Guanylate Cyclase Activator

Lificiguat binds to the β subunit of soluble guanylyl cyclase(sGC) with K_d of 0.6-1.1 μM in the presence of CO.

Vericiguat (BAY1021189) is a potent, orally available and soluble guanylate cyclase stimulator.

Riociguat is an oral stimulator of soluble guanylate cyclase (sGC) used in the treatment of pulmonary hypertension.

LOXL2/sGC modulator-1 (Compound 11k) is a LOXL2 inhibitor (IC₅₀ = 0.13 μM) and an sGC activator. LOXL2/sGC modulator-1 shows good selectivity for LOX (IC₅₀ > 45.9 μM) and LOXL3 (IC₅₀ = 1.30 μM). LOXL2/sGC modulator-1 significantly increases intracellular cGMP levels in the presence of the gGC inhibitor ODQ (HY-101255). LOXL2/sGC modulator-1 significantly inhibits hypoxia-induced collagen deposition and cross-linking, while promoting vasodilation. LOXL2/sGC modulator-1 can be used for the study of pulmonary arterial hypertension.

Cinaciguat is an activator of guanylate cyclase (sGC), and used for acute decompensated heart failure.

BAY 41-2272 is an orally active and soluble guanylate cyclases (sGC) activator, which increases sGC activity by 400-fold in synergy with NO. BAY 41-2272 potently unloaded the heart, increased cardiac output, thus can be used for cardiovascular diseases research.

BAY 60-2770 is a potent, selective, and orally active soluble guanylyl cyclase (sGC) activator. BAY 60-2770 increases the activity of sGC in a nitric oxide-independent manner. BAY 60-2770 shows antifibrotic effect.

Ataciguat (HMR-1766) is a nitric oxide-independent soluble guanylate cyclase (sGC) activator. Ataciguat is able to activate the ferric heme-iron redox form of sGC that stimulate the production of cyclic GMP (cGMP). Ataciguat exhibits vasodilator effects.

Runcaciguat (BAY 1101042) is a selective, orally active, allosteric activator of soluble guanylate cyclase (sGC) that specifically targets its oxidized and heme-free form. Runcaciguat binds to sGC in a histidine-dependent manner and restores cyclic guanosine monophosphate (cGMP) production under oxidative stress, independent of nitric oxide (NO) or heme. Runcaciguat exhibits renoprotective and cardioprotective activities, such as reduced proteinuria and improved renal function. Runcaciguat is primarily being studied in chronic kidney disease (CKD) associated with hypertension, diabetes, and metabolic disorders, as well as potential cardiovascular indications such as heart failure with preserved ejection fraction (HFpEF).

Praliciguat (IW-1973) is a potent and orally active soluble guanylate cyclase (sGC) activator. Praliciguat can increases cGMP via the nitric oxide (NO)-sGC pathway. Praliciguat can inhibit the expression of proinflammatory cytokines and inhibit apoptosis. Praliciguat can promote vasodilation. Praliciguat can be used for the researches of metabolic disease and cardiovascular disease, such as hypertension, diabetes and heart failure.

Cinaciguat hydrochloride is a potent soluble guanylate cyclase (GC) activator with EC₅₀ of 15 nM in platelets.

Olinciguat (IW-1701) is an oral guanylate cyclase (sGC) stimulator with concentration-dependent stimulation of sGC in purified rat and human enzyme assays and a whole cell assay.

Nelociguat (BAY60-4552) is a nitric oxide sensitive soluble guanylate cyclase stimulator.

Guanylin(human) TFA, a 15-amino acid peptide, is an endogenous intestinal guanylate cyclase activator. Guanylin(human) TFA is mainly found in gastrointestinal tract which regulates electrolytead water transport in intestinal and renal epithelia through cyclic GMP-dependent mechanism.

BAY 41-8543 is an orally active, nitric oxide (NO)-independent stimulator of soluble guanylyl cyclase (sGC). BAY 41-8543 has vasodilator activity in the pulmonary and systemic vascular beds in the rat. BAY 41-8543 has antiplatelet effects and has the potential for cardiovascular diseases research.

Prepro-ANF (56-92), human is a human atrial natriuretic factor precursor. Prepro-ANF (56-92), human is also a guanylate cyclase activator that enhances particulate guanylate cyclase activity in the renal membrane and renal unit.

Guanylin (mouse, rat) TFA, a petide, is composed of 15 amino acids. Guanylin (mouse, rat) TFA is an activator of intestinal guanylate cyclase. Guanylin (mouse, rat) TFA can be used for the research of diarrhea.

Guanylin(human), a 15-amino acid peptide, is an endogenous intestinal guanylate cyclase activator. Guanylin(human) is mainly found in gastrointestinal tract which regulates electrolytead water transport in intestinal and renal epithelia through cyclic GMP-dependent mechanism.

(Rac)-MGV354 is the racemate of MGV354. MGV354 is a soluble guanylate cyclase (sGC) activator with EC₅₀s of <0.5 nM, and 5 nM in CHO and GTM-3 E cells, respectively.

NPR-C activator 1 (Compound 1) is a potent activator of natriuretic peptide receptor C (NPR-C). C-type natriuretic peptide (CNP) is involved in the regulation of vascular homeostasis. NPR-C activator 1 is identified as a potent agonist (EC₅₀ ∼ 1 μM) with promising in vivo pharmacokinetic properties.