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Dibutyryl-cGMP sodium (Bt2cGMP sodium) is a cell-permeable cGMP analogue. Dibutyryl-cGMP sodium preferentially activates cGMP-dependent protein kinase (PKG). Dibutyryl-cGMP sodium inhibits the release of [ 3H]-arachidonic acid from γ thrombin-stimulated human platelets. Dibutyryl-cGMP sodium induces peripheral antinociception via activation of ATP-sensitive K + channels[3].
Ethyl β-carboline-3-carboxylate (fl-CCE) is a ligand and short-acting antagonist of benzodiazepine receptors. Ethyl β-carboline-3-carboxylate did not affect cerebellar cGMP levels when used alone, but when taken together with Diazepam, it significantly inhibited the cGMP levels that were upregulated by Diazepam .
MBCQ is a potent and selective cGMP-specific phosphodiesterase (PDE V; PDE5) inhibitor with an IC50 of 19 nM. MBCQ lacks inhibitory activity toward other PDE isozymes (all IC50s>100 μM). MBCQ dilates coronary arteries via specific inhibition of cGMP-PDE [3].
2′,3′-cGMP triethylamine (Guanosine 2',3'-cyclic phosphate triethylamine) is an active compound. 2′,3′-cGMP triethylamine can be used for various studies .
8-Nitro-cGMP is an electrophilic second messenger of redox signaling that can form a protein-S-cGMP adduct in s-guanylation process. 8-Nitro-cGMP is an autophagy inducer. 8-Nitro-cGMP promotes RANKL-induced osteoclast differentiation from macrophages. 8-Nitro-cGMP has vasodilator effect, and ameliorates the vascular endothelial dysfunction in diabetic mice [3] .
PET-cGMP is a cyclic guanosine monophosphate analog and an effective selective agonist of PKG I, the EC50 of PET-cGMP for PKG Iβ is 3.8 nM, while for PKG II, it's 193 nM .
Zaprinast (M&B 22948) is a selective inhibitor of cGMP-selective Phosphodiesterase (PDE5). Zaprinast causes a significant increase in cGMP levels in myocytes. Zaprinast is a G protein-coupled receptor 35 (GPR35) agonist which activates rat GPR35 strongly and activates human GPR35 moderately. Zaprinast reduces vessel remodeling through antiproliferative and proapoptotic effects [3].
Gisadenafil (UK-369003) is a specific, orally active phosphodiesterase 5 (PDE5) inhibitor with an IC50 of 3.6 nM and prevents degradation of cyclic guanosine monophosphate (cGMP) .
Cyclic GMP (cGAMP) is an endogenous second messenger that triggers interferon production in response to cytoplasmic DNA. Cyclic GMP can activate the stimulator of interferon genes (STING), activating the signaling cascade that leads to the production of type I interferons and other immune mediators. Cyclic-GMP-AMP, a conjugate of cyclic GMP and AMP, can induce IRF3 phosphorylation and nuclear translocation, enhancing antiviral immune responses. cGMP may also activate PDE to degrade cAMP, inhibit myocardial calcium current ICa, and regulate myocardial contractility. The derivative of cyclic GMP (cGMP), 8-Br-cGMP, has antiplatelet activity, and cyclic GMP can be used in the study of antiviral immunity and cardiovascular diseases [3] .
Gisadenafil besylate (UK 369003-26) is a specific, orally active phosphodiesterase 5 (PDE5) inhibitor with an IC50 of 3.6 nM and prevents degradation of cyclic guanosine monophosphate (cGMP) .
Avanafil (TA-1790) is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis [3].
AP-C3 is a potent inhibitor of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII) with a pIC50 of 6.3. AP-C3 only weakly inhibits cGKII-dependent anion secretion .
Vardenafil dihydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil dihydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM respectively, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil dihydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil dihydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes - .
Vardenafil is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
Vardenafil-d5 is deuterium labeled Vardenafil. Vardenafil is a selective, orally active, potent inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows selectivity over PDE1 (180 nM), PDE6 (11 nM), PDE2, PDE3, and PDE4 (>1000 nM). Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil can be used for the research of erectile dysfunction .
AP-C4 is an inhibitor of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII) with a pIC50 of 5.2. AP-C3 does not inhibit cGKII-dependent anion secretion .
Avanafil (Standard) is the analytical standard of Avanafil. This product is intended for research and analytical applications. Avanafil (TA-1790) is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis [3].
Avanafil (Standard) is the analytical standard of Avanafil. This product is intended for research and analytical applications. Avanafil (TA-1790) is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis [3].
Avanafil (TA-1790) dibenzenesulfonate is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil dibenzenesulfonate activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil dibenzenesulfonate inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil dibenzenesulfonate can be used for the research of erectile dysfunction and osteoporosis [3].
Quazinone is a selective inhibitor of cGMP-inhibited-phosphodiesterase (cGI-PDE, PDE3). Quazinone inhibits the phosphorylation of p42/p44 MAP kinase. Quazinone possesses antimitogenic effect .
Vardenafil hydrochloride trihydrate is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride trihydrate shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride trihydrate competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride trihydrate can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
Avanafil- 13C5 (TA1790- 13C5) is 13C labeled Avanafil. Avanafil (TA-1790) is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis [3].
Avanafil- 13C5, 15N,d2 is 15N and deuterated labeled Avanafil (HY-18252). Avanafil (TA-1790) is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis [3].
T-0156 is a potent and selective phosphodiesterase type 5 (PDE5) inhibitor. T-0156 specifically inhibits the hydrolysis of cyclic guanosine monophosphate (cGMP) by PDE5 in a competitive manner (IC50=0.23 nM). T-0156 inhibits PDE6 (IC50=56 nM) and has low potencies against PDE1, PDE2, PDE3, and PDE4 (IC50>10 μM). T-0156 enhances the nitric oxide (NO)/cGMP pathway .
Vardenafil-d5 hydrochloride is deuterated labeled Vardenafil hydrochloride (HY-B0442A). Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
Vardenafil (dihydrochloride) (Standard) is the analytical standard of Vardenafil (dihydrochloride). This product is intended for research and analytical applications. Vardenafil dihydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil dihydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM respectively, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil dihydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil dihydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes - .
Vardenafil (Standard) is the analytical standard of Vardenafil. This product is intended for research and analytical applications. Vardenafil is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
Vardenafil (dihydrochloride) (Standard) is the analytical standard of Vardenafil (dihydrochloride). This product is intended for research and analytical applications. Vardenafil dihydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil dihydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM respectively, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil dihydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil dihydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes - .
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 [3].
AP-C7 is an inhibitor of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII) with a pIC50 of 5.0. AP-C7 only weakly inhibits cGKII-dependent anion secretion .
Vardenafil (hydrochloride trihydrate) (Standard) is the analytical standard of Vardenafil (hydrochloride trihydrate). This product is intended for research and analytical applications. Vardenafil hydrochloride trihydrate is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride trihydrate shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride trihydrate competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride trihydrate can be used for the research of erectile dysfunction, hepatitis, diabetes - .
T-0156 free base is a potent and selective phosphodiesterase type 5 (PDE5) inhibitor. T-0156 free base specifically inhibits the hydrolysis of cyclic guanosine monophosphate (cGMP) by PDE5 in a competitive manner (IC50=0.23 nM). T-0156 free base inhibits PDE6 (IC50=56 nM) and has low potencies against PDE1, PDE2, PDE3, and PDE4 (IC50>10 μM). T-0156 free base enhances the nitric oxide (NO)/cGMP pathway .
AP-C1 is a potent inhibitor of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII) with a pIC50 of 6.5. AP-C1 only weakly inhibits cGKII-dependent anion secretion .
PF-05085727 is a potent, selective and brain penetrant inhibitor of cGMP-dependent PDE2A (IC50=2 nM). PF-05085727 inhibits PDE2A >4,000-fold selectivity over PDE1 and PDE3-11 .
Plecanatide, an analogue of Uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist. Plecanatide activates GC-C receptors to stimulate cGMP synthesis with an EC50 of 190 nM in T84 cells assay. Plecanatide shows anti-inflammatory activity in models of murine colitis [3].
AP-C6 is a potent inhibitor of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII) with a pIC50 of 6.5. AP-C6 concentration-dependently inhibits human cGKII activity in vitro. AP-C6 potentiate cAMP signaling by PDE inhibition .
PDE1-IN-8 (Compound 3f) is the inhibitor for PDE1 with an IC50 of 11 nM. PDE1-IN-8 inhibits cAMP and cGMP signaling pathway, inhibits the differentiation and proliferation of cells into myofibroblast, and exhibits anti-fibrotic efficacy in Bleomycin (HY-17565)-induced rat pulmonary fibrosis model .
Plecanatide acetate, an analogue of Uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist. Plecanatide acetate activates GC-C receptors to stimulate cGMP synthesis with an EC50 of 190 nM in T84 cells assay. Plecanatide acetate can be used for the research of chronic idiopathic constipation, and it also shows anti-inflammatory activity in models of murine colitis [3].
SAL-0010042 is the inhibitor for Plasmodiumphosphodiesterase β (PDEβ), that inhibits the hydrolysis of cAMP and cGMP (IC50=48.9 nM) in gametocytes, activates PKG, and inhibits the growth and development of Plasmodium (IC50 for 3D7 and Dd2 is 142 nM and 218 nM). SAL-0010042 inhibits hPDE5 and hPDE6 with IC50 of 632 nM and 73 nM .
Phosphodiesterase II (EC 3.1.16.1), namely phosphodiesterase 2, is mainly involved in the hydrolysis of the important second messengers cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP), and is often used in biochemical research. Phosphodiesterase II is expressed in a variety of tissues, such as the adrenal medulla, brain, heart, platelets, macrophages and endothelial cells, and is involved in the regulation of many different intracellular processes .
Enoximone is an inotropic vasodilating agent and a selective and orally active phosphodiesterase III (PDE3) inhibitor with an IC50 of 5.9 μM. Enoximone induces vasodilatation and increases intracellular levels of cAMP by inhibiting cGMP-inhibited PDE. Enoximone also exhibits PDE4 inhibitory effect with an IC50 of 21.1 μM for myocardial PDE4A. Enoximone has the potential for congestive heart failure research and has bronchodilatory, antiasthma and anti-inflammatory effects [3].
Vasonatrin Peptide (VNP) is a chimera of atrial natriuretic peptide (ANP) and C-type natriuretic peptide (CNP). Vasonatrin peptide possesses the venodilating actions of CNP, the natriuretic actions of ANP, and unique arterial vasodilating actions not associated with either ANP or CNP. Vasonatrin Peptide protects the diabetic heart against ischemia-reperfusion injury by inhibiting ER stress via the cGMP-PKG signaling pathway [3].
3-O-Methylquercetin is an inhibitor of cAMP and CGMP-phosphodiesterase (PDE) with IC50 at 13.8 μM and 14.3 μM, respectively. 3-O-Methylquercetin is an inhibitor of β-secretase with an IC50 of 6.5 μM. 3-O-Methylquercetin has a neuroprotective effect against neuronal death caused by oxidative damage. 3-O-Methylquercetin has strong antiviral activity against poliovirus, coxsackie virus and human rhinovirus. 3-O-Methylquercetin has anti-inflammatory and trachea-relaxing effects and can be used in the study of inflammatory diseases and asthma [3] .
Cenderitide is a potent agonist of particulate guanylyl cyclase receptor (pGC). Cenderitide is a natriuretic peptide (NP) composed of C-type natriuretic peptide (CNP) fused to the C-terminus of Dendroaspis natriuretic peptide (DNP). Cenderitide activates both pGC-A and pGC-B, activates the second messenger cGMP, suppresses aldosterone, and preserves GFR without reducing blood pressure. Cenderitide can be used for heart failure research [3].
AP-C5 displays selective inhibition of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII) with a pIC50 of 7.2, which can be used for the research of diarrheal disease . AP-C5 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Vasonatrin Peptide (VNP) TFA is a chimera of atrial natriuretic peptide (ANP) and C-type natriuretic peptide (CNP). Vasonatrin peptide TFA possesses the venodilating actions of CNP, the natriuretic actions of ANP, and unique arterial vasodilating actions not associated with either ANP or CNP. Vasonatrin Peptide TFA protects the diabetic heart against ischemia-reperfusion injury by inhibiting ER stress via the cGMP-PKG signaling pathway [3].
Phosphodiesterase I (PDE) is an enzyme that can catalyze the hydrolysis of the 3' ring phosphate bond of cyclic nucleotides, and is often used in biochemical research. Phosphodiesterase I acts as an important regulator of signal transduction mediated by the second messenger molecules cAMP and cGMP. According to their specificity to cyclic nucleotides, they can also be divided into different types, such as PDE1-PDE11, which also have certain potential in various diseases .
ID11916 is an orally active androgen receptor (AR) antagonist and a phosphodiesterase 5 (PDE5) inhibitor. ID11916 blocks androgen binding to AR, nuclear translocation, and androgen-dependent transcriptional activity of AR, while increasing intracellular cGMP levels and activating PKG via inhibition. ID11916 shows potent anti-cancer effect in prostate cancer cell lines VCaP and 22Rv1 and in AR-positive breast cancer cell lines SK-BR-3 .
EHNA is a potent and selective dual inhibitor of cyclic nucleotide phosphodiesterase 2 (PDE2)(IC50=4 μM) and adenosine deaminase (ADA). EHNA exerts a concentration inhibition of the cGMP-stimulated PDE II (cGs-PDE)(IC50:0.8 μM (human), 2 μM (porcine myocardium)), but has smaller inhibitory effect on the unstimulated PDE2 activity. EHNA play roles in mediating diverse pharmacological responses, including antiviral, antitumour and antiarrhythmic effects [3].
MDL-100240 is a dual-acting angiotensin-converting enzyme (ACE) and neutral endopeptidase (NEP) inhibitor. MDL-100240 can significantly lower blood pressure, reverse left ventricular hypertrophy, and effectively prevent hypertrophy and dilatation of the aorta and resistance arteries, with an effect comparable to that of ramipril (HY-B0279). In addition, MDL-100240 can also reduce aldosterone levels, but has no significant effect on atrial natriuretic peptide and cGMP. In 3-month-old transgenic rats, MDL-100240 can reduce adrenomedullin concentrations, prevent and reverse severe hypertension and cardiovascular damage, and enhance bradykinin effects.
KT5823, a selective the cGMP-dependent protein kinase (PKG) inhibitor with an Ki value of 0.23 μM, it also inhibits PKA and PKC with Ki values of 10 μM and 4 μM, respectively. KT5823 is a Staurosporine-related protein kinase inhibitor, increases thyroid-stimulating hormone-induced (Na +/I - symporter) NIS expression, and iodide uptake in thyroid cells. KT5823 arrests cells after the G0/G1 boundary and causes increases in the levels of apoptotic DNA fragmentation [3] .
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) [3].
PDE1-IN-4 (compound 2g) is a potent and selective PDE1 (phosphodiesterase-1) inhibitor, with IC50 values of 10, 145, and 354 nM for PDE1C, PDE1A, and PDE1B, respectively. PDE1-IN-4 inhibits myofibroblast differentiation of human lung fibroblasts induced by TGF-β1. PDE1-IN-4 shows anti-fibrosis effects through the regulation of cAMP (3′,5′-cyclic adenosine monophosphate) and cGMP (3′,5′-cyclic guanosine monophosphate). PDE1-IN-4 can be used for idiopathic pulmonary fibrosis (IPF) research .
Cyclic GMP TBAOH is an endogenous second messenger that triggers interferon production in response to cytoplasmic DNA. Cyclic GMP TBAOH can activate the stimulator of interferon genes (STING), activating the signaling cascade that leads to the production of type I interferons and other immune mediators. Cyclic-GMP-AMP, a conjugate of cyclic GMP and AMP, can induce IRF3 phosphorylation and nuclear translocation, enhancing antiviral immune responses. Cyclic GMP TBAOH may also activate PDE to degrade cAMP, inhibit myocardial calcium current ICa, and regulate myocardial contractility. The derivative of Cyclic GMP TBAOH, 8-Br-cGMP, has antiplatelet activity, and Cyclic GMP TBAOH can be used in the study of antiviral immunity and cardiovascular diseases [3] .
Cyclic GMP (cGAMP) sodium is an endogenous second messenger that triggers interferon production in response to cytoplasmic DNA. Cyclic GMP sodium can activate the stimulator of interferon genes (STING), activating the signaling cascade that leads to the production of type I interferons and other immune mediators. Cyclic-GMP-AMP, a conjugate of cyclic GMP and AMP, can induce IRF3 phosphorylation and nuclear translocation, enhancing antiviral immune responses. Cyclic GMP sodium may also activate PDE to degrade cAMP, inhibit myocardial calcium current ICa, and regulate myocardial contractility. The derivative of Cyclic GMP sodium, 8-Br-cGMP, has antiplatelet activity, and Cyclic GMP sodium can be used in the study of antiviral immunity and cardiovascular diseases [3] .
Cyclic GMP (sodium) (Standard) is the analytical standard of Cyclic GMP (sodium). This product is intended for research and analytical applications. Cyclic GMP (cGAMP) sodium is an endogenous second messenger that triggers interferon production in response to cytoplasmic DNA. Cyclic GMP sodium can activate the stimulator of interferon genes (STING), activating the signaling cascade that leads to the production of type I interferons and other immune mediators. Cyclic-GMP-AMP, a conjugate of cyclic GMP and AMP, can induce IRF3 phosphorylation and nuclear translocation, enhancing antiviral immune responses. Cyclic GMP sodium may also activate PDE to degrade cAMP, inhibit myocardial calcium current ICa, and regulate myocardial contractility. The derivative of Cyclic GMP sodium, 8-Br-cGMP, has antiplatelet activity, and Cyclic GMP sodium can be used in the study of antiviral immunity and cardiovascular diseases [3] .
Cyclic GMP sodium- 13C5 is the 13C-labeled Cyclic GMP sodium (HY-113469A). Cyclic GMP (cGAMP) sodium is an endogenous second messenger that triggers interferon production in response to cytoplasmic DNA. Cyclic GMP sodium can activate the stimulator of interferon genes (STING), activating the signaling cascade that leads to the production of type I interferons and other immune mediators. Cyclic-GMP-AMP, a conjugate of cyclic GMP and AMP, can induce IRF3 phosphorylation and nuclear translocation, enhancing antiviral immune responses. Cyclic GMP sodium may also activate PDE to degrade cAMP, inhibit myocardial calcium current ICa, and regulate myocardial contractility. The derivative of Cyclic GMP sodium, 8-Br-cGMP, has antiplatelet activity, and Cyclic GMP sodium can be used in the study of antiviral immunity and cardiovascular diseases [3] .
Cyclic GMP (Standard) is the analytical standard of Cyclic GMP. This product is intended for research and analytical applications. Cyclic GMP is an endogenous second messenger that triggers interferon production in response to cytoplasmic DNA. Cyclic GMP can activate the stimulator of interferon genes (STING), activating the signaling cascade that leads to the production of type I interferons and other immune mediators. Cyclic-GMP-AMP, a conjugate of cyclic GMP and AMP, can induce IRF3 phosphorylation and nuclear translocation, enhancing antiviral immune responses. Cyclic GMP may also activate PDE to degrade cAMP, inhibit myocardial calcium current ICa, and regulate myocardial contractility. The derivative of Cyclic GMP, 8-Br-cGMP, has antiplatelet activity, and Cyclic GMP can be used in the study of antiviral immunity and cardiovascular diseases.
Cuminaldehyde Standard is the analytical standard of Cuminaldehyde. This product is intended for research and analytical applications. Cuminaldehyde is the main component of Cuminum cyminum and has multiple biological activities, including anti-inflammatory, anti-cancer, anti-diabetic, anti-injury, anti-neuropathy and antibacterial effects. Cuminaldehyde is an inhibitor of aldose reductase (IC50= 0.00085 mg/mL) and α-glucosidase (IC50=0.5 mg/mL). Cuminaldehyde also inhibits the fibrillation of α-synuclein and prevents its aggregation Cuminaldehyde can induce apoptosis in colon adenocarcinoma cells by targeting topoisomerase I and II. In addition, Cuminaldehyde also exerts anti-inflammatory activity by inhibiting lipoxygenase. Cuminaldehyde has a strong inhibitory effect on the growth of Aspergillus flavus and the biosynthesis of aflatoxin B1 (AFB1). Cuminaldehyde can exert anti-injury and anti-neuropathy effects by participating in opioid receptors, L-arginine/NO/cGMP pathways and anti-inflammatory effects. Cuminaldehyde has potential application value in the research of neurodegenerative diseases, cancer, diabetes and neuropathic pain diseases [3] .
Plecanatide, an analogue of Uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist. Plecanatide activates GC-C receptors to stimulate cGMP synthesis with an EC50 of 190 nM in T84 cells assay. Plecanatide shows anti-inflammatory activity in models of murine colitis [3].
Plecanatide acetate, an analogue of Uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist. Plecanatide acetate activates GC-C receptors to stimulate cGMP synthesis with an EC50 of 190 nM in T84 cells assay. Plecanatide acetate can be used for the research of chronic idiopathic constipation, and it also shows anti-inflammatory activity in models of murine colitis [3].
Cenderitide is a potent agonist of particulate guanylyl cyclase receptor (pGC). Cenderitide is a natriuretic peptide (NP) composed of C-type natriuretic peptide (CNP) fused to the C-terminus of Dendroaspis natriuretic peptide (DNP). Cenderitide activates both pGC-A and pGC-B, activates the second messenger cGMP, suppresses aldosterone, and preserves GFR without reducing blood pressure. Cenderitide can be used for heart failure research [3].
Vasonatrin Peptide (VNP) TFA is a chimera of atrial natriuretic peptide (ANP) and C-type natriuretic peptide (CNP). Vasonatrin peptide TFA possesses the venodilating actions of CNP, the natriuretic actions of ANP, and unique arterial vasodilating actions not associated with either ANP or CNP. Vasonatrin Peptide TFA protects the diabetic heart against ischemia-reperfusion injury by inhibiting ER stress via the cGMP-PKG signaling pathway [3].
Vasonatrin Peptide (VNP) is a chimera of atrial natriuretic peptide (ANP) and C-type natriuretic peptide (CNP). Vasonatrin peptide possesses the venodilating actions of CNP, the natriuretic actions of ANP, and unique arterial vasodilating actions not associated with either ANP or CNP. Vasonatrin Peptide protects the diabetic heart against ischemia-reperfusion injury by inhibiting ER stress via the cGMP-PKG signaling pathway [3].
Cyclic GMP (cGAMP) is an endogenous second messenger that triggers interferon production in response to cytoplasmic DNA. Cyclic GMP can activate the stimulator of interferon genes (STING), activating the signaling cascade that leads to the production of type I interferons and other immune mediators. Cyclic-GMP-AMP, a conjugate of cyclic GMP and AMP, can induce IRF3 phosphorylation and nuclear translocation, enhancing antiviral immune responses. cGMP may also activate PDE to degrade cAMP, inhibit myocardial calcium current ICa, and regulate myocardial contractility. The derivative of cyclic GMP (cGMP), 8-Br-cGMP, has antiplatelet activity, and cyclic GMP can be used in the study of antiviral immunity and cardiovascular diseases [3] .
Avanafil (TA-1790) is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis [3].
Vardenafil is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
Vardenafil hydrochloride trihydrate is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride trihydrate shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride trihydrate competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride trihydrate can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
Vardenafil dihydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil dihydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM respectively, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil dihydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil dihydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes - .
Avanafil (Standard) is the analytical standard of Avanafil. This product is intended for research and analytical applications. Avanafil (TA-1790) is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis [3].
Avanafil (Standard) is the analytical standard of Avanafil. This product is intended for research and analytical applications. Avanafil (TA-1790) is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis [3].
Avanafil (TA-1790) dibenzenesulfonate is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil dibenzenesulfonate activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil dibenzenesulfonate inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil dibenzenesulfonate can be used for the research of erectile dysfunction and osteoporosis [3].
Vardenafil (dihydrochloride) (Standard) is the analytical standard of Vardenafil (dihydrochloride). This product is intended for research and analytical applications. Vardenafil dihydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil dihydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM respectively, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil dihydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil dihydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes - .
Vardenafil (Standard) is the analytical standard of Vardenafil. This product is intended for research and analytical applications. Vardenafil is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
Vardenafil (dihydrochloride) (Standard) is the analytical standard of Vardenafil (dihydrochloride). This product is intended for research and analytical applications. Vardenafil dihydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil dihydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM respectively, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil dihydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil dihydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes - .
Vardenafil (hydrochloride trihydrate) (Standard) is the analytical standard of Vardenafil (hydrochloride trihydrate). This product is intended for research and analytical applications. Vardenafil hydrochloride trihydrate is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride trihydrate shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride trihydrate competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride trihydrate can be used for the research of erectile dysfunction, hepatitis, diabetes - .
3-O-Methylquercetin is an inhibitor of cAMP and CGMP-phosphodiesterase (PDE) with IC50 at 13.8 μM and 14.3 μM, respectively. 3-O-Methylquercetin is an inhibitor of β-secretase with an IC50 of 6.5 μM. 3-O-Methylquercetin has a neuroprotective effect against neuronal death caused by oxidative damage. 3-O-Methylquercetin has strong antiviral activity against poliovirus, coxsackie virus and human rhinovirus. 3-O-Methylquercetin has anti-inflammatory and trachea-relaxing effects and can be used in the study of inflammatory diseases and asthma [3] .
Cyclic GMP (cGAMP) sodium is an endogenous second messenger that triggers interferon production in response to cytoplasmic DNA. Cyclic GMP sodium can activate the stimulator of interferon genes (STING), activating the signaling cascade that leads to the production of type I interferons and other immune mediators. Cyclic-GMP-AMP, a conjugate of cyclic GMP and AMP, can induce IRF3 phosphorylation and nuclear translocation, enhancing antiviral immune responses. Cyclic GMP sodium may also activate PDE to degrade cAMP, inhibit myocardial calcium current ICa, and regulate myocardial contractility. The derivative of Cyclic GMP sodium, 8-Br-cGMP, has antiplatelet activity, and Cyclic GMP sodium can be used in the study of antiviral immunity and cardiovascular diseases [3] .
Cyclic GMP (sodium) (Standard) is the analytical standard of Cyclic GMP (sodium). This product is intended for research and analytical applications. Cyclic GMP (cGAMP) sodium is an endogenous second messenger that triggers interferon production in response to cytoplasmic DNA. Cyclic GMP sodium can activate the stimulator of interferon genes (STING), activating the signaling cascade that leads to the production of type I interferons and other immune mediators. Cyclic-GMP-AMP, a conjugate of cyclic GMP and AMP, can induce IRF3 phosphorylation and nuclear translocation, enhancing antiviral immune responses. Cyclic GMP sodium may also activate PDE to degrade cAMP, inhibit myocardial calcium current ICa, and regulate myocardial contractility. The derivative of Cyclic GMP sodium, 8-Br-cGMP, has antiplatelet activity, and Cyclic GMP sodium can be used in the study of antiviral immunity and cardiovascular diseases [3] .
Cyclic GMP (Standard) is the analytical standard of Cyclic GMP. This product is intended for research and analytical applications. Cyclic GMP is an endogenous second messenger that triggers interferon production in response to cytoplasmic DNA. Cyclic GMP can activate the stimulator of interferon genes (STING), activating the signaling cascade that leads to the production of type I interferons and other immune mediators. Cyclic-GMP-AMP, a conjugate of cyclic GMP and AMP, can induce IRF3 phosphorylation and nuclear translocation, enhancing antiviral immune responses. Cyclic GMP may also activate PDE to degrade cAMP, inhibit myocardial calcium current ICa, and regulate myocardial contractility. The derivative of Cyclic GMP, 8-Br-cGMP, has antiplatelet activity, and Cyclic GMP can be used in the study of antiviral immunity and cardiovascular diseases.
Cuminaldehyde Standard is the analytical standard of Cuminaldehyde. This product is intended for research and analytical applications. Cuminaldehyde is the main component of Cuminum cyminum and has multiple biological activities, including anti-inflammatory, anti-cancer, anti-diabetic, anti-injury, anti-neuropathy and antibacterial effects. Cuminaldehyde is an inhibitor of aldose reductase (IC50= 0.00085 mg/mL) and α-glucosidase (IC50=0.5 mg/mL). Cuminaldehyde also inhibits the fibrillation of α-synuclein and prevents its aggregation Cuminaldehyde can induce apoptosis in colon adenocarcinoma cells by targeting topoisomerase I and II. In addition, Cuminaldehyde also exerts anti-inflammatory activity by inhibiting lipoxygenase. Cuminaldehyde has a strong inhibitory effect on the growth of Aspergillus flavus and the biosynthesis of aflatoxin B1 (AFB1). Cuminaldehyde can exert anti-injury and anti-neuropathy effects by participating in opioid receptors, L-arginine/NO/cGMP pathways and anti-inflammatory effects. Cuminaldehyde has potential application value in the research of neurodegenerative diseases, cancer, diabetes and neuropathic pain diseases [3] .
cGB-PDE protein regulates signal transduction by specifically hydrolyzing cto 5'-GMP, thereby controlling the intracellular concentration of cyclic nucleotides, particularly nitric-oxide-generated cGMP. cGB-PDE Protein, Mouse (Myc, His) is the recombinant mouse-derived cGB-PDE protein, expressed by E. coli , with N-His, C-Myc labeled tag.
PDE3A protein, a cyclic nucleotide phosphodiesterase, targets cAMP, cGMP, and cUMP, crucial in diverse physiological processes. In an E2/17beta-estradiol-induced pro-apoptotic pathway, E2 stabilizes the PDE3A/SLFN12 complex, leading to SLFN12 dephosphorylation and activating its pro-apoptotic ribonuclease activity. This pathway is implicated in tissues with high E2 concentrations, potentially contributing to processes like placenta remodeling. PDE3A Protein, Human (sf9, His-GST) is the recombinant human-derived PDE3A protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag.
PDE2A is a cGMP-activated cyclic nucleotide phosphodiesterase that exhibits dual specificity for the second messengers cAMP and cGMP, key regulators in various physiological processes. PDE2A exhibits higher efficiency by covering cAMP and plays an important role in cell growth and migration. PDE2A Protein, Human (sf9, His) is the recombinant human-derived PDE2A protein, expressed by Sf9 insect cells , with C-His labeled tag.
PDE9A is a phosphodiesterase that uniquely hydrolyzes second messengers with unparalleled specificity, particularly in the regulation of natriuretic peptide-dependent signaling in the heart, which is critical for the control of cardiac hypertrophy. Its specificity rules out effects on nitric oxide-dependent signaling in the heart. PDE9A Protein, Human (His) is the recombinant human-derived PDE9A protein, expressed by E. coli , with N-His labeled tag.
PDE9A is a phosphodiesterase that uniquely hydrolyzes second messengers with unparalleled specificity, particularly in the regulation of natriuretic peptide-dependent signaling in the heart, which is critical for the control of cardiac hypertrophy. Its specificity rules out effects on nitric oxide-dependent signaling in the heart. PDE9A Protein, Human (sf9, His-GST) is the recombinant human-derived PDE9A protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag.
Vardenafil-d5 is deuterium labeled Vardenafil. Vardenafil is a selective, orally active, potent inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows selectivity over PDE1 (180 nM), PDE6 (11 nM), PDE2, PDE3, and PDE4 (>1000 nM). Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil can be used for the research of erectile dysfunction .
Avanafil- 13C5 (TA1790- 13C5) is 13C labeled Avanafil. Avanafil (TA-1790) is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis [3].
Avanafil- 13C5, 15N,d2 is 15N and deuterated labeled Avanafil (HY-18252). Avanafil (TA-1790) is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis [3].
Vardenafil-d5 hydrochloride is deuterated labeled Vardenafil hydrochloride (HY-B0442A). Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
Cyclic GMP sodium- 13C5 is the 13C-labeled Cyclic GMP sodium (HY-113469A). Cyclic GMP (cGAMP) sodium is an endogenous second messenger that triggers interferon production in response to cytoplasmic DNA. Cyclic GMP sodium can activate the stimulator of interferon genes (STING), activating the signaling cascade that leads to the production of type I interferons and other immune mediators. Cyclic-GMP-AMP, a conjugate of cyclic GMP and AMP, can induce IRF3 phosphorylation and nuclear translocation, enhancing antiviral immune responses. Cyclic GMP sodium may also activate PDE to degrade cAMP, inhibit myocardial calcium current ICa, and regulate myocardial contractility. The derivative of Cyclic GMP sodium, 8-Br-cGMP, has antiplatelet activity, and Cyclic GMP sodium can be used in the study of antiviral immunity and cardiovascular diseases [3] .
AP-C5 displays selective inhibition of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII) with a pIC50 of 7.2, which can be used for the research of diarrheal disease . AP-C5 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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