96-98 °C
MP: 72-74 °C from methanol. /Cis-Form base/
MP: 126-128 °C; C32-H37-N-08; ICI-47699 /Cis-Form citrate/
97 °C
Physical Description
Solid
Appearance
Crystals from petroleum ether.
State
Solid
Computed Properties
Structural Parameters
Heavy atom count
28
Aromatic heavy atom count
18
Fraction Csp3
0.23
Rotatable bonds
8
H-bond acceptors
2
Molar refractivity
119.58
TPSA
12.47
LogP / Solubility
WLOGP
6
MLOGP
5.3
XLogP3
7.1
Consensus LogP
6.13
Log S (ESOL)
-5.87
Class (ESOL)
Slightly soluble
Log S (Ali)
-6.94
Class (Ali)
Insoluble
Log S (SILICOS-IT)
-8.01
Class (SILICOS-IT)
Insoluble
ADME
GI absorption
Low
BBB permeant
No
P-gp substrate
No
CYP1A2 inhibitor
Yes
CYP2C19 inhibitor
Yes
CYP2C9 inhibitor
Yes
CYP2D6 inhibitor
Yes
CYP3A4 inhibitor
Yes
Log Kp (skin permeation)
-0.73
Drug-likeness / Medicinal Chemistry
Lipinski
Yes
Ghose
No
Veber
Yes
Egan
No
Muegge
No
Bioavailability score
0.55
Brenk alerts
1
Leadlikeness
No
Synthetic Accessibility
2.5
Safety & Transport
Pictogram(s)
Irritant
Health Hazard
Environmental Hazard
Signal
Danger
GHS Hazard Statements
H302 (58.3%): Harmful if swallowed [Warning Acute toxicity, oral]
H350 (100%): May cause cancer [Danger Carcinogenicity]
H360 (91.7%): May damage fertility or the unborn child [Danger Reproductive toxicity]
H362 (58.3%): May cause harm to breast-fed children [Reproductive toxicity, effects on or via lactation]
H372 (33.3%): Causes damage to organs through prolonged or repeated exposure [Danger Specific target organ toxicity, repeated exposure]