chronic kidney disease

Finerenone (BAY-948862) is a nonsteroidal antagonist of the mineralocorticoid receptor (MR) (IC50=18 nM) with selective and oral activity. Finerenone is used in the treatment of patients with chronic kidney disease with type 2 diabetes.

Bis-T-23 is a promoter of actin-dependent dynamin oligomerization, an HIV-I integrase inhibitor, and a Telstar derivative. Bis-T-23 promotes actin-dependent dynamin oligomerization. Bis-T-23 can be used in studies of HIV and chronic kidney disease (CKD).

6-Acryloyloxyhexyl phosphater (PA21) is a novel phosphate-binding agent, which is an iron-based reagent, and can be used for the treatment of hyperphosphatemia in chronic kidney disease.

Avosentan(Ro 67-0565; SPP-301) is a potent endothelin receptor (ETA) antagonist with strong inhibitory effects on endothelin-1-induced contraction and may have protective effects against chronic kidney disease. [2]

Calcium polystyrene sulfonate (Poly(styrenesulfonic acid) calcium salt) is an ion-exchange resin. Calcium polystyrene sulfonate reduces blood levels of potassium and can be used for research on the treatment of hyperkalemia in patients with chronic kidney disease.

5-Hydroxy-1-methylhydantoin (HD-003) is an antioxidant potentially for the treatment of renal failure. A creatinine metabolite, 5-Hydroxy-1-methylhydantoin , a hydroxyl radical scavenger, has previously been shown to confer renoprotection by inhibiting the progression of chronic kidney disease in rats. 5-Hydroxy-1-methylhydantoin is a novel anti-oxidant drug completely suppressed the expression of B2-kinin receptors (B2KR) in response to high glucose (25 mM) stimulation in VSMC and was also shown to attenuate the effects of BK on VSMC remodeling. 5-Hydroxy-1-methylhydantoin inhibited the BK-induced increase in MAPK phosphorylation and attenuated the increase in connective tissue growth factor (CTGF) protein levels in VSMC. These findings suggest that 5-Hydroxy-1-methylhydantoin may confer vascular protection against high glucose concentrations and BK-stimulation to ameliorate vascular injury and remodeling through its anti-oxidant properties.

CDDO-dhTFEA, a synthetic oleanane triterpenoid, effectively activates Nrf2 while inhibiting the NF-κB pro-inflammatory transcription factor. It restores mean arterial pressure (MAP), elevates Nrf2 levels and the expression of related genes, attenuates NF-κB and transforming growth factor-β pathway activation, and mitigates glomerulosclerosis, interstitial fibrosis, and inflammation in rats with chronic kidney disease (CKD).

12-Ketodeoxycholic acid, a bile acid and kidney metabolite, serves as a detectable marker for kidney injury [1].

PFI-2 is an effective, specific and cell-active lysine methyltransferase SETD7 inhibitor (Ki IC50: 0.33 2 nM), 1000-fold selectivity over other methyltransferases and other non-epigenetic targets.

DDO-3055 is an orally active PHD2 inhibitor utilized in studies related to anemia associated with chronic kidney disease.

PHM-2-167 (Compound 11) is a selective inhibitor of the prolyl hydroxylase domain enzyme (PHD). It inhibits PHD2 and PHD3 with IC50 values of 0.253 μM and 3.95 μM, respectively. PHM-2-167 is applicable for research in chronic kidney disease.

PHD2-IN-4 (compound 1) is an inhibitor of PHD2, with an IC50 of 4 nM. It is utilized in research related to chronic kidney disease.

p-Cresyl Sulfate is the major uremic toxin present in the blood of patients with chronic kidney disease and is derived from the metabolites of tyrosine and phenylalanine in the liver.

Iron Sorbitex is used for the treatment of Iron Sorbitex deficiency anemia in patients with chronic kidney disease. Iron Sorbitex can be used as an Iron Sorbitex replacement product used for the treatment of Iron Sorbitex deficiency anemia in patients wit

Resolvin E2 (RvE2) is a member of the specialized pro-resolving mediator (SPM) family of bioactive lipids.1It is produced from eicosapentaenoic acidviaan 18-HEPE intermediate, which is formed by aspirin-acetylated COX-2-mediated oxidation of EPA, by 5-lipoxygenase (5-LO) in human polymorphonuclear (PMN) neutrophils.2,3RvE2 (20 ng/animal) inhibits increases in inflammatory exudate neutrophil infiltration in a mouse model of peritonitis induced by zymosan A .3Hepatic RvE2 levels are increased in mice fed normal chow, as well as in a mouse model of high-fat diet-induced non-alcoholic fatty liver disease (NAFLD), by dietary supplementation with EPA.4Plasma levels of RvE2 are increased by dietary supplementation with fish oil containing ω-3 polyunsaturated fatty acids (PUFAs) in patients with peripheral artery disease or chronic kidney disease.1,5,6 1.Chiang, N., and Serhan, C.N.Specialized pro-resolving mediator network: An update on production and actionsEssays Biochem.64(3)443-462(2020) 2.Tjonahen, E., Oh, S.F., Siegelman, J., et al.Resolvin E2: Identification and anti-inflammatory actions: Pivotal role of human 5-lipoxygenase in resolvin E series biosynthesisChemistry & Biology131193-1202(2006) 3.Sungwhan, F.O., Pillai, P.S., Recchiuti, A., et al.Pro-resolving actions and stereoselective biosynthesis of 18S E-series resolvins in human leukocytes and murine inflammationJ. Clin. Invest.121(2)569-581(2011) 4.Echeverría, F., Valenzuela, R., Espinosa, A., et al.Reduction of high-fat diet-induced liver proinflammatory state by eicosapentaenoic acid plus hydroxytyrosol supplementation: Involvement of resolvins RvE1/2 and RvD1/2J. Nutr. Biochem.6335-43(2019) 5.Ramirez, J.L., Gasper, W.J., Khetani, S.A., et al.Fish oil increases specialized pro-resolving lipid mediators in PAD (the OMEGA-PAD II trial)J. Surg. Res.238164-174(2019) 6.Barden, A.E., Shinde, S., Burke, V., et al.The effect of n-3 fatty acids and coenzyme Q10 supplementation on neutrophil leukotrienes, mediators of inflammation resolution and myeloperoxidase in chronic kidney diseaseProstaglandins Other Lipid Mediat.1361-8(2018)

L-Tyrosine-13C9,15N is intended for use as an internal standard for the quantification of L-tyrosine by GC- or LC-MS. L-Tyrosine is a non-essential amino acid.1It is produced by hydroxylation of phenylalanine by phenylalanine hydroxylase but can also be obtained from dietary sources or degradation of endogenous proteins, resulting in L-tyrosine release.1,2L-Tyrosine is a precursor in the biosynthesis of catecholamine neurotransmitters, melanins, and thyroid hormones.3Plasma, skeletal muscle, and erythrocyte levels of L-tyrosine are decreased in patients with chronic kidney disease.1 1.Kopple, J.D.Phenylalanine and tyrosine metabolism in chronic kidney failureJ. Nutr.137(6 Suppl 1)1586S-1590S(2007) 2.Webster, D., and Wildgoose, J.Tyrosine supplementation for phenylketonuriaCochrane DB Syst. Rev.2013(6)CD001507(2013) 3.Slominski, A., and Paus, R.Towards defining receptors for L-tyrosine and L-DOPAMol. Cell Endocrinol.99(2)C7-C11(1994)

Difelikefalin (CR-845; FE-202845) is a peripherally restricted, selective kappa opioid receptor (KOR) agonist with anti-inflammatory properties, demonstrating potential for modulating pruritus in chronic kidney disease.

Zevaquenabant ((S)-MRI-1867), a dual cannabinoid CB1 receptor and inducible NOS (iNOS) antagonist, is orally bioavailable and peripherally restricted. It effectively mitigates obesity-induced chronic kidney disease (CKD).

DDR1-IN-4 (Compound 2.45) is a highly potent inhibitor that selectively targets Discoidin Domain Receptor 1 (DDR1) autophosphorylation, demonstrating exceptional efficacy with IC50 values of 29 nM for DDR1 and 1.9 μM for DDR2.

PFI-2 hydrochloride ((R)-PFI-2 hydrochloride) is a potent, highly selective, and cell-active inhibitor of the methyltransferase activity of SETD7 (IC50: 2 nM), 500 fold active than (S)-PFI-2.

Vadadustat is a novel, titratable, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor in development for the treatment of anemia.

Potassium 1H-indol-3-yl sulfate (Potassium 3-indoxyl sulfate) is an agonist for the human Aryl Hydrocarbon Receptor (AhR), a key regulator of immune-inflammatory conditions. A metabolite of tryptophan derived from dietary protein, it is produced by intestinal bacteria and metabolized in the liver. In chronic kidney disease patients with impaired renal function, it accumulates in serum as a uremic toxin, inducing oxidative stress and accelerating disease progression. At 250 μM, it activates NF-Κb, promoting TGF-β1 and Smad3 expression in rat proximal tubular cells, which is associated with profibrotic activity.

SSAO inhibitor-2 (Compound 1) is an inhibitor of semicarbazide-sensitive amine oxidase (SSAO) with IC50 values <10 nM for human SSAO and 10-100 μM for MAO-A, respectively [1]. It can be used in the research of atherosclerosis, diabetes and its complications, obesity, stroke, chronic kidney disease, retinopathy, chronic obstructive pulmonary disease (COPD), autoimmune diseases, and multiple sclerosis.

SSAO inhibitor-3 (Compound 2) is an inhibitor of semicarbazide-sensitive amine oxidase (SSAO) with IC50 values of 0.1-10 μM and <10 nM for human AOC1 and SSAO, respectively, and can be used in the study of atherosclerosis, diabetes and its complications, obesity, stroke, chronic kidney disease, retinopathy, chronic obstructive pulmonary disease (COPD), autoimmune diseases, and multiple sclerosis, etc. [1].