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An orally active, selective and potent Glucosylceramide synthase (GCS) inhibitor with central nervous system (CNS) access; exhibits significantly lower tissue levels of GL-3 and lyso-GL-3 and a delayed progression of a thermal nociceptive response in administered Fabry mice; shows favorable pharmacological properties and safety profile.
Sivelestat sodium tetrahydrate
A potent, specific and competitive inhibitor of human neutrophil elastase with IC50 of 44 nM; also inhibits leukocyte elastase obtained from rabbit, rat, hamster and mouse, do not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G (>10 uM); attenuates LPS-induced acute lung inflammation in the hamster.
An irreversible, membrane-permeable inhibitor of lysosomal and cytosolic cysteine proteases with the ability to inhibit calpain activity in intact platelets; reduces brain amyloid-β and improves memory deficits in Alzheimer's disease animal models by inhibiting cathepsin B.
Cortexolone 17 alpha-propionate (CB-03-01, Clascoterone) is a topical and peripherally selective androgen antagonist, displays a strong local antiandrogenic activity in hamster's flank organ test, does not exhibit antiandrogenic activity after subcutaneous injection in vivo.
KZR-616 (KZR616) is a potent, selective dual immunoproteasome subunit LMP7/LMP2 inhibitor with IC50 of 39 nM/139 nM, weakly inhibits β5, MECL-1 and no acitivty against β1 subunit; shows no inhibition at 10 uM against a broad selectivity panel of 20 serine, metallo-, cysteine and aspartyl proteases and 11 hydrolases; demonstrates efficacy in the anti-collagen antibody induced arthritis (CAIA) models.
Mosedipimod (EC-18, 1-palmitoyl-2-linoleoyl-3-acetylglycerol) is a synthetic monoacetyldiaglyceride that stimulates T cell production of IL-2, IL-4, IL-12, IFN-γ, and GM-CSF in vitro; attenuates the asthmatic response in an aluminum hydroxide/ovalbumin-induced model of asthma, inhibits hematogenous metastasis of KIGB-5 biliary cancer cell in hamster model.
Hetrombopag is a potent, selective, orally-active Thrombopoietin (TPO) receptor agonist; specifically stimulates proliferation and/or differentiation of human TPOR-expressing cells, including 32D-MPL and human hematopoietic stem cells, with low nanomolar EC50 values through stimulation of STAT, PI3K and ERK signalling pathways; specifically enhances the viability and promoted the growth of 32D-MPL cells in hollow fibres implanted in nude mice, exhibiting much higher potency than eltrombopag in vivo.
BPN14770 (BPN-14770) is an allosteric inhibitor of phosphodiesterase 4D (PDE4D) with IC50 of 7.8 and 7.4 nM for human PDE4D7 and PDE4D3 respectively, displays 16-fold less potent against monomeric form of PDE4D lacking the UCR1 dimerization domain (PDE4D2 IC50 = 127 nM); BPN14770 is 17-fold less potent against mouse PDE4D7 (IC50 = 133 nM), binds to a primate-specific, N-terminal region of PDE4D; elevates brain cAMP and facilitates hippocampal long-term potentiation (LTP) in wild-type and humanized PDE4D mice, improves cognitive performance, antagonized the amnesic effects of scopolamine and increased cAMP signaling in brain, and increased BDNF and markers of neuronal plasticity associated with memory.
LHF-535 (LHF535, LHF 535) is a small-molecule viral entry inhibitor that targets the arenavirus envelope glycoprotein, exhibits potent antiviral activity against a broad array of hemorrhagic fever arenaviruses with IC50 of 0.1-0.3 nM; LHF-535 has sub-nanomolar potency against the viral envelope glycoproteins from all Lassa virus lineages, with the exception of the glycoprotein from the LP strain from lineage I, which was 100-fold less sensitive than that of other strains; potently inhibited Jun¨ªn virus, but not Candid#1 in virus-yield reduction assays; protects mice in a lethal Tacaribe virus model at 10 mg/kg.
KBP-5074 (KBP5074) is a novel non-steroidal, highly selective mineralocorticoid receptor antagonist for the treatment of hypertensive chronic kidney disease.
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