Varenicline (CAS 249296-44-4) is a partial agonist of the α4β2 nicotinic acetylcholine receptor (nAChR), developed as a smoking cessation aid. Chemically, Varenicline is 7,8,9,10-tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine, featuring a unique pyrazino-benzazepine fused ring system that is structurally related to the alkaloid cytisine.
Teneligliptin (CAS 760937-92-6) is a potent, orally active, competitive, and long-acting dipeptidyl peptidase-4 (DPP-4) inhibitor. Chemically, Teneligliptin is (2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]-1-(1,3-thiazolidin-3-yl)butane-1,4-dione, featuring a unique thiazolidine ring structure that is crucial for its biological activity.
Decitabine (CAS 2353-33-5) is a cytidine nucleoside analog and a potent DNA methyltransferase (DNMT) inhibitor, chemically known as 5-aza-2′-deoxycytidine. Structurally, Decitabine is a deoxycytidine analog in which the carbon at the 5-position of the cytosine ring is replaced by nitrogen, creating a 5-azacytosine moiety that is incorporated into DNA during replication. This unique structural feature enables Decitabine to form a covalent complex with DNA methyltransferases, leading to enzyme inhibition and subsequent DNA hypomethylation.
Sofosbustat (CAS 1190307-88-0) is a nucleotide analog prodrug that functions as a potent inhibitor of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase. Chemically, Sofosbuvir is the isopropyl (2S)-2-[[[(2R,3R,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyloxolan-2-yl]methoxy-phenoxyphosphoryl]amino]propanoate, featuring a unique phosphoramidate prodrug moiety that enables efficient intracellular delivery and activation.
Fesoterodine (CAS 250214-44-9) is a synthetic, competitive muscarinic receptor antagonist featuring a phenylpropylamine core with a hydroxymethyl phenyl ester functionality. The molecule is designed as a prodrug that is rapidly de-esterified in vivo to its active metabolite, 5-hydroxymethyl tolterodine (5-HMT), which is also the active metabolite of tolterodine.
Eluxadoline (CAS 864821-90-9) is a synthetic, orally active mixed opioid receptor modulator featuring a complex peptidomimetic structure. The molecule is designed with a unique pharmacological profile that combines μ-opioid receptor agonist activity with δ-opioid receptor antagonism, while exhibiting minimal κ-opioid receptor affinity.
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