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Camicinal hydrochloride

Catalog No. T11508L CAS 923565-22-4

Synonyms: GSK962040 hydrochloride

Camicinal hydrochloride (GSK962040 hydrochloride) is a selective agonist of motilin receptor (pEC50 = 7.9).

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Camicinal hydrochloride Chemical Structure

Camicinal hydrochloride, CAS 923565-22-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 163.00
5 mg	In stock	$ 347.00
10 mg	In stock	$ 497.00
25 mg	In stock	$ 793.00
50 mg	In stock	$ 1,130.00
100 mg	In stock	$ 1,520.00
500 mg	In stock	$ 2,970.00
1 mL * 10 mM (in DMSO)	In stock	$ 388.00

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Purity: 98.02%

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Description	Camicinal hydrochloride (GSK962040 hydrochloride) is a selective agonist of motilin receptor (pEC50 = 7.9).
Targets&IC50	Motilin receptor:7.9 (pEC50)
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].

Synonyms	GSK962040 hydrochloride
Molecular Weight	461.02
Formula	C25H34ClFN4O
CAS No.	923565-22-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 95 mg/mL (206.06 mM), Sonication is recommended.

H2O: 95 mg/mL (206.06 mM), Sonication is recommended.

References and Literature

1. Sanger, G.J., et al., GSK962040: a small molecule, selective motilin receptor agonist, effective as a stimulant of human and rabbit gastrointestinal motility. Neurogastroenterol Motil, 2009. 21(6): p. 657-64, e30-1. 2. Leming, S., et al., GSK962040: a small molecule motilin receptor agonist which increases gastrointestinal motility in conscious dogs. Neurogastroenterol Motil, 2011. 23(10): p. 958-e410. 3. Westaway, S.M., et al., Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-pi peridinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate. J Med Chem, 2009. 52(4): p. 1180-9. 4. Broad, J., et al., Regional- and agonist-dependent facilitation of human neurogastrointestinal functions by motilin receptor agonists. Br J Pharmacol, 2012. 167(4): p. 763-74.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library GPCR Compound Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Bioactive Compound Library Clinical Compound Library ReFRAME Related Library Bioactive Compounds Library Max

Related Products

Related compounds with same targets

[Leu13]-Motilin Motilin (26-47), human, porcine

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Keywords

Camicinal hydrochloride 923565-22-4 GPCR/G Protein Others Motilin Receptor GSK962040 Hydrochloride GSK962040 Inhibitor GSK-962040 Hydrochloride GSK 962040 GSK962040 hydrochloride Camicinal MLNR Camicinal Hydrochloride GSK-962040 inhibit GSK 962040 Hydrochloride inhibitor

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