Tradipitant (VLY-686, LY686017)

Chemical Structure : Tradipitant

CAS No.: 622370-35-8

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货号: 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.

规格	价格	库存
5 mg	￥1280	In stock
10 mg	￥1980	In stock
25 mg	￥3280	In stock
50 mg	￥5280	In stock
100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	587.9
分子式	C28H16ClF6N5O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

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.