GSK-2181236A

  Cat. No.:  DC70145  
Chemical Structure
1160426-89-0
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More than 5000 active chemicals with high quality for research!
Field of application
A potent, selective soluble guanylate cyclase (sGC) stimulator that increases sGC activity (cGMP formation) with EC50s of 27 and 25 nM for rat and human sGC, respectively; displays 23-fold selectivity for sGC over OATP1B1 and >197-fold selectivity over a panel of 38 proteins; increases P-VASP levels in rat aortic smooth muscle cells with EC50 of 12.7 nM; attenuates the development of cardiac hypertrophy in a blood pressure-independent fashion.
Cas No.: 1160426-89-0
Chemical Name: GSK-2181236A
Synonyms: GSK 2181236A;GSK2181236A
Formula: C31H21F6N3O4
M.Wt: 613.14
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
DC70592 MCUF-651 MCUF-651 (MCUF651) is a small molecule guanylyl cyclase A receptor (GC-A) positive allosteric modulator (PAM), potentiate ANP-mediated cGMP with EC50 of 0.45 uM (Emax=82%) in HEK293 GC-A cells.MCUF-651 enhanced ANP-mediated cGMP generation in human cardiac, renal, and fat cells and inhibited cardiomyocyte hypertrophy in vitro.MCUF-651 binds to GC-A (Kd=397 nM) and selectively enhances the binding of ANP to GC-A ( MCUF-651+ANP, Kd=0.06 nM).MCUF-651 is orally bioavailable in mice and enhances the ability of endogenous ANP and BNP to generate GC-A-mediated cGMP ex vivo.
DC40112 Plecanatide 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.
DC11526 Praliciguat Praliciguat (IW-1973, IW1973) is a potent, orally available sGC stimulator that concentration-dependently increases the production of cGMP with EC50 of 267 nM.
DC7782 BAY 41-2272 Activator of soluble guanylyl cyclase (sGC); acts at a nitric oxide (NO)-independent regulatory site in the sGC α1 subunit. Inhibits platelet aggregation (IC50 = 36 nM) and phenylephrine-induced contractions of rabbit aorta (IC50 = 0.30 μM). Also reduces vascular smooth muscle growth through cAMP- and cGMP-dependent PKA and PKG pathways.. For the detailed information of BAY 41-2272, the solubility of BAY 41-2272 in water, the solubility of BAY 41-2272 in DMSO, the solubility of BAY 41-2272 in PBS buffer, the animal experiment (test) of BAY 41-2272, the cell expriment (test) of BAY 41-2272, the in vivo, in vitro and clinical trial test of BAY 41-2272, the EC50, IC50,and affinity,of BAY 41-2272, Please contact DC Chemicals.
DC11904 Olinciguat (IW-1701) 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.
DC70731 Rat C53 peptide Rat C53 peptide (C53, pGC-B activator C53) is a novel potent, selective particulate guanylyl cyclase B (pGC-B) activator, activates pGC-B/cGMP signaling pathway, and enhances cGMP generating actions.C53 is highly resistant to NEP degradation and has less interaction with NPRC compared to CNP in vitro.C53 activates the protective pGC-B/cGMP signaling pathway and possesses enhanced cGMP generating actions.C53 inhibits fibroblast proliferation chronically and suppresses the differentiation of fibroblasts to myofibroblasts.
DC70498 Human C53 peptide Human C53 peptide (C53, pGC-B activator C53) is a novel potent, selective particulate guanylyl cyclase B (pGC-B) activator, activates pGC-B/cGMP signaling pathway, and enhances cGMP generating actions.C53 is highly resistant to NEP degradation and has less interaction with NPRC compared to CNP in vitro.C53 activates the protective pGC-B/cGMP signaling pathway and possesses enhanced cGMP generating actions.C53 inhibits fibroblast proliferation chronically and suppresses the differentiation of fibroblasts to myofibroblasts.
DC70329 C-type natriuretic peptide C-type natriuretic peptide (CNP, pGC-B activator) is the native particulate guanylyl cyclase B receptor (pGC-B) activator.CNP induces anti-remodeling actions in the heart and kidney through the generation of the second messenger cGMP.CNP selectively activates pGC-B and generates cGMP in vitro.CNP is abundantly expressed in the endothelium and kidneys as well as the heart, but to lesser extent than trial natriuretic peptide (ANP) and b-type natriuretic peptide (BNP).CNP is produced as a prohormone that is cleaved intracellularly by the enzyme, furin, to yield a 53-AA intermediate form (C53).
DC70145 GSK-2181236A A potent, selective soluble guanylate cyclase (sGC) stimulator that increases sGC activity (cGMP formation) with EC50s of 27 and 25 nM for rat and human sGC, respectively; displays 23-fold selectivity for sGC over OATP1B1 and >197-fold selectivity over a panel of 38 proteins; increases P-VASP levels in rat aortic smooth muscle cells with EC50 of 12.7 nM; attenuates the development of cardiac hypertrophy in a blood pressure-independent fashion.
DC48911 CFM 1571 hydrochloride CFM 1571 hydrochloride is the stimulator of the nitric oxide receptor, soluble guanylate cyclase (sGC) with an EC50 and IC50 of 5.49 μM and 2.84 μM, respectively. Soluble guanylate cyclase (sGC) is a key signal-transduction enzyme activated by nitric oxide (NO). CFM 1571 (hydrochloride) (compound 32) has the potential for the research of cardiovascular and other diseases.
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