GSK962040 (Synonyms: GSK962040) |
| Catalog No.GC16491 |
GSK962040 (GSK962040) is a small molecule, selective motilin receptor agonist with pEC50 of 7.9.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 923565-21-3
Sample solution is provided at 25 µL, 10mM.
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GSK962040 is a first small-molecule agonist of motilin receptor with pEC50 value of 7.9 [1].
GSK962040 is discovered as a therapeutic agent for conditions associated with delayed gastric emptying. In the in vitro assay using recombinant human motilin receptor, GSK962040 shows an excellent inhibition activity against motilin receptor with pEC50 value of 7.9. GSK962040 is highly selective against motilin receptor over the human ghrelin receptor and hERG. It also has no significant activity against other receptors including 5-HT, adrenergic, dopamine, histamine and adenosine receptors. In rabbit isolated gastric antrum, GSK962040 is found to enhance the EFS-induced cholinergic contraction and cause a small muscle contraction at high concentration. GSK962040 also induces the contraction of human-isolated stomach preparations at 10μM [1, 2].
References:
[1] Westaway S M, Brown S L, Fell S C M, et al. Discovery of N-(3-Fluorophenyl)-1-[(4-([(3 S)-3-methyl-1-piperazinyl] methyl) phenyl) acetyl]-4-piperidinamine (GSK962040), the First Small Molecule Motilin Receptor Agonist Clinical Candidate. Journal of medicinal chemistry, 2009, 52(4): 1180-1189.
[2] Sanger G J, Westaway S M, Barnes A A, et al. GSK962040: a small molecule, selective motilin receptor agonist, effective as a stimulant of human and rabbit gastrointestinal motility. Neurogastroenterology & Motility, 2009, 21(6): 657-e31.
| Cas No. | 923565-21-3 | SDF | |
| Synonyms | GSK962040 | ||
| Chemical Name | 1-[4-(3-fluoroanilino)piperidin-1-yl]-2-[4-[[(3S)-3-methylpiperazin-1-yl]methyl]phenyl]ethanone | ||
| Canonical SMILES | CC1CN(CCN1)CC2=CC=C(C=C2)CC(=O)N3CCC(CC3)NC4=CC(=CC=C4)F | ||
| Formula | C25H33FN4O | M.Wt | 424.55 |
| Solubility | DMSO : 100 mg/mL (235.54 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 | 2.3554 mL | 11.7772 mL | 23.5544 mL |
| 5 mM | 0.4711 mL | 2.3554 mL | 4.7109 mL |
| 10 mM | 0.2355 mL | 1.1777 mL | 2.3554 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
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 23 reference(s) in Google Scholar.)
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