Metabolism

ICMT-IN-45 (compound 24) serves as an ICMT inhibitor, demonstrating an IC50 value of 0.132 μM [1].

Raloxifene Bismethyl Ether hydrochloride is a Raloxifene metabolite and an estrogen receptor inactive compound on which both hydroxyl groups are absent.

CMI-392 is a dual 5-lipoxygenase inhibitor and platelet-activating factor (PAF) receptor antagonist (IC50s: 100 and 10 nM).

CLB-016 is an inhibitor of hypoxia-inducible factor (HIF)-1.

hMAO-B-IN-32 is a potent hMAO-B selective inhibitor with an IC50 of 45.52 μM.

C18 ((±)-2'-hydroxy) Ceramide (d18:1/18:0) is a lipid molecule that can be used in life science related research. The CAS number of C18 ((±)-2'-hydroxy) Ceramide (d18:1/18:0) is 34249-41-7.

Leramistat is a mitochondrial complex I (NIC1) inhibitor that alters cellular metabolism and reduces proliferation in human primary lung fibroblasts.

Celgosivir (6 O-butanoyl castanospermine) is an inhibitor of α-glucosidase I. In vitro assay, it inhibits bovine viral diarrhoea virus (BVDV) ( IC50: 1.27 μM ).

LMPTP INHIBITOR 1 hydrochloride is a selective inhibitor of low molecular weight protein tyrosine phosphatase ( LMPTP ), with an IC 50 of 0.8 μM for LMPTP-A.

(R)-Azasetron besylate (SENS-401), an orally active calcineurin inhibitor, has been shown to mitigate cisplatin-induced hearing loss and cochlear damage [1][2].

GSK2973980A is a selective Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) inhibitor (IC50: 3 nM).

8-Hydroxyguanine, generated through the oxidative degradation of DNA by the hydroxyl radical, serves as an indicator of oxidative stress in biological systems.

SR11237 is a Pan retinoid X receptor (RXR) agonist.

AZD2716 is an effective selective phospholipase A2 inhibitor for the treatment of coronary artery and cardiovascular disease.

Casein kinase 1δ-IN-5 is a selective CK1δ inhibitor (IC50 47 nM) with neuroprotective activity, supporting neurodegeneration research.

Arbaprostil, a synthetic PGE analog, guards stomach lining, aids ulcer healing, and blocks pancreatic function and tumor growth.

Clocortolone pivalate, a synthetic steroid, treats dermatitis and psoriasis.

17(R)-Resolvin D1 (17(R)-RvD1) is an aspirin-triggered epimer of RvD1 that equivalently inhibits human polymorphonuclear leukocyte migration across the endothelium (EC50= ~30 nM), a precursor to acute inflammation. Unlike RvD1, it resists rapid degradation by eicosanoid oxidoreductases. In a mouse peritonitis model, 17(R)-RvD1 dose-dependently reduces leukocyte infiltration, achieving up to a 35% decrease with a 100 ng dose. Additionally, its methyl ester derivative, designed to enhance its pharmacokinetic and distribution properties as a more lipophilic prodrug, can be converted back into the active acid form by intracellular esterases.

3-Bromotyrosine, a product of protein oxidation, is generated after eosinophil activation during allergic responses. It serves as a biomarker for eosinophil peroxidase-induced protein oxidation both in vitro and in vivo. Beyond its association with eosinophils, 3-bromotyrosine levels are significantly elevated in peritoneal exudate from K. pneumoniae-infected mice, indicating a fivefold increase compared to uninfected controls, which implies that neutrophils may release increased levels of oxidized products during inflammation. Furthermore, in humans, allergen-challenged lung samples from patients with allergen-induced asthma show a tenfold increase in 3-bromotyrosine, highlighting its potential as a marker for oxidative stress in allergic conditions.

Chenodeoxycholic acid 24-acyl-β-D-glucuronide (CDCA-24G), a metabolite of CDCA, is synthesized from CDCA via the action of the UDP-glucuronosyltransferase (UG UT) isoform UGT1A3.