| Identification | Back Directory | [Name]
PF-06372865 | [CAS]
1614245-70-3 | [Synonyms]
Darigabat
PF-06372865
PF06372865,PF 06372865
CVL-865|||PF-6372865|||PF-06372865
7-Ethyl-4-(4'-(ethylsulfonyl)-6-fluoro-2'-methoxy-[1,1'-biphenyl]-3-yl)-7H-imidazo[4,5-c]pyridazine
7H-Imidazo[4,5-c]pyridazine, 7-ethyl-4-[4'-(ethylsulfonyl)-6-fluoro-2'-methoxy[1,1'-biphenyl]-3-yl]- | [Molecular Formula]
C22H21FN4O3S | [MDL Number]
MFCD31693840 | [MOL File]
1614245-70-3.mol | [Molecular Weight]
440.49 |
| Chemical Properties | Back Directory | [Melting point ]
184 - 186°C | [Boiling point ]
577.2±60.0 °C(Predicted) | [density ]
1.35±0.1 g/cm3(Predicted) | [storage temp. ]
-20°C Freezer, Under inert atmosphere | [solubility ]
Chloroform (Slightly), DMSO (Slightly), Methanol (Slightly, Heated) | [form ]
Solid | [pka]
-0.55±0.30(Predicted) | [color ]
White to Light Beige |
| Hazard Information | Back Directory | [Uses]
PF 06372865 are used as GABAA receptor modulators to treat pain. | [in vivo]
PF-06372865 (compound 34; 3, 10 mg/kg; orally; single dose) significantly increases the paw withdrawal threshold (PWT) in chronic constriction injury (CCI) animals[1].
PF-06372865 (0.3, 3, 10 mg/kg for mouse and 1, 3, 10 mg/kg for rat; orally) exhibits efficacy in two models of epilepsy, PTZ induced seizures (mouse), and amygdala kindling (rat)[1].
PF-06372865 (0.1, 0.32, 1, 3.2 and 10 mg/kg; orally) has anxiolytic activity at 3.2 and 10 mg/kg in elevated plus maze (male C57Bl/6 mice)[1].
PF-06372865 has a T1/2 of 1.1 hours, a Clp of 22 mL/min/kg, and a Vss of 2.1 L/kg for rats[1].
PF-06372865 has a T1/2 of 0.9 hours, a Clp of 29 mL/min/kg, and a Vss of 3.4 L/kg for dogs[1].
| Animal Model: | Chronic constriction injury (CCI) model (male Wistar rats)[1] | | Dosage: | 3, 10 mg/kg | | Administration: | Orally | | Result: | Significantly increased paw withdrawal latency.
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