PF-06372865

PF-06372865

P655006-1ml

1ml

10mM in DMSO

避光,-80℃储存

超低温冰袋运输

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)

PF-06372865 是一种口服活性、α2/α3/α5 亚型选择性 GABA A 阳性异位调节剂 (PAM)。PF-06372865 是一种对含有 α1/α2/α3/α5 亚基的 GABA A 受体具有高亲和力的配体（α2、α1 PAM、α2 PAM 和 α5 亚基的 K i 分别为 2.9 nM、21 nM 和 134 nM）。

1614245-70-3(DMSO)

C22H21FN4O3S

440.49 g/mol

CCN1C=NC2=C1N=NC=C2C3=CC(=C(C=C3)F)C4=C(C=C(C=C4)S(=O)(=O)CC)OC