ChemicalBook--->CAS DataBase List--->1024033-43-9

1024033-43-9

1024033-43-9 Structure

1024033-43-9 Structure
IdentificationBack Directory
[Name]

AZD 4017
[CAS]

1024033-43-9
[Synonyms]

AZD 4017
EOS-62043
AZD 4017 (AZD4017)
AZD 4017,inhibit,AZD4017,Inhibitor,AZD-4017
(S)-2-(1-(5-(Cyclohexylcarbamoyl)-6-(propylthio)pyridin-2-yl)piperidin-3-yl)acetic acid
2-[(3s)-1-[5-(cyclohexylcarbamoyl)-6-propylsulfanylpyridin-2-yl]piperidin-3-yl]acetic Acid
3-Piperidineacetic acid, 1-[5-[(cyclohexylaMino)carbonyl]-6-(propylthio)-2-pyridinyl]-, (3S)-
(S)-2-(1-(5-(CYCLOHEXYLCARBAMOYL)-6-(PROPYLTHIO)PYRIDIN-2-YL)PIPERIDIN-3-YL) ACETIC ACID (AZD 4017)
[Molecular Formula]

C22H33N3O3S
[MDL Number]

MFCD25976912
[MOL File]

1024033-43-9.mol
[Molecular Weight]

419.58
Chemical PropertiesBack Directory
[Boiling point ]

654.7±55.0 °C(Predicted)
[density ]

1.22±0.1 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

Soluble in DMSO
[form ]

Solid
[pka]

4.65±0.10(Predicted)
[color ]

Light yellow to yellow
Safety DataBack Directory
[Symbol(GHS) ]


GHS07
[Signal word ]

Warning
[Hazard statements ]

H302
[Precautionary statements ]

P264-P270-P301+P312-P330-P501
[HS Code ]

2933399990
Hazard InformationBack Directory
[Uses]

AZD 4017 is a potent, selective 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) inhibitor, with an IC50 of 7 nM.
[in vivo]

Since AZD 4017 has lower potency against the mouse enzyme, only a limited number of preclinical pharmacodynamic measurements are performed. Increasing the dose further led to a maximal effect of approximately 70% inhibition at 1500 mg/kg, equivalent to 10×IC50 in the mouse, demonstrating the dose dependent inhibition of 11β-HSD1 by AZD 4017 in this model[1].

[References]

[1] Scott JS, et al. Discovery of a potent, selective, and orally bioavailable acidic 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor: discovery of 2-[(3S)-1-[5-(cyclohexylcarbamoyl)-6-propylsulfanylpyridin-2-yl]-3-piperidyl]acetic acid (AZD4017). J Med Chem. 2012 Jun 28;55(12):5951-64. DOI:10.1021/jm300592r
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