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Tradipitant

Cat. No. M30382
Tradipitant Structure
Synonym:

VLY-686; LY686017

Size Price Availability Quantity
5mg USD 140  USD140 In stock
10mg USD 225  USD225 In stock
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Quality Control & Documentation
Biological Activity

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

Chemical Information
Molecular Weight 587.9
Formula C28H16ClF6N5O
CAS Number 622370-35-8
Form Solid
Solubility (25°C) DMSO 100 mg/mL (ultrasonic)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Eli D Ehrenpreis, et al. Aliment Pharmacol Ther. Editorial: tradipitant has promise for treating gastroparesis but leaves gastric function alone

[2] Michael Camilleri, et al. Aliment Pharmacol Ther. Editorial: tradipitant has promise for treating gastroparesis but leaves gastric function alone-authors' reply

[3] Vasilios M Polymeropoulos, et al. Front Neurol. Tradipitant in the Treatment of Motion Sickness: A Randomized, Double-Blind, Placebo-Controlled Study

[4] Jesse L Carlin, et al. Gastroenterology. Efficacy and Safety of Tradipitant in Patients With Diabetic and Idiopathic Gastroparesis in a Randomized, Placebo-Controlled Trial

[5] Chia-Yu Chu. Clin Rev Allergy Immunol. Treatments for Childhood Atopic Dermatitis: an Update on Emerging Therapies

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Keywords: Tradipitant, VLY-686; LY686017 supplier, Neurokinin Receptor, inhibitors, activators


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