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

Product Name2-(S)-(3,5-Bis(4-(trifluoromethyl)phenyl)phenyl)-4-methylpentanoic acid
CAS1146594-87-7
MFC26H22F6O2
MW480.44
EINECS
MOL File1146594-87-7.mol

Chemical Properties

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 Information

Hazard Codes	T
Risk Statements	25
Safety Statements	45
RIDADR	UN 2811 6.1 / PGIII
WGK Germany	3
Storage Class	6.1A - Combustible acute toxic Cat. 1 and 2 very toxic hazardous materials
Hazard Classifications	Acute Tox. 2 Oral Aquatic Chronic 4

Usage And Synthesis

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 cultures, JNJ-40418677 blocked secretion of Aβb42 (IC50 = 20 nM), with no affects on total Ab concentration, Notch 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.

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