mk 5

MK-6186 HCl, a novel non-nucleoside reverse transcriptase inhibitor with antiviral activity, can be used to study HIV.

MK2-IN-5, a pseudosubstrate of Mk2 with an inhibition constant (K_i) of 8 μM, selectively targets the protein interaction domain of the MAPK pathway and inhibits the phosphorylation of HSP25 and HSP27 [1] [2] [3].

Rizatriptan benzoate (MK-462 Benzoate) selectively binds to and activates serotonin (5-HT) 1B receptors and 5-HT 1D receptors providing relief of migraine headaches.

Finasteride (MK-906) is an oral inhibitor of active testosterone 5-alpha-reductase and Ki value is 10 nM.

Fluvoxamine maleate (DU-23000 (maleate)) is a selective serotonin reuptake inhibitor that is used in the treatment of depression and a variety of anxiety disorders.

MK 0434 is an orally active steroidal 5 alpha-reductase inhibitor.

MK-886 (L 663536) is an inhibitor of leukotriene biosynthesis, acting by inhibiting the 5-lipoxygenase-activating protein (FLAP), and serves as a moderately potent PPARα antagonist.

MK 212 hydrochloride is a 5-HT2C receptor agonist

MK-0752, a γ-secretase inhibitor, reduces Aβ40 production(IC50=5 nM).

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).

MK2-IN-3 (MK2 Inhibitor III) is a potent, cell-permeable inhibitor of mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2 or MK-2) and can be used for the treatment of rheumatoid arthritis

Ascr#2 (asc-C6-MK) is a glycoside analogue in Cryptococcus hidradii that promotes dauer formation.Ascr#2 mixtures with ascr#3 at low concentrations act as a male elicitor and can be used to detect population density.Ascr#5 (asc-ωC3) is a highly conserved ascaroside analogue in Cryptococcus hidradii that regulates a variety of responses in Cryptococcus hidradii.

MK-8245 trifluoroacetate is a phenoxy piperidine isoxazole derivative functioning as a potent, liver-targeting stearoyl-CoA desaturase (SCD) inhibitor, demonstrating significant anti-diabetic and anti-dyslipidemic effects. It showcases high specificity and efficacy against SCD1 across various species, with IC50 values of 1 nM for human SCD1 and 3 nM for both rat and mouse SCD1. MK-8245's mechanism includes a tetrazole acetic acid moiety that facilitates liver-targeting through OATPs recognition. Its inhibition potency in rat hepatocyte assays (IC50 of 68 nM) surpasses that in HepG2 cell assays devoid of active OATPs (IC50 of ~1 μM), highlighting its liver specificity. Moreover, MK-8245 exhibits over 100,000-fold selectivity against Δ-5 and Δ-6 desaturases in comparative assays. In vivo studies reveal MK-8245's preferential liver distribution in mice, rats, dogs, and rhesus monkeys, underscoring its potential for minimizing adverse effects in non-target tissues. Additionally, its administration in eDIO mice before glucose challenges significantly improves glucose clearance, indicating its therapeutic promise in diabetes management.

MK-3207 is a potent and orally bioavailable CGRP receptor antagonist (IC 50 = 0.12 nM; K i = 0.024 nM); highly selective versus human AM1, AM2, CTR, and AMY3. IC50 Value: 0.024 nM (Ki, Human CGRP) [1] As other CGRP receptor antagonists, MK-3207 shows a lower affinity for human CGRP receptors from other species, including canine and rodent. in vitro: MK-3207 is a potent antagonist of the human and rhesus monkey CGRP receptors (K(i) = 0.024 nM). in vivo: MK-3207 produced a concentration-dependent inhibition of dermal vasodilation, with plasma concentrations of 0.8 and 7 nM required to block 50 and 90% of the blood flow increase, respectively. The tritiated analog [3H]MK-3207 was used to study the binding characteristics on the human CGRP receptor. [3H]MK-3207 displayed reversible and saturable binding (K(D) = 0.06 nM), and the off-rate was determined to be 0.012 min(-1), with a t(1/2) value of 59 min [1]. After the first interim analysis, the two lowest MK-3207 doses (2.5, 5 mg) were identified as showing insufficient efficacy. Per the pre-specified adaptive design decision rule, only the 2.5-mg group was discontinued and the five highest doses (5, 10, 20, 50, 100 mg) were continued into the second stage [2]. Clinical trial: MK-3207 for the treatment of acute migraines. Phase 2b

MK-8153 is a selective, potent, orally active inhibitor of extrarenal medullary potassium channels (ROMK), acting on ROMK EP (IC50: 5 μM) and hERG EP (IC50: 34 μM).MK-8153 can be used as a diuretic.

Enalapril D5 maleate is deuterium labeled Enalapril, which is an angiotensin converting enzyme (ACE) inhibitor.

Enalaprilat D5 is the deuterium labeled Enalaprilat, which is an angiotensin-converting enzyme (ACE) inhibitor.

Fmoc-5-aminopentanoic acid is an alkane chian with terminal Fmoc-protected amine and carboxylic acid groups. The compound can be used as a PROTAC linker in the synthesis of PROTACs. The Fmoc group can be deprotected under basic condition to obtain the free amine which can be used for further conjugations. The terminal carboxylic acid can react with primary amine groups in the presence of activators (e.g. EDC, or HATU) to form a stable amide bond.

Compound 8 (5-HT6R antagonist 1), a 5-HT6R antagonist (K i : 5 nM), not only demonstrates inhibition of platelet aggregation and excellent metabolic stability but also reverses MK-801-induced memory impairments in rats, suggesting its utility in Alzheimer's disease (AD) research [1].

Enalaprilat D5 Sodium Salt is the deuterium labeled Enalaprilat, which is an angiotensin-converting enzyme (ACE) inhibitor.