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Tradipitant

Chemical Structure : Tradipitant

CAS No.: 622370-35-8

Tradipitant (VLY-686, LY686017)

Catalog No.: PC-38599Not For Human Use, Lab Use Only.

Tradipitant (VLY-686, LY686017) is a selective, orally bioavailable, centrally-acting neurokinin-1 receptor (NK1) antagonist with potential anti-emetic, anti-pruritic and anti-inflammatory activities.

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Biological Activity

Tradipitant (VLY-686, LY686017) is a selective, orally bioavailable, centrally-acting neurokinin-1 receptor (NK1) antagonist with potential anti-emetic, anti-pruritic and anti-inflammatory activities.
Tradipitant competitively binds to and blocks the activity of the NK1R in the central nervous system (CNS), thereby inhibiting the binding of the endogenous ligand and neuropeptide, substance P (SP; neurokinin-1; NK1).
Tradipitant inhibits SP/NK1-mediated signal transduction and may prevent both SP-induced emesis and pruritis, also reduces neurogenic inflammation which is triggered by the release of neuropeptides, such as substance P, from nerve cells.

Physicochemical Properties

M.Wt 587.9
Formula C28H16ClF6N5O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(2-(1-(3,5-bis(trifluoromethyl)benzyl)-5-(pyridin-4-yl)-1H-1,2,3-triazol-4-yl)pyridin-3-yl)(2-chlorophenyl)methanone

References

1. Coe MA, et al. Psychopharmacology (Berl). 2021 Jul;238(7):1857-1866.

2. Polymeropoulos VM, et al. Front Neurol. 2020 Sep 29;11:563373.

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