| MDL | MFCD28900744 |
|---|---|
| Molecular Weight | 349.35 |
| Molecular Formula | C21H15F2N2O |
| SMILES | FC1=CC(F)=C(C2=CC=NC(C2=CC=[NH+]3[O-])=C3C4=C(C)C=CC=C4)C=C1 |
p38 MAPK-IN-1 (Compound 4) is a novel potent and selective inhibitor of p38 MAPK with IC 50 of 68 nM. p38 MAPK-IN-1 shows sustained levels, low clearance and good bioavailability.
|
p38 MAPK 68 nM (IC 50 ) |
p38 MAPK-IN-1 (Compound 4; 1 mg/kg for iv and 10 mg/kg for po) has a t
1/2
of 7.4 hours and CL of 2.7 mL/min/kg for iv, and a C
max
of 5.3 μM for po in male wistar rats
[1]
.
p38 MAPK-IN-1 dose-dependently inhibits TNFα production with an ED
50
of 0.5 mg/kg
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male wistar rats [1] |
| Dosage: | 10 mg/kg for po and 1 mg/kg for iv (Pharmacokinetic Analysis) |
| Administration: | Po and iv |
| Result: | Had a t 1/2 of 7.4 hours and CL of 2.7 mL/min/kg for iv, and a C max of 5.3 μM for po. |
Solid
Room temperature in continental US; may vary elsewhere.
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
DMSO : 33.33 mg/mL ( 95.41 mM ; ultrasonic and warming and heat to 60°C)
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.8625 mL | 14.3123 mL | 28.6246 mL |
| 5 mM | 0.5725 mL | 2.8625 mL | 5.7249 mL |
| 10 mM | 0.2862 mL | 1.4312 mL | 2.8625 mL |