Pavinetant (MLE-4901) (Synonyms: AZD 2624, AZD 4901) |
| Catalog No.GC30861 |
Pavinetant (MLE-4901) (MLE-4901) es un antagonista del receptor de neuroquinina-3 (NK3R).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 941690-55-7
Sample solution is provided at 25 µL, 10mM.
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Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist.
Pavinetant (AZD2624) is a potent and selective NK3 receptor antagonist which is developed for the treatment of schizophrenia. Pavinetant exhibits an inhibitory effect on microsomal CYP3A4/5 activities with apparent IC50 values of 7.1 and 19.8 μM for midazolam and testosterone assays, respectively. No time-dependent inactivation of CYP3A4/5 activity by Pavinetant is observed. Pavinetant demonstrates weak to no inhibition of CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, and CYP2D6[1].
[1]. Li Y, et al. In vitro assessment of metabolic drug-drug interaction potential of AZD2624, neurokinin-3 receptor antagonist, through cytochrome P(450) enzyme identification, inhibition, and induction studies. Xenobiotica. 2010 Nov;40(11):721-9.
Kinase experiment: | The potential of Pavinetant (AZD2624) to cause time-dependent inhibition of CYP3A activities is evaluated by pre-incubating 10 μM of Pavinetant at 37°C for 0, 3, 10, 20, and 30 min in 0.1 M pH 7.4 phosphate buffer incubation mixture (0.2 mL) containing 2 mg/mL HLM and 1 mM NADPH. Verapamil, tested at 10 μM, is also incubated separately as a positivecontrol. An aliquot of 20 μL is removed from pre-incubation tube at each time point and added to a secondary 5-min incubation(180 μL) containing 15 μM of midazolam and 1 mM of NADPH. The formation of 1′-hydroxymidazolam is used as the marker activity for CYP3A enzymes and analyzed using LC-MS. CYP3A enzyme activities after pre-incubation with Pavinetant arecompared to activities following incubation with vehicle solvent (1% methanol) and without pre-incubation[1]. |
References: [1]. Li Y, et al. In vitro assessment of metabolic drug–drug interaction potential of AZD2624, neurokinin-3 receptor antagonist, through cytochrome P(450) enzyme identification, inhibition, and induction studies. Xenobiotica. 2010 Nov;40(11):721-9. | |
| Cas No. | 941690-55-7 | SDF | |
| Sinónimos | AZD 2624, AZD 4901 | ||
| Canonical SMILES | CC[C@H](NC(C1=C(C=CC=C2)C2=NC(C3=CC=CC=C3)=C1NS(C)(=O)=O)=O)C4=CC=CC=C4 | ||
| Formula | C26H25N3O3S | M.Wt | 459.56 |
| Solubility | DMSO : ≥ 50 mg/mL (108.80 mM);Water : < 0.1 mg/mL (insoluble) | 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 | 2.176 mL | 10.88 mL | 21.7599 mL |
| 5 mM | 435.2 μL | 2.176 mL | 4.352 mL |
| 10 mM | 217.6 μL | 1.088 mL | 2.176 mL |
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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
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- Purity: >99.50%
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- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 24 reference(s) in Google Scholar.)
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