Benzonitrile, 3-[4-(4-amino-1-piperidinyl)-3-(3,5-difluorophenyl)-6-quinolinyl]-2-hydroxy-
- Product Name
- Benzonitrile, 3-[4-(4-amino-1-piperidinyl)-3-(3,5-difluorophenyl)-6-quinolinyl]-2-hydroxy-
- 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;Paltusotine CRN00808;3-(4-(4-Aminopiperidin-1-yl)-3-(3,5-difluorophenyl)quinolin-6-yl)-2-hydroxybenzonitrile;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
- Formula Weight
- 456.49
- MOL File
- 2172870-89-0.mol
Benzonitrile, 3-[4-(4-amino-1-piperidinyl)-3-(3,5-difluorophenyl)-6-quinolinyl]-2-hydroxy- Property
- 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
- pka
- 5.89±0.35(Predicted)
- form
- Solid
- 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 and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P501Dispose of contents/container to..…
Benzonitrile, 3-[4-(4-amino-1-piperidinyl)-3-(3,5-difluorophenyl)-6-quinolinyl]-2-hydroxy- Chemical Properties,Usage,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
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