f050

Chlorpromazine Sulfone Hydrochloride is a metabolite of Chlorpromazine -- an anti-emetic and anti-psychotic agent. It may also be used as a potential N-methyltransferase inhibitor.

F-050 is a biochemical that has been shown to inhibit platelet aggregation induced by CaCl2, arachidonic acid, collagen, adenosine diphosphate (ADP) and thrombin in guinea pigs, rabbits and rats in vitro. F-050 may be useful in the treatment of thrombotic diseases.

PKF050-638 inhibits the CRM1-mediated Rev nuclear export by disrupting CRM1-NES interaction. PKF050-638 is an effective and selective inhibitor of HIV-1 Rev (IC50=0.04 μM).

PF05020182 is novel potent and selective Kv7.2/4 potassium channel opener. PF-05020182 (2) significantly inhibits convulsions in the MES assay at doses tested, consistent with in vitro activity measure. The physiochemical properties, in vitro and in vivo activities of PF-05020182 support further development as an adjunctive treatment of refractory epilepsy. Facilitating activation, or delaying inactivation, of the native Kv7 channel reduces neuronal excitability, which may be beneficial in controlling spontaneous electrical activity during epileptic seizures.

PF-05085727 inhibits PDE2A >4,000-fold selectivity over PDE1 and PDE3-11. PF-05085727 is an effective, selective and brain penetrant inhibitor of cGMP-dependent PDE2A (IC50=2 nM) .

Azamitosene is a DNA cleaving agent exhibiting G and A base specificity. Azamitosene may exhibit a growth inhibitory effect on human gastric cancer cells.

PF-05089771 is a voltage-gated sodium channel 1.7 (Nav1.7) blocker (IC50: 11, 16, 33, and 20 nM for 5N11S, 5A11L, 5A11S, and 5A11L Nav1.7 splice variants, respectively). It is selective for Nav1.7 over Nav1.1-1.6 and 1.8 channels (IC50: 0.11-25 μM), L-typ

PF 05089771 is a Selective inhibitor of Nav1.7 (IC50 = 11 nM) that interacts with the voltage-sensor domain of domain IV. It shows a slow onset of the block that is depolarization and concentration-dependent.

Utomilumab (PF 05082566) is a humanized IgG2 antibody that targets the T-cell co-stimulatory receptor 4-1BB/CD137 and acts as a 4-1BB/CD137 agonist. It exhibits antitumor activity and may be used in the study of patients with advanced malignancies.