10mM in DMSO for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
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SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABA A positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABA A receptors containing α1/α2/α3/α5 subunits ( K i s of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. PF-06372865 can across the blood-brain barrier (BBB). PF-06372865 has anxiolytic activity and has the potential for epilepsy
In Vitro
PF-06372865 (compound 34) has K i values of 0.18 nM, 2.9 nM, 1.1 nM, 18 nM for human GABA A α1β3γ2, α2β2γ2, α3β3γ2, α5β2γ2 and 0.34 nM, 4.58 nM for rat GABA A α1β3γ2, α2β2γ2. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 . 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) . 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) . PF-06372865 has a T 1/2 of 1.1 hours, a Cl p of 22 mL/min/kg, and a V ss of 2.1 L/kg for rats . PF-06372865 has a T 1/2 of 0.9 hours, a Cl p of 29 mL/min/kg, and a V ss of 3.4 L/kg for dogs . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Chronic constriction injury (CCI) model (male Wistar rats) Dosage: 3, 10 mg/kg Administration: Orally Result: Significantly increased paw withdrawal latency.
IC50& Target:Ki: 2.9 nM (α2), 21 nM (α1 PAM) and 134 nM (α2 PAM)
| ALogP | 2.9 |
|---|
| Isomeric SMILES | CCN1C=NC2=C1N=NC=C2C3=CC(=C(C=C3)F)C4=C(C=C(C=C4)S(=O)(=O)CC)OC |
|---|---|
| Alternate CAS | 1614245-70-3 |
| PubChem CID | 76287260 |
| MeSH Entry Terms | 7-ethyl-4-(3-(4-ethylsulfonyl-2-methoxyphenyl)-4-fluorophenyl)imidazo(4,5-c)pyridazine;PF-06372865 |
| Molecular Weight | 440.49 |
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