JNJ-40411813
JNJ-40411813 Basic information
- Product Name:
- JNJ-40411813
- Synonyms:
-
- 1-butyl-3-chloro-4-(4-phenylpiperidin-1-yl)pyridin-2(1H)-one
- 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-2(1H)-Pyridinone
- JNJ-40411813
- CS-1035
- JNJ 40411813;JNJ-40411813
- ADX 71149
- 2(1H)-Pyridinone, 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-
- 1-butyl-3-chloro-4-(4-phenylpiperidin-1-yl)pyridin-2-one
- CAS:
- 1127498-03-6
- MF:
- C20H25ClN2O
- MW:
- 344.88
- Mol File:
- 1127498-03-6.mol
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JNJ-40411813 Chemical Properties
- Boiling point:
- 463.5±45.0 °C(Predicted)
- Density
- 1.18±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:25.0(Max Conc. mg/mL);72.49(Max Conc. mM)
- form
- Solid
- pka
- 1.06±0.40(Predicted)
- color
- White to off-white
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JNJ-40411813 Usage And Synthesis
Uses
ADX 71149 is drug candidate; used in preparation of Bipyridinones as positive allosteric modulators of mGluR2 for treating neurological and psychiatric disorders.Also, use as a treatment for ADHD.
in vivo
JNJ-40411813 (ADX-71149) (5-20 mg/kg; p.o.; 6 times in 24 h) clearly potentiated glutamate response in brain regions, more specifically in the cortical regions, striatum, and the hippocampus, coaddition of Glutamate (HY-N0455B)[2].
Pharmacokinetic Analysis in SD rat[2]
| Route | Dose (mg/kg) | AUCINF_obs (ng·h/mL) | t1/2 (h) | Tmax (h) | Cmax (ng/mL) | Clobs (L·h/kg) | Vss_obs (L/kg) |
| i.v. | 2.5 | 1833±90 | / | / | / | 1.4±0.1 | 2.31.4±0.10.2 |
| p.o. | 10 | 2250±417 | 2.31±0.5 | 7 | 938 | / | / |
| Animal Model: | Male Wistar Rats (150 mg)[2] |
| Dosage: | 5 mg/kg, 20 mg/kg |
| Administration: | Oral Gavage (p.o.) |
| Result: | Showed increasing in basal binding with an EC50 of 48 μM and a Combined with 10 μM glutamate, [35S]GTPγS binding with an EC50 of 7.3 μM and a maximal effect of 380%. |
IC 50
mGlu2 Receptor: 147 nM (EC50)
JNJ-40411813Supplier
Haoyuan Chemexpress Co., Ltd.
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shanghai cooperpharm co.,LTD .
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