T1608

ADH-1 trifluoroacetate (Exherin trifluoroacetate) is a cyclic pentapeptide vascular-targeting agent with potential antineoplastic and antiangiogenic activities. ADH-1 selectively and competitively binds to and blocks N-cadherin, which may result in disruption of tumor vasculature, inhibition of tumor cell growth, and the induction of tumor cell and endothelial cell apoptosis.

MK-0674 is an orally available, selective and potent cathepsin K inhibitor (IC50: 0.4 nM) that inhibits Cat B, Cat F, Cat L, and Cat S. It can be used in metabolism-related diseases.

MIV-150 is a nonnucleoside inhibitor of reverse transcriptase (NNRT). MIV-150 also blocking HIV-1 and HIV-2 infections (EC50<1 nM against HIV-1/HIV-2MN).

Mizagliflozin is an orally active, selective SGLT1 inhibitor with a Ki value of 27 nM for human SGLT1. Mizagliflozin is 303 times more selective for SGLT1 than for SGLT2. Mizagliflozin is an anti-diabetic drug that can improve postprandial blood sugar fluctuations and may have the potential to improve chronic constipation.

MK-0343, also known as MRK-409, is a GABAA receptor subtype-selective partial agonist that exhibits non-sedating anxiolytic activity in preclinical species but induces sedation in humans, binding with high affinity to α1-, α2-, α3-, and α5-containing human recombinant GABA(A) receptors while demonstrating greater agonist efficacy at α3 relative to α1 subtypes, thereby providing mechanistic insight into subtype-specific modulation of inhibitory neurotransmission.

MK-0429 is an orally active, selective, and nonpeptide antagonist of αvβ3 integrin (IC50: 80 nM).

MK-0493 is an effective and selective agonist of the melanocortin receptor 4 (MC4R). It also demonstrated significant reductions in energy intake.

Quiflapon (MK-591) causes cell apoptosis. Quiflapon is a selective and specific 5-lipoxygenase-activating protein (FLAP) inhibitor (IC50: 1.6 nM in a FLAP binding assay) and is also an effective and orally active Leukotriene biosynthesis (LT) inhibitor (IC50: 3.1 and 6.1 nM in intact human and elicited rat PMNLs, respectively).

MK-0608 is an orally bioavailable HCV replication inhibitor in vitro(EC50 = 0.3 μM and EC90=1.3 μM in the subgenomic-replicon assay).