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TPT-004

Chemical Structure : TPT-004

CAS No.:

TPT-004 (TPT004)

Catalog No.: PC-21320Not For Human Use, Lab Use Only.

TPT-004 is a highly potent, selective tryptophan hydroxylase (TPH) with IC50 of 77 nM and 16 nM for TPH1 and TPH2, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

TPT-004 is a highly potent, selective tryptophan hydroxylase (TPH) with IC50 of 77 nM and 16 nM for TPH1 and TPH2, respectively.
TPT-004 displays no relevant impact at 20 μM on the function of the LAT1 transporter involved in the transport of tryptophan, phenylalanine, leucine, and histidine to the brain.
TPT-004 reduced the intracellular serotonin levels with IC50 of 0.952 uM in serotonergic BON cells, a human carcinoid cell line known to express TPH1.
TPT-004 showed efficacy in preclinical models of peripheral serotonin attenuation and colorectal tumor growth.

Physicochemical Properties

M.Wt 400.46
Formula C18H20N6O3S
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

3-Ethyl-8-((2-methylimidazo[2,1-b]thiazol-6-yl)methyl)-7-(oxetan-3-ylmethyl)-3,7-dihydro-1H-purine-2,6-dione

References

1. Edgar Specker, et al. J Med Chem. 2023 Nov 9;66(21):14866-14896.

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