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Paltusotine

Chemical Structure : Paltusotine

CAS No.: 2172870-89-0

Paltusotine (CRN00808, CRN 00808)

Catalog No.: PC-38007Not For Human Use, Lab Use Only.

Paltusotine (CRN00808) is an orally bioavailable, nonpeptide, somatostatin receptor subtype 2 (SST2) agonist with EC50 of 0.25 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Paltusotine (CRN00808) is an orally bioavailable, nonpeptide, somatostatin receptor subtype 2 (SST2) agonist with EC50 of 0.25 nM.
Paltusotine is >4000-fold selective for SST2 over other somatostatin receptor subtypes.
Paltusotine suppresses stimulated-GH and IGF-1 secretion in rats. Paltusotine suppresses GH and IGF-1 in a dose-dependent fashion, with a safety profile similar to currently approved SST2 receptor ligands.
Paltusotine is a promising once-daily oral nonpeptide SST2 agonist candidate for managing acromegaly and neuroendocrine tumors.

Physicochemical Properties

M.Wt 456.497
Formula C27H22F2N4O
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-(4-(4-aminopiperidin-1-yl)-3-(3,5-difluorophenyl)quinolin-6-yl)-2-hydroxybenzonitrile

References

1. Gadelha MR, et al. J Clin Endocrinol Metab. 2022 Jan 18;107(2):297-308.

2. Madan A, et al. Pituitary. 2022 Apr;25(2):328-339.

3.  Betz SF, et al. Endocrine Rev. 2018;39(2):i1-i1417.

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