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).

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]

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.

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.

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.

Roxadustat-d5 is intended for use as an internal standard for the quantification of roxadustat by GC- or LC-MS. Roxadustat is an inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH; IC50s = 1.4, 1.26, and 1.32 µM for HIF-PH1, HIF-PH2, and HIF-PH3, respectively). It is selective for HIF-PH over other 2-oxoglutarate-dependent dioxygenases, including lysine-specific demethylase 5A (KDM5A), KDM5B, -5C, -5D, and -6B (IC50s = >100 µM for all). Roxadustat (10-200 µM) stabilizes HIF-1α and HIF-2α in Hep3B hepatocellular carcinoma cells. It increases levels of secreted erythropoietin in Hep3B cells in a concentration-dependent manner and increases erythropoiesis in rats when administered at doses of 25 and 50 mg kg. Roxadustat reverses anemia in a rat model of chronic inflammation induced by peptidoglycan-polysaccharide, as well as a rat model of chronic kidney disease induced by 5 6 nephrectomy. It reduces tumor growth and increases survival in a murine Lewis lung carcin......

EPI-X4, an endogenous peptide fragment of human serum albumin (amino acids 408-423), serves as an antagonist to the chemokine (C-X-C motif) receptor 4 (CXCR4). It effectively prevents calcium mobilization and receptor internalization triggered by chemokine (C-X-C motif) ligand 12 (CXCL12) in HEK293 cells with CXCR4 expression, at concentrations between 0.8 and 1,000 µM. Moreover, EPI-X4 hampers the CXCL12-driven migration of both Jurkat T cells and human CD34+ hematopoietic stem cells. In an acute allergic airway hypereosinophilia mouse model, EPI-X4 intrinsically decreases Cxcr4-dependent inflammatory cell infiltration in airways at a dose of 16 µmol/kg. Additionally, increased urinary EPI-X4 levels, inversely related to glomerular filtration rate (GFR), are observed in chronic kidney disease patients, indicating its potential biomarker role.

BRD4 Inhibitor-32 (example 15), a BRD4 inhibitor, is applicable in research pertaining to both acute and chronic kidney disease [1].

TRPC5-IN-1 is a TRPC5 inhibitor active in various animal models of chronic kidney disease.

COR-001, a human anti-IL-6 monoclonal antibody, efficiently lowers serum CRP levels and exhibits anti-inflammatory properties. It is potentially useful in researching chronic systemic inflammation and cardiovascular diseases linked to chronic kidney disease (CKD) [1].

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).

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

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)

OK2, a specific inhibitor of the CCN2 EGFR interaction, effectively disrupts this interaction by binding to the CT domain of CCN2 and holds potential for research on kidney fibrosis and chronic kidney disease [1].

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.

KP-6 is a peptide that acts as an inhibitor of the Wnt β-catenin signaling pathway. It suppresses TGF-β and disrupts key signals that lead to rapid fibrosis in vivo. KP-6 helps prevent kidney tissue damage and fibrosis, offering the potential to reverse the progression of chronic kidney disease (CKD).

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).

Oleoyl-L-carnitine, a long-chain acylcarnitine, acts as a selective inhibitor of glycine transporter 2 (GlyT2; IC50 = 340 nM) while demonstrating significantly lesser affinity for GlyT1 (IC50 = >10,000 nM). Elevated plasma levels of this compound have been observed in patients suffering from chronic kidney disease or end-stage renal disease undergoing initial hemodialysis, correlating with an increased risk of cardiovascular mortality.

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.

AZD9977 is a novel, selective modulator of mineralocorticoid receptor .

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].

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.

TRPC5-IN-4, a potent and safe TRPC inhibitor, exhibits IC50 values of 14.07 nM and 65 nM for TRPC5 and TRPC4, respectively, indicating high efficacy. It does not cause damage to liver and kidney cellular components, making it suitable for chronic kidney disease (CKD) research [1].