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Camicinal hydrochloride

Camicinal hydrochloride
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Purity:98.02%
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Camicinal hydrochloride

Catalog No. T11508LCas No. 923565-22-4
Camicinal hydrochloride (GSK962040 hydrochloride) is a selective agonist of motilin receptor (pEC50 = 7.9).
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Pack SizePriceAvailabilityQuantity
1 mg$117In Stock
5 mg$289In Stock
10 mg$455In Stock
25 mg$787In Stock
50 mg$1,130In Stock
100 mg$1,520In Stock
500 mg$2,970In Stock
1 mL x 10 mM (in DMSO)$388In Stock
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Product Introduction

Bioactivity
Description
Camicinal hydrochloride (GSK962040 hydrochloride) is a selective agonist of motilin receptor (pEC50 = 7.9).
In vitro
Camicinal hydrochloride activated the dog motilin receptor (pEC50 5.79; intrinsic activity 0.72, compared with [Nle13]-motilin) [1]. Camicinal hydrochloride was preferred because its initial IC50 values at CYP3A4 were significantly higher than our preferred threshold of 10 μM [2]. Camicinal hydrochloride had no significant activity at a range of other receptors (including ghrelin), ion channels, and enzymes. In rabbit gastric antrum, Camicinal hydrochloride (300 nmol/L -10 μmol/L) caused prolonged facilitation of the amplitude of cholinergically mediated contractions, to a maximum of 248 ± 47% at 3 μmol/L. The pEC50 values for motilin, erythromycin and Camicinal hydrochloride were, respectively, 10.4 ± 0.01 (n = 770), 7.3 ± 0.29 (n = 4) and 7.9 ± 0.09 (n = 17) [4].
In vivo
Camicinal hydrochloride induced phasic contractions, the duration of which was dose-related (48 and 173 min for 3 and 6 mg/kg), driven by mean plasma concentrations >1.14 μmol/L. After the effects of Camicinal hydrochloride faded, migrating motor complex (MMC) activity returned. Migrating motor complex restoration was unaffected by 3 mg/kg Camicinal hydrochloride but at 6 mg/kg, MMCs returned 253 min after dosing, compared with 101 min after saline (n = 5 each) [1]. The oral bioavailability (Fpo) of Camicinal hydrochloride was found to be 48 (13%. Camicinal hydrochloride 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) [2]. Camicinal hydrochloride (5 mg/kg) also produced an increase in total faecal weight over the 2-h postdose period (21.2 ± 4.5 g; P < 0.05) [4]. Camicinal hydrochloride strongly facilitated cholinergic activity in the antrum, with lower activity in the fundus and small intestine only [4].
AliasGSK962040 hydrochloride
Chemical Properties
Molecular Weight461.02
FormulaC25H34ClFN4O
Cas No.923565-22-4
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 95 mg/mL (206.06 mM)
H2O: 95 mg/mL (206.06 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.1691 mL10.8455 mL21.6910 mL108.4552 mL
5 mM0.4338 mL2.1691 mL4.3382 mL21.6910 mL
10 mM0.2169 mL1.0846 mL2.1691 mL10.8455 mL
20 mM0.1085 mL0.5423 mL1.0846 mL5.4228 mL
50 mM0.0434 mL0.2169 mL0.4338 mL2.1691 mL
100 mM0.0217 mL0.1085 mL0.2169 mL1.0846 mL

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