cyclase

Glutaminyl Cyclase Inhibitor 1, a glutaminyl cyclase inhibitor with an IC50 of 0.5 μM, can be utilized for studying neurological disorders.

Glutaminyl Cyclase Inhibitor 3, a designed anti-Alzheimer's compound, is a potent human Glutaminyl Cyclase (GC) inhibitor (IC50: 4.5 nM). It significantly reduced the brain concentrations of pyroform Aβ and total Aβ and restored cognitive functions.

Glutaminyl Cyclase Inhibitor 2 is a glutaminyl cyclase inhibitor with an IC50 of 1.23 μM.

Guanylate cyclase-IN-1 (Example 46) is a specific guanylate cyclase inhibitor used in cardiovascular disease research.

2',5'-Dideoxyadenosine is a potent and non-competitive adenylyl cyclase inhibitor, binding to the P-site with an IC50 of 3 μM.

Ataciguat (HMR-1766) (HMR-1766) is a potent and specific soluble guanylate cyclase (sGC) activator.

BMS-986122 (BMS 986122) is a positive allosteric modulator of μ-opioid receptors that increases β-arrestin recruitment stimulated by endomorphin 1 in U2OS-OPRM1 human osteosarcoma cells expressing μ-opioid receptors (EC50 = 3 μM).

BIBB 515 is a selective and potent inhibitor of OSC in vivo with an ED50 value of 0.2-0.5 and 0.36-33.3 mg/kg in rats and mice, respectively. 2, 3-Oxidosqualene cyclase (OSC) is an important enzyme in the biosynthesis of animal, plant, and fungal sterols.

Forskolin (Coleonol) is a natural product, an adenylate cyclase activator (EC50=0.5 μM). Forskolin increases cAMP levels, activates PXR and FXR, and induces autophagy. Forskolin produces positive inotropic effects in the heart, and has platelet anticoagulant and antihypertensive effects.

9-CP-Ade Mesylate (9 CP Ade Mesylate) is a cell-permeable, stable and non-competitive inhibitor of adenylate cyclase.

Bithionol (Actamer), formerly marketed as an active ingredient in various topical drug products, was shown to be a potent photosensitizer with the potential to cause serious skin disorders. Approvals of the NDA's for bithionol drug products were withdrawn on October 24, 1967.

Riociguat (BAY 632521) is a stimulator of guanylate cyclase which causes relaxation of vascular smooth muscle and is used to treat severe pulmonary arterial hypertension.

Nitroprusside disodium dihydrate (Sodium Nitroprusside Dihydrate) is a potent vasodilator working through releasing NO spontaneously in blood.

Nelociguat (BAY60-4552)(BAY60-4552) is a soluble guanylate cyclase stimulator (sGC stimulator). Soluble guanylate cyclase (sGC) is a key enzyme in the nitric oxide (NO) signalling pathway.

Linaclotide, developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) and chronic constipation, is a potent and selective guanylate cyclase C agonist.

Lysipressin ([Lys8]-Vasopressin), Induces contraction of the rabbit urinary bladder smooth muscle, activate adenylate-cyclase. Lysipressin is Antidiuretic hormone that have been found in pigs and some marsupial families.

MGV354 is a soluble activator of guanylate cyclase(sGC) with EC 50 s of <0.5 nM, and 5 nM in CHO and GTM-3 E cells, respectively [1] [2].

CB-7921220 (6-[2-(4-Aminophenyl)vinyl]-2-pyridinecarboxylic acid) is an inhibitor of adenylate cyclase.

KH7 is a soluble inhibitor of adenylyl cyclase (sAC)-specific. It has IC50s of 3-10 μM toward both recombinant purified human sACt protein and heterologously expressed sACt in cellular assays. KH7 is also a cAMP inhibitor.

LRE1 is a specific and allosteric inhibitor of soluble adenylyl cyclase (sAC).

NKH477 (Colforsin dapropate hydrochloride) is a derivative of forskolin with antidepressant activity. It inhibits ACh-induced Ca2+ mobilization by acting on ionomycin-sensitive storage sites. NKH477 is an adenylyl cyclase activator with bronchodilatory effects, inhibiting the production of CTL, T-cell proliferation in mixed lymphocyte reactions (MLR), as well as IL-2 production and mitogen responses.

NKY80 regulates the adenylyl cyclase catalytic activity in heart and lung tissues. NKY80 is a non-competitive inhibitor of adenylyl cyclase type V isoform (IC50s: 8.3 µM, 132 µM, and 1.7 mM for type V, III and II, respectively).

NS-2028 is a highly selective soluble Guanylyl Cyclase (sGC) inhibitor (IC50: 30 nM and 200 nM for basal and NO-stimulated enzyme activity) commonly used in nitric oxide signaling pathway research. It inhibits sGC activity in mouse cerebellum homogenates and neuronal NO synthase (IC50: 17 nM and 20 nM), inhibits 3-morpholino-sydnonimine (SIN-1)-elicited cyclic GMP formation in human cultured umbilical vein endothelial cells (IC50: 30 nM), and completely inhibits NO-dependent relaxant responses in non-vascular smooth muscle (1 μM). NS-2028 also decreases vascular endothelial growth factor-induced angiogenesis and permeability.

Runcaciguat is a soluble guanylate cyclase stimulator. Runcaciguat combines with selective partial adenosine A1 receptor agonists and can be used in studies about cardiovascular and renal diseases.