Tradipitant
Based on 1 Customer Validation
Tradipitant (VLY-686) is a neurokinin-1 (NK-1) antagonist.
For research use only. We do not sell to patients.
- Purity: 99.95%
- CAS No.: 622370-35-8
- Formula: C28H16ClF6N5O
- Molecular Weight:587.90
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
NK-1[1]
Results reveal that Tradipitant ([3H]-LY686017) bind to sections of guinea pig brain with a distribution similar to that previously reported for NK-1 receptors. Areas with the highest density are the accessory olfactory nucleus, anteroventral thalamic nucleus, paraventricular hypothalamic nucleus central amygdaloid nucleus (lateral) and the medial amygdaloid nucleus (anterodorsal)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 622370-35-8
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Appearance Solid
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Molecular Weight 587.90
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Formula C28H16ClF6N5O
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Color Light brown to gray
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SMILES
O=C(C1=CC=CN=C1C2=C(C3=CC=NC=C3)N(CC4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4)N=N2)C5=CC=CC=C5Cl
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Synonyms
VLY-686; LY686017
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : 100 mg/mL (170.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Brains from male, Hartley guinea pigs (350 to 400 g) are removed, rinsed for 5 to 15 min in cold PBS, patted dry with a paper towel and frozen on aluminum foil lined with parafilm placed on dry ice. Once frozen, the brains are stored at -80°C until they are sectioned using a cryostat set at a thickness of 12 μm. The tissue sections are thaw mounted onto chrome alum/gelatin coated slides and allowed to air dry for 5 to 20 min before being frozen again. To assess the binding of Tradipitant ([3H]-LY686017) to sections, the slides are preincubated for 30 min in modified Kreb’s phosphate buffer followed by an incubation in the same buffer containing 0.05% bacitracin, 0.4% BSA and various concentrations of Tradipitant. Rinse time, incubation time and saturation binding are determined using sections through the caudate nucleus[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Male, Hartley guinea pigs (550 to 650 g) are used. Guinea pigs are singly housed in cages for 2 to 4 days before being used in an experiment. On the day of the experiment, the catheters are flushed with heparinized 0.9% saline and, if the catheter is clear, the animal received 25 microCi of Tradipitant ([3H]-LY686017) in saline for time course and compound displacement studies (n=4 to 6/group) and 100 microCi for autoradiography studies (n=5). The catheter line is cleared of radioactivity by again flushing the line with 0.5 mL heparinized saline. The end of the catheter is subsequently plugged using the original steel wire plug. Based on data from initial time course experiments, the animals are sacrificed by rapid decapitation 2 h post-jugular injection for compound displacement and autoradiography studies[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.7010 mL | 8.5048 mL | 17.0097 mL | 42.5242 mL |
| 5 mM | 0.3402 mL | 1.7010 mL | 3.4019 mL | 8.5048 mL | |
| 10 mM | 0.1701 mL | 0.8505 mL | 1.7010 mL | 4.2524 mL | |
| 15 mM | 0.1134 mL | 0.5670 mL | 1.1340 mL | 2.8349 mL | |
| 20 mM | 0.0850 mL | 0.4252 mL | 0.8505 mL | 2.1262 mL | |
| 25 mM | 0.0680 mL | 0.3402 mL | 0.6804 mL | 1.7010 mL | |
| 30 mM | 0.0567 mL | 0.2835 mL | 0.5670 mL | 1.4175 mL | |
| 40 mM | 0.0425 mL | 0.2126 mL | 0.4252 mL | 1.0631 mL | |
| 50 mM | 0.0340 mL | 0.1701 mL | 0.3402 mL | 0.8505 mL | |
| 60 mM | 0.0283 mL | 0.1417 mL | 0.2835 mL | 0.7087 mL | |
| 80 mM | 0.0213 mL | 0.1063 mL | 0.2126 mL | 0.5316 mL | |
| 100 mM | 0.0170 mL | 0.0850 mL | 0.1701 mL | 0.4252 mL |
Tradipitant Related Classifications
HY-16732 Related Classifications
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