Vasotide, D(Cys-Leu-Pro-Arg-Cys) [abbreviated as D(CLPRC)], is a novel and potent peptidomimetic compound that targets two retinal VEGF receptors (VEGFR-1 and VEGFR-2) and reduces pathological angiogenesis in murine and nonhuman primate models of retinal disease. Blood vessel growth from preexisting vessels (angiogenesis) underlies many severe diseases including major blinding retinal diseases such as retinopathy of prematurity […]

PRL-8-53 is a nootropic research chemical derived from benzoic acid and phenylmethylamine (Benzylamine) that has been shown to act as a hypermnesic drug in humans; it was first synthesized by medical chemistry professor Nikolaus Hansl at Creighton University in the 1970s as part of his work on amino ethyl meta benzoic acid esters. PRL-8-53 is […]

KT5823 (KT-5823), a staurosporine-related analog, is a selective inhibitor of protein kinase G (PKG) with anticancer activity. It inhibits protein kinases with Ki values of 0.23, 4 and > 10 μM for PKG, PKC and PKA respectively. KT5823 has been shown to increase thyroid-stimulating hormone-induced NIS expression, and thus iodide uptake, in thyroid cells. In […]

KMUP-3, a xanthine derivative, has been demonstrated to modulate K+-channel activity in smooth muscles and is a stimulator of the NO/sGC/cGMP pathway. KMUP-3 (7-{2-[4-(4-nitrobenzene) piperazinyl]ethyl}-1, 3-dimethylxanthine) displays cardioprotection and increases cardiac output, and is suggested to increase cardiac performance and improve myocardial infarction. KMUP-3 (0.1-10μM) increased PKA, RhoA/ROCKII, and PKC translocation and CIP-17 (an endogenous […]

KMUP-1, a xanthine derivative, has been demonstrated to modulate K+-channel activity in smooth muscles and is a stimulator of the NO/sGC/cGMP pathway. KMUP-1 prevents STZ impairment of MA reactivity, eNOS levels and KATP channels, and accordingly protects against vascular dysfunction in diabetic rats. . KMUP-1 significantly attenuated STZ-stimulated MA contractions in response to high K+, […]

BAY-1316957 (BAY1316957) is a novel, highly potent, selective, and orally bioavailable antagonist of human prostaglandin E2 receptor subtype 4 (hEP4 receptor) with the potential to be used for the Treatment of Endometriosis. It inhibits hEP4-R with an IC50 of 15.3 nM. The presence and growth of endometrial tissue outside the uterine cavity in endometriosis patients […]

MK-3328 is a novel and potent candidate PET ligand for the clinical assessment of β-amyloid plaque load. As a β-Amyloid PET ligand, MK-3328 exhibits high binding potency with an IC50 of 10.5 nM. MK-3328 has a favorable potency versus human β-amyloid plaque and has been radiolabeled for further evaluation in in vitro binding and in […]

Unifiram (also known as DM-232), a piperazine derived ampakine-like drug, has potent nootropic effects in animal studies with significantly higher potency than piracetam. DM 232 and DM 235 are novel antiamnesic compounds structurally related to ampakines. The involvement of AMPA receptors in the mechanism of action of DM 232 and DM 235 was, therefore, investigated […]

BAY-Y 3118 is novel and potent chlorofluoroquinolone derivative with antimicrobial activity against Haemophilhs influenzae, Moraxela catarrhalis, Acinetobacter baumannii, Xanthomonas maltophiia, gram-positive cocci, and anaerobes; MICs for 50%o of the strains (MIC50s) and MIC90s are ≤0.015 and ≤0.015, ≤0.015 and ≤0.015, 0.03 and 2, 0.25 and 0.5, 0.06 and 1, and 0.12 and 0.25 μg/mL, respectively. […]

SCY-635 is a novel and potent nonimmunosuppressive cyclosporine-based analog that exhibits potent suppression of hepatitis C virus (HCV) replication in vitro. SCY-635 inhibited the peptidyl prolyl isomerase activity of cyclophilin A at nanomolar concentrations but showed no detectable inhibition of calcineurin phosphatase activity at concentrations up to 2 μM. Metabolic studies indicated that SCY-635 did […]