chronic

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.

Moxifloxacin hydrochloride (BAY12-8039 HCl) is a fourth generation fluoroquinolone with expanded activity against gram-positive bacteria as well as atypical pathogens. Moxifloxacin has been linked to mild ALT elevations during therapy and to rare instances of idiosyncratic acute liver injury with symptoms and jaundice.

Pivanex (Pivalyloxymethyl butyrate) is an orally active HDAC inhibitor and an antimetastatic and antiangiogenic agent. Pivanex downregulates the Bcr-Abl protein and enhances apoptosis.

Camostat mesylate (FOY-S980) is a trypsin-like protease inhibitor and inhibits airway epithelial sodium channel (ENaC) function.

Cladribine (2CdA), an adenosine deaminase inhibitor, is utilized in the treatment of lymphoproliferative diseases.

Acalabrutinib (ACP-196), also known as ACP-196, is an orally available inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity. Upon administration, ACP-196 inhibits the activity of BTK and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents both B-cell activation and BTK-mediated activation of downstream survival pathways. This leads to an inhibition of the growth of malignant B cells that overexpress BTK. BTK, a member of the src-related BTK/Tec family of cytoplasmic tyrosine kinases, is overexpressed in B-cell malignancies; it plays an important role in B lymphocyte development, activation, signaling, proliferation and survival.

Ethyl linoleate is a natural product.

Promestriene (3-propyl ethyl) (INN) is a synthetic estrogen and glucocorticoid used topically in a 1% cream formulation. It is described as a tropic agent and antiseborrheic.

SR33805 is a potent antagonist of Ca2+ channel(EC50s of 4.1 nM and 33 nM in depolarized and polarized conditions, respectively)

IA-Alkyne (Iodoacetamide-alkyne) is a TRP channel (TRPC) agonist. IA-Alkyne can be used to develop an isotopically tagged probe for quantitative cysteine-reactivity profiling. It also has the potential for the study of respiratory infection.

Mizagliflozin is an orally active, selective SGLT1 inhibitor with a Ki value of 27 nM for human SGLT1. Mizagliflozin is 303 times more selective for SGLT1 than for SGLT2. Mizagliflozin is an anti-diabetic drug that can improve postprandial blood sugar fluctuations and may have the potential to improve chronic constipation.

NVR 3-778 is a first-in-class, orally bioavailable HBV CAM belonging to the SBA class, exhibiting anti-HBV activity.

Tyrphostin AG957, a tyrosine kinase inhibitor with anti-BCR/ABL tyrosine kinase activity restores beta1 integrin-mediated adhesion and inhibitory signaling in chronic myelogenous leukemia hematopoietic progenitors[1].

Arformoterol Tartrate ((R,R)-Formoterol tartrate) is the tartrate salt of arformoterol. Arformoterol is a long-acting beta-2 adrenergic agonist with bronchodilator activity[2].

T.cruzi-IN-1 (MDK1088) is a Trypanosoma cruzi inhibitor.

Talniflumate (Somalgen) is a calcium-activated chloride channel (hCLCA1/mCLCA3) blocker that reduces mucin synthesis and releases in animal models and cell culture. It possesses anti-inflammatory actions via inhibition of Cox (cyclooxygenase) and inhibits Cl-/HCO3- exchange activity. It also increases survival in a cystic fibrosis mouse model of the distal intestinal obstructive syndrome.

Cilomilast (SB-207499) is a potent PDE4 inhibitor with an IC50 of approximately 110 nM, demonstrating anti-inflammatory activity and minimal central nervous system effects. Phase 3.

Sevelamer carbonate is a non-absorbed phosphate binding crosslinked polymer, with the same polymeric structure as sevelamer hydrochloride, in which carbonate replaces chloride as the counterion.

Phytic acid dipotassium salt is an endogenous metabolite that inhibits β-secretase 1 (BACE1).

Aurintricarboxylic acid (NSC-4056) is a strong inhibitor of topoisomerases and other nucleases. It is a potent inhibitor of ribonuclease and topoisomerase II by preventing the binding of the nucleic acid to the enzyme.

Eliapixant (BAY 1817080) (BAY 1817080) is a potent and selective P2X3 receptor antagonist, with an IC50 of 8 nM. Eliapixant can be used for the research of refractory chronic cough.

(25S)-delta7-Dafachronic acid, an orphan nuclear receptor DAF-12 ligand, inhibits the dauer-promoting activity of DAF-12.

Doxorubicin hydrochloride is an anthracycline antibiotic with cytotoxic and antitumor activity. It is an effective inhibitor of human DNA topoisomerase I and II, with IC50 values of 0.8 μM and 2.67 μM, respectively. In addition to inhibiting DNA topoisomerases, it can reduce the phosphorylation of AMPK and its downstream target, acetyl-CoA carboxylase. Doxorubicin hydrochloride also induces apoptosis and autophagy. In animal studies, it is commonly used to induce models of acute renal failure, chronic kidney injury, and heart failure.

Candoxatril (UK 79300) is an orally active neutral peptide endonuclease (NEP, EC 3.4.24.11) inhibitor that improves exercise capacity in patients with chronic heart failure undergoing angiotensin-converting enzyme inhibition.