GSK962040 (hydrochloride)
Modify Date: 2024-01-02 10:37:49
GSK962040 (hydrochloride) structure
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Common Name | GSK962040 (hydrochloride) | ||
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| CAS Number | 923565-22-4 | Molecular Weight | 461.02 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C25H34ClFN4O | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of GSK962040 (hydrochloride)Camicinal (GSK962040) hydrochloride is a small molecule, selective motilin receptor agonist with pEC50 of 7.9. |
| Name | 1-{4-[(3-Fluorophenyl)amino]-1-piperidinyl}-2-(4-{[(3S)-3-methyl- 1-piperazinyl]methyl}phenyl)ethanone |
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| Synonym | More Synonyms |
| Description | Camicinal (GSK962040) hydrochloride is a small molecule, selective motilin receptor agonist with pEC50 of 7.9. |
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| Related Catalog | |
| Target |
pEC50: 7.9 (Motilin Receptor)[1]. |
| In Vitro | Camicinal (GSK962040) had no significant activity at a range of other receptors (including ghrelin), ion channels and enzymes. In rabbit gastric antrum, Camicinal (GSK962040) 300 nmol L 1-10 μmol L 1 caused a prolonged facilitation of the amplitude of cholinergically mediated contractions, to a maximum of 248 ± 47% at 3 μmol L 1. The pEC50 values for motilin, erythromycin and Camicinal (GSK962040) were, respectively, 10.4 ± 0.01 (n = 770), 7.3 ± 0.29 (n = 4) and 7.9 ± 0.09 (n = 17) [1]. Camicinal (GSK962040) activated the dog motilin receptor (pEC50 5.79; intrinsic activity 0.72, compared with [Nle13]-motilin) [2]. Camicinal (GSK962040) was preferred because its initial IC50 values at CYP3A4 were significantly higher than our preferred threshold of 10 μM [3]. |
| In Vivo | Camicinal (GSK962040) (5 mg free base kg 1) also produced an increase in total faecal weight over the 2-h postdose period (21.2 ± 4.5 g; P < 0.05) [1]. Camicinal (GSK962040) induced phasic contractions, the duration of which was dose-related (48 and 173 min for 3 and 6 mg kg 1), driven by mean plasma concentrations >1.14 μmol L 1. After the effects of Camicinal (GSK962040) faded, migrating motor complex (MMC) activity returned. Migrating motor complex restoration was unaffected by 3 mg kg 1 Camicinal (GSK962040) but at 6 mg kg 1, MMCs returned 253 min after dosing, compared with 101 min after saline (n = 5 each) [2]. he oral bioavailability (Fpo) of Camicinal (GSK962040) was found to be 48 ( 13%. Camicinal (GSK962040) shows a long lasting effect (T1/2 ) 46.9 ( 5.0 min at 3 μM) when compared with the short-lived effect of [Nle13]motilin (T1/2 ) 11.4 ( 1.5 min at 0.3 μM) [3]. Camicinal (GSK962040) strongly facilitated cholinergic activity in the antrum, with lower activity in fundus and small intestine only [4]. |
| References |
| Molecular Formula | C25H34ClFN4O |
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| Molecular Weight | 461.02 |
| PSA | 47.61000 |
| LogP | 3.54260 |
| GSK962040 (hydrochloride) |