For research use only. Not for therapeutic Use.
Paltusotine (CRN00808) is an orally active, nonpeptide selective somatostatin type 2 (SST2) receptor agonist. Paltusotine has the potential for maintaining GH and IGF-1 levels after depot somatostatin receptor ligand therapy.Paltusotine can be used in research on acromegaly and neuroendocrine tumors[1][2][3].
Paltusotine (3 10, 30 mg/kg, oral, single dose) inhibit growth hormone (GH) secretion induced by exogenous growth hormone releasing hormone (GHRH) stimulation in both male and female rats[3].
| Catalog Number | I034181 |
| CAS Number | 2172870-89-0 |
| Synonyms | 3-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorophenyl)quinolin-6-yl]-2-hydroxybenzonitrile |
| Molecular Formula | C27H22F2N4O |
| Purity | ≥95% |
| InChI | InChI=1S/C27H22F2N4O/c28-19-10-18(11-20(29)13-19)24-15-32-25-5-4-16(22-3-1-2-17(14-30)27(22)34)12-23(25)26(24)33-8-6-21(31)7-9-33/h1-5,10-13,15,21,34H,6-9,31H2 |
| InChIKey | GHILNKWBALQPDP-UHFFFAOYSA-N |
| SMILES | C1CN(CCC1N)C2=C3C=C(C=CC3=NC=C2C4=CC(=CC(=C4)F)F)C5=CC=CC(=C5O)C#N |
| Reference | [1]. Murray B. Gordon, et al. Identification of a dose range for once daily oral paltusotine in patients with acromegaly that maintains IGF-1 levels when switching from long-acting somatostatin receptor ligand therapy. Endocrine Abstracts (2021) 73 OC15.4. [2]. Rosa Luo, et al. Pharmacokinetics and Safety of an Improved Oral Formulation of Paltusotine, a Selective, Non-Peptide Somatostatin Receptor 2 (SST2) Agonist for the Treatment of Acromegaly. Journal of the Endocrine Society, Volume 5, Issue Supplement_1, April-May 2021. [3]. Zhao J, et al. Discovery of Paltusotine (CRN00808), a Potent, Selective, and Orally Bioavailable Non-peptide SST2 Agonist. ACS Med Chem Lett. 2022 Dec 10;14(1):66-74. |
