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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
228 Results for "
CGMP
" in MedChemExpress (MCE) Product Catalog:
Products (228)
228 Results for "CGMP" in MCE Product Catalog:
Cat. No.: HY-165568
CAS No.: 76470-87-6
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OPC 3911 is a highly selective inhibitor of cGMP-inhibited cAMP phosphodiesterase (cGI-PDE/PDE3) and a vasodilator, with an IC50 of 0.042 μM against rat cGI-PDE. OPC 3911 upregulates the expression of Osteopontin. OPC 3911 mediates vasodilation of arterial smooth muscle, induces vasodilatory responses in isolated rat arteriovenous tissues, and exhibits additive vasodilatory effects with Isoprenaline (HY-108353) and Forskolin (HY-15371). OPC 3911 can be used in studies related to congestive heart failure and insulin resistance .
Cat. No.: HY-P11861
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Cat. No.: HY-103160AR
CAS No.: 58337-38-5
Research Areas:
Infection Cardiovascular Disease Neurological Disease Cancer
EHNA hydrochloride (Standard) is the analytical standard of EHNA hydrochloride (HY-103160A). This product is intended for research and analytical applications. EHNA hydrochloride is a potent and selective dual inhibitor of cyclic nucleotide phosphodiesterase 2 (PDE2)(IC50=4 μM) and adenosine deaminase (ADA). EHNA hydrochloride 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 hydrochloride play roles in mediating diverse pharmacological responses, including antiviral, antitumour and antiarrhythmic effects .
Cat. No.: HY-131691
CAS No.: 76991-05-4
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NMDAR blocker 1 is an NMDA receptor channel blocker with an IC50 of 5.0 μM. NMDAR blocker 1 exhibits fast on-off blockade kinetics and strong voltage dependence, and does not compete with glutamate or glycine. NMDAR blocker 1 prevents glutamate/NMDA-induced intracellular Ca 2+ overload, modulates the glutamate-nitric oxide-cGMP pathway. NMDAR blocker 1 prevents in vitro excitotoxic neurodegeneration of cultured cerebellar and hippocampal neurons. NMDAR blocker 1 attenuates excitotoxic insult in an mouse model of hyperammonemia-induced excitotoxicity. NMDAR blocker 1 can be used for the research of neurodegenerative diseases .
Cat. No.: HY-182638
CAS No.: 1829530-11-1
Synonyms: CPL500036
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Alofropodect is an orally active, blood-brain barrier permeable phosphodiesterase 10A (PDE10A) inhibitor with IC50 values of 1 nM (Reference 1) and 35 nM (Reference 2). Alofropodect acts as a negative allosteric modulator of the M2 muscarinic receptor with an IC50 of 9.2 μM. Alofropodect alters cyclic nucleotide levels in basal ganglia circuits, inhibits the hydrolysis of cAMP and cGMP, and suppresses hERG potassium channel tail currents. Alofropodect induces catalepsy in rats and reverses injury-induced contralateral forelimb use impairment. Alofropodect can be used in research related to schizophrenia, Parkinson's disease, and levodopa-induced dyskinesia .
Cat. No.: HY-187700
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BRD3290 is a GluA3-preferring AMPA receptor positive allosteric modulator with brain exposure in Mus musculus (mice) following peripheral administration. BRD3290 preferentially potentiates GluA3-containing AMPA receptors over GluA1/2-containing AMPA receptors. BRD3290 increases cerebellar cGMP levels in Mus musculus (mice). BRD3290 does not induce convulsions, alter motor function, or improve novel object recognition task performance in Mus musculus (mice) at tested doses. BRD3290 can be used for the research of schizophrenia .
Cat. No.: HY-W795967
CAS No.: 108605-69-2
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Cat. No.: HY-100113A
CAS No.: 1947313-60-1
Synonyms: AT2 receptor agonist C21 hydrochloride
Research Areas:
Cardiovascular Disease Neurological Disease Inflammation/Immunology
Buloxibutid (AT2 receptor agonist C21) hydrochloride is an orally active, selective angiotensin II type 2 receptor (AT2R) agonist, with a Ki value of 0.4 nM for porcine AT2R. Buloxibutid hydrochloride exerts vasodilatory, anti-inflammatory, antifibrotic (promoting the expression of collagenase MMP-13) and tissue repair effects mainly by activating the NO/cGMP pathway, inhibiting the pro-proliferative MAPK signaling, and suppressing the pro-fibrotic TGF-β/Smad pathway and inflammatory NF-κB pathway. Buloxibutid hydrochloride can be used in research related to idiopathic pulmonary fibrosis, hypertension, systemic sclerosis and other conditions .
Cat. No.: HY-118264
CAS No.: 142695-08-7
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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.
Cat. No.: HY-178191
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sGC stimulator 1 is a carbonyl sulfide (COS)/H2S-donor hybrid soluble guanylyl cyclase (sGC) stimulator (EC50 = 496 nM). sGC stimulator 1 exhibits a well-characterized H2S-releasing property. sGC stimulator 1 reduces fibrosis in TGF-β1-treated cardiac fibroblasts by increasing cGMP and H2S levels. sGC stimulator 1 can exert anti-fibrotic effects by activating sGC and increasing H2S. sGC stimulator 1 can be used for the study of heart failure (HF) .
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Flavonoids Flavones Aconitum apetalum (Huth) B. Fedtsch. Plants Disease Research Fields Inflammation/Immunology Rhamnaceae Extract
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Cat. No.: HY-120314
CAS No.: 144576-10-3
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GEA 3162 is an orally active compound that acts as a NO/ONOO⁻ donor. GEA 3162 significantly inhibits the activation of human polymorphonuclear leukocytes (PMNs) through the cGMP pathway, inhibits the release of inflammatory mediators, and exerts anti-inflammatory and protective effects. GEA 3162 induces apoptosis of neutrophils and bone marrow cells by activating caspase-2/3/8/9 through the ONOO⁻ pathway. GEA 3162 has a bidirectional effect in the rat gastric ulcer model: at low doses, it significantly reduces gastric mucosal damage, while at high doses, it aggravates the ulcer area. GEA 3162 can be used for research on inflammatory conditions such as gastric ulcers .
Cat. No.: HY-120314A
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GEA 3162 hydrochloride is an orally active compound that acts as a NO/ONOO⁻ donor. GEA 3162 hydrochloride significantly inhibits the activation of human polymorphonuclear leukocytes (PMNs) through the cGMP pathway, inhibits the release of inflammatory mediators, and exerts anti-inflammatory and protective effects. GEA 3162 hydrochloride induces apoptosis of neutrophils and bone marrow cells by activating caspase-2/3/8/9 through the ONOO⁻ pathway. GEA 3162 hydrochloride has a bidirectional effect in the rat gastric ulcer model: at low doses, it significantly reduces gastric mucosal damage, while at high doses, it aggravates the ulcer area. GEA 3162 hydrochloride can be used for research on inflammatory conditions such as gastric ulcers .
Cat. No.: HY-180916
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CAII-IN-11 (Compound A1) is a dual-target compound that contains a hCA II inhibitor (IC₅₀ = 2 nM) portion and a NO donor portion. CAII-IN-11 also has inhibitory activity against hCA IX, hCA XII, and hCA I, with IC50 values of 6, 3, and 152 nM respectively. CAII-IN-11 significantly increases the intracellular cGMP level in human trabecular meshwork cells. CAII-IN-11 reduces the apoptosis of retinal ganglion cells by reducing oxidative stress (ROS levels), inhibiting astrocytes and the NLRP3 inflammasome activation. CAII-IN-11 has hypotensive activity in rabbit models and can be used for the study of glaucoma .
Cat. No.: HY-183644
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LNO 9 is an orally active LOXL2 inhibitor and NO donor, with an IC50 of 0.17 μM against human LOXL2. LNO 9 competitively binds to the LTQ cofactor of LOXL2 to form an irreversible complex, thereby inhibiting collagen oxidation and abnormal cross-linking. LNO 9 releases nitric oxide (NO) to increase cGMP levels in pulmonary artery smooth muscle cells. LNO 9 inhibits hypoxia-induced collagen modification and possesses vasodilatory activity. LNO 9 ameliorates right ventricular hypertrophy and pulmonary artery medial thickness in rat models induced by hypoxia and Monocrotaline (HY-N0750), and can be used for research on pulmonary hypertension .
Cat. No.: HY-18740
CAS No.: 79855-88-2
Synonyms: HL 725 free base
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Trequinsin (HL 725 free base) is a PDE inhibitor, CatSper channel activator, and sperm potassium channel modulator. Trequinsin targets PDE3 with an IC50 of <1 nM. Trequinsin enhances currents and elevates intracellular calcium and cGMP levels via direct activation of the CatSper channel, while inhibiting the outward current conductance of sperm potassium channels. Without inducing premature acrosome reaction, Trequinsin significantly enhances sperm hyperactivated motility, forward motility, and the ability to penetrate viscous media. Trequinsin exerts age-specific positive inotropic and positive lusitropic effects on rabbit ventricular papillary muscles. Trequinsin has been used in studies on the mechanisms underlying male infertility (e.g., asthenozoospermia) .
Cat. No.: HY-18740A
CAS No.: 78416-81-6
Synonyms: HL 725
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Trequinsin hydrochloride (HL 725) is a PDE inhibitor, CatSper channel activator, and sperm potassium channel modulator. Trequinsin hydrochloride targets PDE3 with an IC50 of <1 nM. Trequinsin hydrochloride enhances currents and elevates intracellular calcium and cGMP levels via direct activation of the CatSper channel, while inhibiting the outward current conductance of sperm potassium channels. Without inducing premature acrosome reaction, Trequinsin hydrochloride significantly enhances sperm hyperactivated motility, forward motility, and the ability to penetrate viscous media. Trequinsin hydrochloride exerts age-specific positive inotropic and positive lusitropic effects on rabbit ventricular papillary muscles. Trequinsin hydrochloride has been used in studies on the mechanisms underlying male infertility (e.g., asthenozoospermia) .
Cat. No.: HY-N3320
CAS No.: 14957-38-1
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Cat. No.: HY-109136R
CAS No.: 1402936-61-1
Synonyms: BAY 1101042 (Standard)
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Runcaciguat (Standard) is the analytical standard of Runcaciguat (HY-109136). This product is intended for research and analytical applications. 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) .
Cat. No.: HY-147946
CAS No.: 3031349-98-8
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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 .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
