | GlaxoSmithKline | September 10, 2007 | Phase 1 |
Effects of motilin and GSK962040 on contractions to EFS in circular muscle strips from human gastric antrum and fundus. Br J Pharmacol . 2012 Oct;167(4):763-74. td> |
Experimental records showing the response of circular muscle strips from human gastric fundus and antrum to the continuous presence of motilin and GSK962040. Br J Pharmacol . 2012 Oct;167(4):763-74. td> |