| Identification | Back Directory | [Name]
Benzonitrile, 3-[4-(4-amino-1-piperidinyl)-3-(3,5-difluorophenyl)-6-quinolinyl]-2-hydroxy- | [CAS]
2172870-89-0 | [Synonyms]
CRN00808
CRN-00808
CRN 00808
Paltusotine
Benzonitrile, 3-[4-(4-amino-1-piperidinyl)-3-(3,5-difluorophenyl)-6-quinolinyl]-2-hydroxy-
Paltusotine,Somatostatin Receptor,CRN-00808,CRN 00808,Inhibitor,IGF-1,orally,CRN00808,SSTR,inhibit,SSTRs | [Molecular Formula]
C27H22F2N4O | [MDL Number]
MFCD34470008 | [MOL File]
2172870-89-0.mol | [Molecular Weight]
456.49 |
| Chemical Properties | Back Directory | [Boiling point ]
640.4±55.0 °C(Predicted) | [density ]
1.41±0.1 g/cm3(Predicted) | [solubility ]
DMSO: Slightly soluble: 0.1-1 mg/ml | [form ]
Solid | [pka]
5.89±0.35(Predicted) | [color ]
White to yellow | [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]
C(#N)C1=CC=CC(C2=CC=C3C(=C2)C(N2CCC(N)CC2)=C(C2=CC(F)=CC(F)=C2)C=N3)=C1O |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
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].
| [References]
[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. DOI:10.1021/acsmedchemlett.2c00431 |
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