liver injury

Perphenazine (Trilafon) is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties.

Pioglitazone (U 72107) is a PPARγ agonist with EC50 of 0.93 and 0.99 μM on human and mouse PPARγ, respectively, and has selective and oral activity. Pioglitazone can be used in diabetes research.

SEW 2871 is an orally available, highly selective S1P1 agonist with an EC50 of 13.8 nM.It reduces the number of lymphocytes in the blood and is used in studies related to diabetes, Alzheimer's disease, liver fibrosis, and inflammation. It activates ERK, Akt and Rac signaling pathways and induces S1P1 internalization and recycling.

Tamoxifen is an orally active selective estrogen receptor modulator (SERM) that acts as an estrogen antagonist in breast cells and an agonist in bone, liver, and uterine cells. It can be used to induce gene knockout and liver injury models in mice, and also exhibits multiple biological activities, including activation of Hsp90, induction of autophagy and apoptosis, and inhibition of EBOV and MARV viral infections.

KD-3010 (Kalypsys) is an orally active potent and selective PPARδ agonist for the study of liver injury.

mPGES-1 Inhibitor-1 is a novel selective inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1) with anti-inflammatory and analgesic activity for the study of acute liver injury.

Ono-3307 mesylate is a protease inhibitor with inhibitory effects on a variety of proteases.Ono-3307 mesylate has significant protective effects against liver injury in rats and inhibits the deposition of radiofibrillar proteins in the kidneys and lungs.PF-184298 is a protease inhibitor with potential antioxidant effects in plasma and adipose tissue.PF-184298 can be used in the study of pancreatitis.

FK-330 (FR-260330) is a novel orally active inducible nitric oxide synthase inhibitor with potential anticancer and antitumor activity that prevents ischemia and reperfusion injury in rat liver transplantation.

SY-640 is an Acetamide derivative. SY-640 exhibits potent hepatoprotective effect. SY-640 reduces liver injury in mice induced by Propionibacterium acnes and Lipopolysaccharide.

FK-330 dihydrate (FR-260330 dihydrate) is a novel and effective nitric oxide synthase inhibitor. It can prevent ischemia and reperfusion injury in rat liver transplantation.

Clk1-in-3 is a + selective and highly potent sexual Clk1 inhibitor with an IC50 of 5 nM and 300 pairs higher affinity than Dyrk1A. CLK1-IN-3 also showed highly effective inhibition of Clk2 and Clk4, with IC50 values of 42 and 108 nM, respectively. CLK1-IN-3 is effective in inducing autophagy in vitro and can be used for prevention and human treatment of acute liver injury (ALI).

Lapatinib ditosylate (Lapatinib tosilate) monohydrate is a tyrosine kinase receptor inhibitor used in the therapy of advanced breast cancer and other solid tumors. Lapatinib ditosylate monohydrate therapy is associated with transient elevations in serum aminotransferase levels and rare instances of clinically apparent acute liver injury.

Entecavir (SQ34676) is a guanosine nucleoside analogue used in the treatment of chronic hepatitis B virus (HBV) infection. Entecavir therapy can be associated with flares of the underlying hepatitis B during or after therapy, but has not been linked to cases of clinically apparent liver injury.

Mirtazapine (6-Azamianserin) is a tetracyclic antidepressant with a somewhat unique mechanism of action. Mirtazapine therapy can be associated with transient asymptomatic elevations in serum aminotransferase levels and has been linked to rare instances of clinically apparent acute liver injury.

Benazepril hydrochloride (CGS 14824A HCl) is an angiotensin-converting enzyme (ACE) inhibitor widely used in the therapy of hypertension. Benazepril hydrochloride is associated with a low rate of transient serum aminotransferase elevations and has been linked to rare instances of acute liver injury.

Pemetrexed disodium (LY-231514) is a parenterally administered folate antagonist and antineoplastic agent, used in the treatment of non-small cell lung cancer and malignant mesothelioma. Pemetrexed disodium therapy has been associated with moderate rates of serum enzyme elevations during therapy, but has not been convincingly linked to instances of acute, clinically apparent liver injury.

Meropenem (SM 7338) is a broad-spectrum carbapenem antibiotic administered intravenously for severe bacterial infections caused by sensitive agents. It commonly causes mild, transient aminotransferase elevations and can rarely lead to clinically apparent cholestatic liver injury.

Betaxolol hydrochloride (SL 75212 HCl) is a cardioselective beta-blocker used in the treatment of hypertension.Betaxolol hydrochloride has not been linked to instances of clinically apparent drug induced liver injury.

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.

Quinapril hydrochloride (PD-109452-2) is an angiotensin-converting enzyme (ACE) inhibitor used in the therapy of hypertension and congestive heart failure. Quinapril hydrochloride is associated with a low rate of transient serum aminotransferase elevations, but has yet to be linked to instances of acute liver injury.

Tamoxifen Citrate is an orally active selective estrogen receptor modulator (SERM) that blocks estrogen activity in breast cells while activating estrogen signaling in cells such as those of the bone, liver, and uterus. As an Hsp90 activator, it enhances the ATPase activity of the Hsp90 chaperone complex, induces autophagy and apoptosis, and can be used to generate gene knockout models in CreER(T2) transgenic mice as well as liver injury models.

Docusate sodium (Aerosol OT) is an orally available, over-the-counter laxative and stool softener used to treat or prevent constipation. Docusate has not been linked to serum enzyme elevations during therapy or to clinically apparent liver injury with jaundice.

Repaglinide (AG-EE 623ZW) is a benzoic acid derivative that stimulates insulin secretion from the pancreas and is used in the therapy of type 2 diabetes. Repaglinide has been linked to rare instances of clinically apparent acute liver injury.

Milnacipran hydrochloride (Savella) is a serotonin and norepinephrine reuptake inhibitor used to treat major depressive disorders. Milnacipran hydrochloride is an enantiomer of milnacipran, which is used to treat fibromyalgia. Milnacipran hydrochloride and milnacipran have been associated with a low rate of transient elevations in serum aminotransferase levels during treatment and with rare instances of clinically apparent acute liver injury with jaundice.