| Identification | Back 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 Properties | Back 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 |
| Hazard Information | Back 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 |
|
| Company Name: |
Lynnchem
|
| Telephone: |
86-(0)29-85992781 17792393971 |
| Website: |
http://www.lynnchem.com/ |
| Company Name: |
Energy Chemical
|
| Telephone: |
400-0056266 |
| Website: |
www.energy-chemical.com |
|