Desmopressin acetate, the acetate salt of desmopressin (also known as DDAVP), is a synthetic octapeptide and an analogue of the human antidiuretic hormone arginine vasopressin. Compare with vasopressin, Desmopressin has improved pharmacokinetics such as prolonged half life and better pharmacodynamics such as higher selectivity for the V2 membrane receptor. Vasopressin is a hormone that reduces […]
(S)-4CPG [also known as (S)-4-Carboxyphenylglycine, and (S)-4C-PG] is a novel, potent, competitive and orally bioactive antagonist of metabotropic glutamate receptor 1 (mGluR) with selectivity for mGluR-1 over mGluR-5. Group I (mGluR-1 and mGluR-5) receptors are coupled to Gq/11 and are activators of phospholipase C. (S)-4-CPG and (S)-MCPG were the most selective mGlu1alpha receptor antagonists. Longer […]
GNF-6231 is a novel, potent, orally active and selective Porcupine inhibitor that blocks Wnt signaling with IC50 of 0.8 nM (Wnt3a Co-culture RGA). GNF-6231 has low/no drug drug interaction potential with IC50s of greater than 10 μM on all CYP isoforms tested. GNF-6231 showed excellent pathway inhibition and induced robust antitumor efficacy in a mouse […]
LGD-3303 is a potent, selective, orally bioavailable, and non-sterdoidal androgen receptor modulator (SARM) with anabolic effects on muscle and cortical bone not observed with bisphosphonates. It shows little or no cross-reactivity with related nuclear receptors. Upon oral administration of LGD-3303 for 14 days in orchidectomized male rats, the tissue selective activity of LGD-3303 was assessed, […]
Tirasemtiv (also known as CK2017357) is a novel small-molecule activator of fast-skeletal-troponin, it is being developed as a potential treatment for diseases and conditions associated with aging, muscle weakness and wasting or neuromuscular dysfunction. Tirasemtiv slows the rate of calcium release from troponin, thus sensitizing fast skeletal muscle fibers to calcium. Tirasemtiv demonstrated increases in […]
CP-55940 (CP-55,940; CP55,940) is a novel, potent and non-selective cannabinoid receptor agonist with Ki values of 0.58 and 0.69 nM for human recombinant CB1 and CB2, respectively. It is a cannabinoid which mimics the effects of naturally occurring THC (one of the psychoactive compounds found in cannabis). CP 55,940 was created by Pfizer in 1974 […]