GSK962040 hydrochloride (Synonyms: GSK962040 hydrochloride) |
| Katalog-Nr.GC10609 |
GSK962040-Hydrochlorid (GSK962040-Hydrochlorid) ist ein niedermolekularer, selektiver Motilin-Rezeptor-Agonist mit einem pEC50-Wert von 7,9.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 923565-22-4
Sample solution is provided at 25 µL, 10mM.
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Camicinal hydrochloride (GSK962040 hydrochloride) is a small molecule, selective motilin receptor agonist with pEC50 of 7.9.
Camicinal hydrochloride (GSK962040 hydrochloride) had no significant activity at a range of other receptors (including ghrelin), ion channels and enzymes. In rabbit gastric antrum, Camicinal hydrochloride (GSK962040 hydrochloride) 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 hydrochloride (GSK962040 hydrochloride) were, respectively, 10.4 ± 0.01 (n = 770), 7.3 ± 0.29 (n = 4) and 7.9 ± 0.09 (n = 17) [1]. Camicinal hydrochloride (GSK962040 hydrochloride) activated the dog motilin receptor (pEC50 5.79; intrinsic activity 0.72, compared with [Nle13]-motilin) [2]. Camicinal hydrochloride (GSK962040 hydrochloride) was preferred because its initial IC50 values at CYP3A4 were significantly higher than our preferred threshold of 10 μM [3].
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 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:
[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.
| Cas No. | 923565-22-4 | SDF | |
| Überlieferungen | GSK962040 hydrochloride | ||
| Chemical Name | (S)-1-(4-((3-fluorophenyl)amino)piperidin-1-yl)-2-(4-((3-methylpiperazin-1-yl)methyl)phenyl)ethanone hydrochloride | ||
| Canonical SMILES | C[C@@]1([H])CN(CC2=CC=C(CC(N3CCC(NC4=CC=CC(F)=C4)CC3)=O)C=C2)CCN1.Cl | ||
| Formula | C25H34ClFN4O | M.Wt | 461.02 |
| Löslichkeit | H2O : 100 mg/mL (216.91 mM; Need ultrasonic); DMSO : 100 mg/mL (216.91 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1691 mL | 10.8455 mL | 21.691 mL |
| 5 mM | 0.4338 mL | 2.1691 mL | 4.3382 mL |
| 10 mM | 0.2169 mL | 1.0846 mL | 2.1691 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 2 reference(s) in Google Scholar.)
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