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]

BLU2864 is an orally active, highly selective, ATP-competitive PRKACA inhibitor with an IC50 of 0.3 nM, exhibiting anti-tumor activity and potential applications in cancer and polycystic kidney disease research [1] [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.

Irbesartan (SR-47436) is an Angiotensin 2 Receptor Blocker whose mechanism of action involves antagonizing the Angiotensin 2 Receptor.

Bisphenol A is an endogenous metabolic compound of phenols and is widely used in the production of epoxy resins and polycarbonate plastics. It is reproductive, developmental and systemic toxicant and is often classified as an endocrine disruptor. It has been linked to many diseases, including respiratory disease, cardiovascular disease, diabetes, kidney disease, obesity and reproductive disorders.

GFB-8438 is a potent and subtype selective inhibitor of TRPC5(IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively).

Trapidil (Avantrin) is a coronary vasodilator agent. It was originally developed as a vasodilator and anti-platelet agent and has been used to treat patients with ischemic coronary heart, liver, and kidney disease.

2-Iodohippuric Acid can be used to measure renal clearance for renal function studies, and for the diagnosis of certain diseases, such as liver and kidney disease. In addition, it is used in the synthesis of certain drugs.

Ocedurenone, a corticosteroid receptor antagonist, is a compound utilized in the investigation of kidney disease (WO2018054357, compound I).

Polythiazide (NSC-108161, P-2525) is used to treat fluid retention (edema) caused by a variety of causes, including congestive heart failure, severe liver disease (cirrhosis), kidney disease, or steroid or hormonal medication.

LJ-2698 is an adenosine A3 receptor antagonist under investigation for treating emphysema and DKD (Diabetic Kidney Disease). In mouse lung models, LJ-2698 effectively mitigates elastase-induced adverse effects and inhibits matrix metalloproteinase activity and apoptosis. Additionally, it is being explored for its potential in treating diabetic nephropathy, successfully preventing various types of kidney damage in mice.

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].

Camostat, also known as FOY 305, is a serine protease inhibitor. Camostat is used in the treatment of some forms of cancer and is also effective against some viral infections, as well as inhibiting fibrosis in liver or kidney disease or pancreatitis. It is an inhibitor of the enzyme transmembrane protease, serine 2 (TMPRSS2). Inhibition of TMPRSS2 partially blocked infection by SARS-CoV and Human coronavirus NL63 in HeLa cell cultures. In vitro study showed that camostat significantly reduces the infection of Calu-3 lung cells by SARS-CoV-2, the virus responsible for COVID-19.

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].

AChE BuChE-IN-6 (Compound 11f) is an inhibitor of AChE and BuChE, with IC50 values of 1.24 and 1.85 μg mL, respectively. It exhibits strong DPPH radical scavenging activity (IC50 = 3.15 μg mL). In vivo toxicity studies demonstrate that AChE BuChE-IN-6 is safe, showing no significant differences in blood and biochemical parameters compared to controls, and no abnormalities in liver and kidney tissues. This compound shows potential for Alzheimer's disease research.

GFB-12811 is an orally active, selective, and potent CDK5 inhibitor, used in the study of autosomal dominant polycystic kidney disease.

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).