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Camicinal

Catalog No. T11508 CAS 923565-21-3

Synonyms: GSK962040

Camicinal is a selective motilin receptor agonist (pEC50: 7.9).

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Camicinal, CAS 923565-21-3

Pack Size	Availability	Price/USD
2 mg	6-8 weeks	$ 198.00
5 mg	6-8 weeks	$ 347.00
25 mg	6-8 weeks	$ 1,140.00
50 mg	6-8 weeks	$ 1,490.00
100 mg	6-8 weeks	$ 1,990.00
1 mL * 10 mM (in DMSO)	6-8 weeks	$ 382.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Camicinal is a selective motilin receptor agonist (pEC50: 7.9).
Targets&IC50	Motilin receptor:(pEC50)7.9
In vitro	Camicinal ?had no significant activity at a range of other receptors (including ghrelin), ion channels and enzymes. In rabbit gastric antrum, Camicinal ?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 ?were, respectively, 10.4 ± 0.01 (n = 770), 7.3 ± 0.29 (n = 4) and 7.9 ± 0.09 (n = 17) . Camicinal ?activated the dog motilin receptor (pEC50 5.79; intrinsic activity 0.72, compared with [Nle13]-motilin) . Camicinal ?was preferred because its initial IC50 values at CYP3A4 were significantly higher than our preferred threshold of 10 μM .
In vivo	Camicinal (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 1.14 μmol L 1.?After the effects of GSK962040 faded, migrating motor complex (MMC) activity returned.?Migrating motor complex restoration was unaffected by 3 mg kg 1 GSK962040 but at 6 mg kg 1, MMCs returned 253 min after dosing, compared with 101 min after saline (n = 5 each) .?he oral bioavailability (Fpo) of Camicinal (GSK962040) was found to be 48 ( 13%.?Camicinal ?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 ?strongly facilitated cholinergic activity in the antrum, with lower activity in fundus and small intestine only .

Synonyms	GSK962040
Molecular Weight	424.55
Formula	C25H33FN4O
CAS No.	923565-21-3

Storage

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

Solubility Information

DMSO: 100 mg/mL (235.54 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.

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Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Keywords

Camicinal 923565-21-3 Others GSK962040 GSK-962040 GSK 962040 inhibitor inhibit

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