chronic kidney disease

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.

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.

M1001 is a HIF-2α agonist.

AZD9977 is a novel, selective modulator of mineralocorticoid receptor .

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.

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.

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].

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.

TRPC4/5-IN-2 (Compound 12) is an orally active transient receptor potential (TRPC5) inhibitor with an IC50 value of 81 nM. This compound exhibits good biosafety and low hepatic and renal toxicity, making it a promising candidate for the treatment of chronic kidney disease (CKD).

SC-919 (LI-2124) is an orally active and selective inhibitor that targets inositol hexakisphosphate kinases (IP6K, including the subtypes IP6K1, IP6K2, and IP6K3), with an IC50 value of 0.65 nM for IP6K3. By inhibiting IP6K, SC-919 reduces the production of inositol pyrophosphates (such as InsP₇), thereby inhibiting XPR1-mediated phosphate efflux from cells and increasing intracellular ATP levels. SC-919 shows potential for research in hyperphosphatemia associated with chronic kidney disease (CKD).

MPO-IN-9 is a specific myeloperoxidase (MPO) inhibitor with an IC50 value of 3.9 nM. It suppresses MPO-mediated ROS production and safeguards NO-dependent vascular functions by obstructing the chlorination and peroxidase cycles of MPO. MPO-IN-9 has potential applications in researching diseases such as chronic kidney disease and non-alcoholic steatohepatitis.

Bixalomer is a phosphate binder that alleviates hyperphosphatemia in rat models of chronic kidney disease (CKD). By binding phosphate in the small intestine, Bixalomer reduces phosphate absorption, thereby decreasing plasma phosphate levels in CKD rat models. It is applicable for research related to hyperphosphatemia.

H111-H7 is an inhibitor of the E3 ubiquitin ligase 27 containing the WW domain (WWP2), with a KD value of 717 nM. In a unilateral ischemia-reperfusion (UIR) mouse model, H111-H7 inhibits the expression of WWP2, restores the level of succinate dehydrogenase complex subunit C (SDHC), and slows the progression from acute kidney injury (AKI) to chronic kidney disease (CKD). H111-H7 is applicable for studying the transition from AKI to CKD.

XRF-1021 is an orally active HIPK2 inhibitor with an IC50 value of 0.18 μM. It reduces the expression of fibrosis markers such as fibronectin, type I collagen, and α-SMA in NRK-49F and HK-2 cells stimulated by TGF-β1. XRF-1021 blocks signaling pathways including TGF-β, NF-κB, p53, Wnt/β-catenin, and Notch. Additionally, it alleviates renal injury and fibrosis in vivo and can be utilized for research in chronic kidney disease.

H36-E4 is an inhibitor of the E3 ubiquitin ligase 27 containing WW domains (WWP2), with a KD value of 6.25 μM. In a unilateral renal ischemia-reperfusion (UIR) mouse model, H36-E4 suppresses WWP2 expression, restores levels of succinate dehydrogenase complex subunit C (SDHC), and slows the transition from acute kidney injury (AKI) to chronic kidney disease (CKD). This compound is useful for research on the progression of AKI to CKD.

PHD-IN-5 (ISM4808) is an orally active PHD inhibitor that can be used to study anemia associated with chronic kidney disease.