2. GPCR/G Protein Neuronal Signaling
  3. Neurokinin Receptor
  4. Tradipitant

Tradipitant  (Synonyms: VLY-686; LY686017)

Cat. No.: HY-16732 Purity: 99.66%
COA Handling Instructions

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Tradipitant (VLY-686) is a neurokinin-1 (NK-1) antagonist.

For research use only. We do not sell to patients.

Tradipitant Chemical Structure

Tradipitant Chemical Structure

CAS No. : 622370-35-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 194 In-stock
Solution
10 mM * 1 mL in DMSO USD 194 In-stock
Solid
1 mg USD 71 In-stock
5 mg USD 150 In-stock
10 mg USD 250 In-stock
50 mg   Get quote  
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Customer Review

Based on 1 publication(s) in Google Scholar

Tradipitant Related Antibodies

Top Publications Citing Use of Products

View All Neurokinin Receptor Isoform Specific Products:

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Tradipitant (VLY-686) is a neurokinin-1 (NK-1) antagonist.

IC50 & Target

NK-1[1]
In Vitro

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.

Tradipitant Related Antibodies
In Vivo

Autoradiography experiments reveal that intravenously administered Tradipitant ([3H]-LY686017) localizes in the guinea pig brain and has a distribution similar to that described for the NK-1 receptor using agonist or antagonist radioligands[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

587.90

Formula

C28H16ClF6N5O
CAS No.
Appearance

Solid

Color

Light brown to gray

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7010 mL 8.5048 mL 17.0097 mL
5 mM 0.3402 mL 1.7010 mL 3.4019 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.25 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.66%

COA (259 KB) LCMS (96 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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
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
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Tradipitant Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tradipitant622370-35-8VLY-686 LY686017VLY686VLY 686LY686017LY 686017LY-686017Neurokinin ReceptorNK receptorTachykinin receptorInhibitorinhibitorinhibit

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