renal diseases

Temocapril is an inhibitor of tyrosine kinase.

Temocapril hydrochloride (CS-622 HCl), the hydrochloride of Temocapril, is a long-acting ACE inhibitor used for the therapy of hypertension.

Belzutifan (MK-6482, PT2977) is a small-molecule inhibitor and a HIF-2α inhibitor (IC50 = 9 nM) with high selectivity, oral activity, and improved pharmacokinetic characteristics, used for the treatment of clear cell renal cell carcinoma and related VHL diseases.

IPN60090 is a novel, potent, orally bioavailable, renal-type glutaminase (GLS1)-specific inhibitor with an IC50 value of 31 nM for GLS1. IPN60090 has potential anticancer and immunostimulant/immunomodulatory activity, selectively targets, binds, and inhibits human glutaminase, and can be used to study GLS1-mediated diseases.

Levocarnitine propionate hydrochloride (ST-261) is used for the treatment of the deterioration of renal function, congestive heart failure, intermittent claudication, and other diseases.

N-Acetyl-L-arginine (Ac-Arg-OH), an N-acyl-L-alpha-amino acid with a strong basic nature (based on its pKa), has elevated serum levels in hyperargininemic patients and is associated with several diseases, including uremia and colorectal cancer. In untreated hyperargininemic patients, it reaches its highest levels in cerebrospinal fluid. It has also been detected in apples and loquats, suggesting it could be a potential biomarker for consumption of these foods. Additionally, a low-arginine diet combined with sodium benzoate therapy leads to a marked decrease in plasma N-acetyl-L-arginine concentrations.

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.

Runcaciguat is a soluble guanylate cyclase stimulator. Runcaciguat combines with selective partial adenosine A1 receptor agonists and can be used in studies about cardiovascular and renal diseases.

DM-4111, one of the primary monohydroxy metabolites of Tolvaptan, is an effective vasopressin V2 receptor (vasopressin V2 receptor) inhibitor. By inhibiting water reabsorption in renal tubules, it facilitates the excretion of electrolyte-free water. DM-4111 holds potential for research in cardiovascular diseases.

MARY1 is a selective 5-HT2BR antagonist with an IC50 of 380 nM and a Ki of 764 nM [human 5-HT2BR]. It promotes mitochondrial biogenesis (MB) in the kidneys and enhances mitochondrial function by increasing mitochondrial respiration capacity, protein levels, and number in renal proximal tubular cells (RPTC). MARY1 induces MB in RPTCs through the 5-HT2BR and dual PI3K/AKT and RAS/MEK/ERK signaling pathways. It is useful for studying kidney diseases related to metabolic and mitochondrial dysfunction.

Diosuxentan is an inhibitor of ETA and is utilized in research pertaining to cardiovascular, renal, and neuronal inflammatory diseases.

Linvemastat (Compound FC-4) is an orally active MMP-12 inhibitor with an IC50 of less than 10 nM and demonstrates high selectivity over MMP-1, -2, -3, -7, -9, -10, and -14. It significantly reduces lung fibrosis in a mouse model of bleomycin-induced unilateral pulmonary fibrosis and effectively alleviates kidney damage, interstitial inflammation, or fibrosis in a unilateral ureteral obstruction renal fibrosis model. Linvemastat is suitable for research into inflammatory diseases such as idiopathic pulmonary fibrosis (IPF), inflammatory bowel disease (IBD), and asthma.

STING-IN-17 is an orally active inhibitor of STING (human STING IC50= 29 nM, murine STING IC50= 15 nM). It effectively suppresses the phosphorylation of STING, TBK1, and IRF3. The compound inhibits the expression of IP10, IFNB1, and ISG56 mRNA in a dose-dependent manner. Additionally, STING-IN-17 reduces ROS and inhibits the expression of cleaved-PARP/caspase-3. It shows potential for improving renal function and can be utilized in research on inflammatory diseases such as acute kidney injury.

AM-0883 is an agonist of TRPC6 (transient receptor potential canonical 6) with a human TRPC6 EC50 of 46 nM. It is applicable for research in cardiac and renal diseases.

GS-1291269 is a potent neutral ketohexokinase (KHK) inhibitor, exhibiting IC50 values of 0.38 nM for KHK-C and 2.1 nM for KHK-A. In a rat fructose challenge model, GS-1291269 effectively reduces fructose-1-phosphate (F1P) levels in the liver and kidneys. It is applicable in the study of renal diseases and metabolic dysfunction-associated steatotic liver disease (MASLD).

Enuvaptan is a vasopressin receptor antagonist and has the potential for research into renal and cardiovascular diseases.

PF-06761281 (Compound 4a) is a potent and partially selective sodium-coupled citrate transporter protein (NaCT/SLC13A5) inhibitor with IC50 values of 0.51, 13.2, and 14.1 µM for NaCT, NaDC, and NaDC, respectively, and has the advantage of being orally active, reducing hepatic and renal uptake of citrate and plasma glucose concentration for metabolic diseases.

SGC agonist 2 is a potent soluble guanylate cyclase (SGC) agonist with potential therapeutic applications for cardiovascular diseases (heart failure, angina, pulmonary hypertension, myocardial infarction) and fibrotic diseases (renal fibrosis, systemic sclerosis).

ADMA-D6 is intended for use as an internal standard for the quantification of NG,NG-dimethyl-L-arginine by GC- or LC-MS. ADMA (T7682) is an endogenous inhibitor of nitric oxide synthase (NOS). It is formed from arginine by protein arginine methyltransferases (PRMTs) and degraded by dimethylarginine dimethylaminohydrolases (DDAHs) and alanine-glyoxylate aminotransferase 2 (AGXT2). ADMA (T7682) levels are increased concomitant with an increase in blood pressure in Dahl salt-sensitive rats fed a high-salt diet. ADMA (T7682) levels are increased in the plasma in a variety of endothelial dysfunction-related diseases, including hypertension, congestive heart failure, and end-stage renal disease.

Ilacirnon sodium is a potent CCR2 antagonist that may be useful in the treatment of renal diseases including Focal Segmental Glomerulosclerosis and Diabetic Nephropathy.

Glutamate dehydrogenase NAD(P) (GLDH), a mitochondrial enzyme found in hepatocytes, renal tissue, brain, muscle, and intestinal cells, catalyzes the reversible oxidative deamination of glutamate to α-ketoglutarate (α-KG), playing a critical role in the urea cycle [1], and is frequently utilized in biochemical research.

Tabalumab (LY2127399) is a humanised monoclonal antibody targeting BAFF that neutralises both soluble and membrane-bound forms of BLyS and affects B-cell populations, and can be used for research into autoimmune diseases such as rheumatoid arthritis, kidney failure, and systemic lupus erythematosus.

Nurulimab (BCD-145) is an immune checkpoint inhibitor composed of a humanized monoclonal antibody and is also a CTLA-4 antagonist. By binding to CTLA-4, Nurulimab lifts the inhibitory brake on T-cell activation, enhances the function of effector T cells, and reduces the immunosuppressive activity of Tregs. In preclinical studies, the combination of nurulimab with the PD-1 inhibitor prolgolimab (BCD-100) produced synergistic antitumor effects. Nurulimab has demonstrated good tolerability and is suitable for use in studies of solid tumors such as melanoma, non-small cell lung cancer, and renal cell carcinoma. Nurulimab may also be used in studies of skin and musculoskeletal disorders.

TOL101 is a humanized antibody with αβ TCR specificity and acts as a non-depleting T-cell immunomodulator. TOL101 blocks T-cell activation signals by reversibly downregulating the CD3 complex on the surface of αβ T cells. TOL101 can be used to study organ transplant rejection and autoimmune diseases.