Netupitant (Synonyms: Ro 6731898/000) |
Catalog No.GC17596
One-Click Copy Product Info
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Netupitant (CID-6451149) es un antagonista del receptor de neuroquinina-1 (NK1) muy potente, selectivo y activo por vÍa oral con una Ki de 0,95 nM para hNK1 en células CHO.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 290297-26-6
Sample solution is provided at 25 µL, 10mM.
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Netupitant (CID-6451149) is a highly potent and selective, orally active neurokinin-1 receptor antagonist with Ki of 0.95 nM.IC50 value: 0.95 nM (Ki) [1]Target: NK1 receptorin vitro: Netupitant also dose-dependently inhibited the SP response as expected from an NK1 receptor antagonist. Importantly, when both palonosetron and netupitant were present, they exhibited an enhanced inhibition of the SP response compared to either of the two antagonists alone [2].in vivo: In mice the intrathecal injection of SP elicited the typical scratching, biting and licking response that was dose-dependently inhibited by Netupitant given intraperitoneally in the 1-10mg/kg dose range. In gerbils, foot tapping behavior evoked by the intracerebroventricular injection of a NK(1) agonist was dose-dependently counteracted by Netupitant given intraperitoneally (ID(50) 1.5mg/kg) or orally (ID(50) 0.5mg/kg) [3].
References:
[1]. Hoffmann T, et al. Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1362-5.
[2]. Stathis M, et al. Inhibition of substance P-mediated responses in NG108-15 cells by netupitant and palonosetron exhibit synergistic effects. Eur J Pharmacol. 2012 Aug 15;689(1-3):25-30.
[3]. Rizzi A, et al. In vitro and in vivo pharmacological characterization of the novel NK1 receptor selective antagonist Netupitant. Peptides. 2012 Sep;37(1):86-97.
[4]. Ajit G. Thomas, et al. Netupitant and palonosetron trigger NK1 receptor internalization in NG108-15 cells. Exp Brain Res. 2014; 232(8): 2637–2644.
| Cas No. | 290297-26-6 | SDF | |
| Sinónimos | Ro 6731898/000 | ||
| Chemical Name | 2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethyl-N-(6-(4-methylpiperazin-1-yl)-4-(o-tolyl)pyridin-3-yl)propanamide | ||
| Canonical SMILES | CC1=CC=CC=C1C2=CC(N3CCN(CC3)C)=NC=C2N(C(C(C)(C4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4)C)=O)C | ||
| Formula | C30H32F6N4O | M.Wt | 578.59 |
| Solubility | DMSO : 9.09 mg/mL (15.71 mM; ultrasonic and warming and heat to 60°C) | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7283 mL | 8.6417 mL | 17.2834 mL |
| 5 mM | 345.7 μL | 1.7283 mL | 3.4567 mL |
| 10 mM | 172.8 μL | 864.2 μL | 1.7283 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
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 saline, 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: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 8 reference(s) in Google Scholar.)