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KAR-5417

Chemical Structure : KAR-5417

CAS No.: 1673568-73-4

KAR-5417 (KAR5417)

Catalog No.: PC-62807Not For Human Use, Lab Use Only.

KAR-5417 is a potent, selective TPH1 (tryptophan hydroxylase-1) inhibitor with IC50 of 33 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

KAR-5417 is a potent, selective TPH1 (tryptophan hydroxylase-1) inhibitor with IC50 of 33 nM; also shows potent inhibition of TPH2 (IC50=7 nM), an enzyme responsible for 5-HT production in the CNS, KAR5417 is found to be essentially confined to peripheral tissues in rats; produces robust 5-HT reduction in mice intestinal mucosa.

Physicochemical Properties

M.Wt 561.99
Formula C27H27ClF3N5O3
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

(S)-8-(2-amino-6-((R)-1-(5-chloro-[1,1'-biphenyl]-2-yl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)-2,8-diazaspiro[4.5]decane-3-carboxylic acid

References

1. Goldberg DR, et al. Bioorg Med Chem Lett. 2017 Feb 1;27(3):413-419.

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