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ChemicalBook--->CAS DataBase List--->1146594-87-7

1146594-87-7

1146594-87-7 Structure

1146594-87-7 Structure
IdentificationBack Directory
[Name]

2-(S)-(3,5-Bis(4-(trifluoromethyl)phenyl)phenyl)-4-methylpentanoic acid
[CAS]

1146594-87-7
[Synonyms]

JNJ 40418677,JNJ40418677
JNJ-40418677 >=98% (HPLC)
2-(S)-(3,5-Bis(4-(trifluoromethyl)phenyl)phenyl)-4-methylpentanoic acid
[1,1':3',1''-Terphenyl]-5'-acetic acid, α-(2-methylpropyl)-4,4''-bis(trifluoromethyl)-, (αS)-
[Molecular Formula]

C26H22F6O2
[MOL File]

1146594-87-7.mol
[Molecular Weight]

480.44
Chemical PropertiesBack Directory
[Boiling point ]

514.9±50.0 °C(Predicted)
[density ]

1.258±0.06 g/cm3(Predicted)
[storage temp. ]

2-8°C
[solubility ]

DMSO: soluble15mg/mL, clear
[form ]

powder
[pka]

4.21±0.42(Predicted)
[color ]

white to beige
Safety DataBack Directory
[Symbol(GHS) ]


GHS06
[Signal word ]

Danger
[Hazard statements ]

H300-H413
[Precautionary statements ]

P264-P270-P273-P301+P310-P405-P501
[Hazard Codes ]

T
[Risk Statements ]

25
[Safety Statements ]

45
[RIDADR ]

UN 2811 6.1 / PGIII
[WGK Germany ]

3
Hazard InformationBack Directory
[Uses]

2-(S)-(3,5-Bis(4-(trifluoromethyl)phenyl)phenyl)-4-methylpentanoic Acid is a therapeutic agent used in the treatment of Alzheimer’s.
[Biological Activity]

JNJ-40418677 is a γ-secretase modulator th at selectively blocks γ-site cleavage of the APP without affecting processing of Notch. In human neuroblastoma cells and r at primary neuronal culturesJNJ-40418677 blocked secretion of Aβb42 (IC50 = 20 nM)with no affects on total Ab concentrationNotch signaling or COX activity. In vivo experiments showed th at JNJ-40418677 dose dependently inhibited Aβ42 accumulation in the brain while promoting an increase in Aβ38.
[in vivo]

JNJ-40418677 (10-300 mg/kg; p.o.) decreases Aβ42 brain levels in a dose-dependent manner 4 h after treatment, while increasing Aβ38 level in non-transgenic mouse brain[1].
JNJ-40418677 (30 mg/kg; p.o.; once) shows the mean brain and plasma levels 4 h after single dose are both 17 μM, indicating good brain penetration in non-transgenic mouse brain[1].
JNJ-40418677 (20-120 mg/kg; p.o.; 7 months) has good biological tolerance with no adverse effects in a chronic treatment in Tg2576 mice[1].
JNJ-40418677 (20-120 mg/kg; p.o.; 7 months) decreases the plaque number and the area occupied by plaques in Tg2576 mice dose-dependently[1].

Animal Model:Non-transgenic mouse (6-month-old)[1]
Dosage:10, 30, 100, 300 mg/kg
Administration:Oral gavage; once
Result:Reduced the Aβ42 brain levels dose-dependently, with 82%, 64%, 39%, and 31% at the doses of 10, 30, 100, 300 mg/kg, respectively.
Animal Model:Tg2576 mice (6-month-old)[1]
Dosage:20, 60, 120 mg/kg
Administration:Oral gavage; 7 months
Result:Exhibited well tolerated activity, without adverse effects on body weight.
Showed no influence on the steady state levels of full-length APP, CTF-a, and CTF-b at a dosage of 120 mg/kg.
Significantly reduced plaque area fraction and number of plaques.
[storage]

Store at -20°C
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