Benzonitrile, 3-[4-(4-amino-1-piperidinyl)-3-(3,5-difluorophenyl)-6-quinolinyl]-2-hydroxy-
![Benzonitrile, 3-[4-(4-amino-1-piperidinyl)-3-(3,5-difluorophenyl)-6-quinolinyl]-2-hydroxy- Structure](CAS/20210305/GIF/2172870-89-0.gif)
- CAS No.
- 2172870-89-0
- Chemical Name:
- Benzonitrile, 3-[4-(4-amino-1-piperidinyl)-3-(3,5-difluorophenyl)-6-quinolinyl]-2-hydroxy-
- 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
- CBNumber:
- CB29377677
- Molecular Formula:
- C27H22F2N4O
- Molecular Weight:
- 456.49
- MDL Number:
- MFCD34470008
- MOL File:
- 2172870-89-0.mol
Benzonitrile, 3-[4-(4-amino-1-piperidinyl)-3-(3,5-difluorophenyl)-6-quinolinyl]-2-hydroxy- Properties
Boiling point | 640.4±55.0 °C(Predicted) |
---|---|
Density | 1.41±0.1 g/cm3(Predicted) |
pka | 5.89±0.35(Predicted) |
form | Solid |
color | White to yellow |
FDA UNII | F2IBD1GMD3 |
Benzonitrile, 3-[4-(4-amino-1-piperidinyl)-3-(3,5-difluorophenyl)-6-quinolinyl]-2-hydroxy- Chemical Properties,Uses,Production
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
Benzonitrile, 3-[4-(4-amino-1-piperidinyl)-3-(3,5-difluorophenyl)-6-quinolinyl]-2-hydroxy- Preparation Products And Raw materials
Raw materials
Preparation Products
Benzonitrile, 3-[4-(4-amino-1-piperidinyl)-3-(3,5-difluorophenyl)-6-quinolinyl]-2-hydroxy- Suppliers
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TargetMol Chemicals Inc. | support@targetmol.com | United States | 38663 | 58 | |
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ShangHai Caerulum Pharma Discovery Co., Ltd. | 18149758185 18149758185 | sales-cpd@caerulumpharma.com | China | 3466 | 58 |
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