Pristinamycin (Virginiamycin antibiotic complex; NSC-246121; Antibiotic 899; Founderguard) is a novel, naurally occuring streptogramin-like and potent antibiotic used primarily in the treatment of staphylococcal infections, and to a lesser extent streptococcal infections. Pristinamycin is a mixture of two components that have a synergistic antibacterial action. Pristinamycin IA is a macrolide, and results in pristinamycin’s having […]

Deacetoxycephalosporin C (also known as DAOC), a cephalosporin derived from a cephalosporin C, is a novel and potent cephalosporin antibiotic and a precursor of cephalosporins excreted by Cephalosporium and Streptomyces species. It is formed by the action of enzyme DAOC synthetase/DAC hydroxylase.

Dagrocorat (also known as PF-00251802) is a novel and potent dissociated glucocorticoid receptor agonist with the potential usefulness as an anti-inflammatory agent. The dissociated agonists of the glucocorticoid receptor are a novel class of agents in clinical development for rheumatoid arthritis. PF-04171327 (fosdagrocorat) is a phosphate ester prodrug of PF-00251802 (dagrocorat), a selective high-affinity partial […]

cFMS Receptor Inhibitor III is a novel, potent and cell-permeable anilinoquinoline compound that acts as a strong, active site-targeting inhibitor of M-CSF/c-Fms-CSF-1R (MCSF receptor/cFMS) with IC50 of 8 nM. cFMS Receptor Inhibitor III is 100-fold more potent in inhibiting the cFMS-dependent growth of M-NSF-60 cells than the cFMS-independent growth of NSO cells with IC50 values […]

Apraclonidine (iopidine) HCl, the hydrochloride salt of Apraclonidine, is a potent sympathomimetic acting as an alpha2-adrenergic agonist and is used in glaucoma therapy. It is also a weak alpha-1 adrenergic receptor agonist. Apraclonidine enhances aqueous humor uveoscleral outflow and decreases aqueous production by vasoconstriction.

PF 750 is a novel, potent, selective and covalent/irreversible fatty acid amide hydrolase (FAAH) inhibitor, with IC50s varying from 16.2-595 nM. Fatty acid amide hydrolase (FAAH) is an integral membrane enzyme that degrades the fatty acid amide family of signaling lipids, including the endocannabinoid anandamide. Genetic or pharmacological inactivation of FAAH leads to analgesic, anti-inflammatory, […]

CP 316311 is a novel, potent, selective and orally bioactive antagonist of the corticotropin-releasing factor 1 (CRF 1) receptor with an IC50 value of 6.8 nM. CP-316311 demonstrates oral efficacy in central nervous system (CNS) in vivo models. CP-316311 was advanced to phase II depression trials to test the hypothesis that CRF 1 antagonists could […]

CDD3505 is a novel HDL cholesterol level inducing compound used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.

NE10790, an analog of risedronate, is a poor farnesyl pyrophosphate synthase inhibitor and a weak antiresorptive agent. It belongs to the group of phosphonocarboxylates in which one of the phosphonate groups is substituted by a carboxyl group. NE-10790 had strongly reduced binding affinity, but still retained some antiresorptive activity. The group of phosphonocarboxylates, with strongly […]

BI 689648 is a novel, potent and highly selective aldosterone synthase (AS) inhibitor that can attenuate the production of aldosterone directly and has been proposed as an alternative to mineralocorticoid receptor antagonists for blocking the pathologic effects of excess aldosterone. It can inhibit CYP11B1 and CYP11B2 with IC50s of 310 and 2.1 nM, respectively. BI […]