Metabolism

Fidexaban (CI1031) is a novel, potent, selective and orally active factor Xa inhibitor that has demonstrated antithrombotic activity in a variety of assays

Tofimilast (CP-325366), a PDE4 inhibitor, is used potentially for the treatment of asthma and chronic obstructive pulmonary disease.

Mopidamol (RA 233) is a phosphodiesterase inhibitor, a dipyridamole derivative, with anticancer activity that prevents retinal vascular defects in experimental

BPDA2 selectively inhibits SHP2 (IC50=92nM) over SHP1/1B (33.39/40.71μM), curbs RTKs, and hampers SHP2-driven breast cancer cell traits.

Ulodesine (BCX4208), a PNP inhibitor, has an IC50 of 2.293 nM/L, potentially useful for hyperuricaemia research.

PKUMDL-LC-101-D04 enhances GPX4, curbs iron death, boosts enzyme activity 150% at 20 μM, effective in wild-type MEF, reduces lipid peroxide toxicity.

VU0155069, a selective PLD1 inhibitor (IC50: 46 nM), halts cancer cell migration in transwell assays.

MLS000544460 is a highly selective and reversible Eya2 phosphatase inhibitor (Kd: 2.0 μM, IC50: 4 μM).MLS000544460 exhibits inhibitory effects on Eya2

Cronidipine (LF 20254), a calcium channel antagonist, is used potentially for the treatment of hypertension and myocardia ischemia.

UK-50001 is a PDE4 inhibitor for treating inflammation, allergies, respiratory issues, and wounds.

Clozic (ICI 55897) exhibits reversible anti-proliferative effects and can be used in studies about serving as a potential anti-arthritic agent.

Chloramphenicol succinate is a bacteriostatic antibiotic. CPSA is a competitive substrate and inhibitor of succinate dehydrogenase (SDH),can be oxidized by.

alphaSYN-IN-NAB2: a NAB2 gene protein guarding neurons against alpha-SYN harm; aids endosomal transport, cell processes, and can study various diseases.

BMS-823778 is a potent inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) for the study of type 2 diabetes.

Aleplasinin (PAZ 417) is a selective and orally active inhibitor of Plasminogen activator inhibitor-1(PAI-1) and a key negative regulator of the fibrinolytic

Azacosterol (Diazasterol) is a DHCR24 inhibitor.Azacosterol undergoes a series of reactions in cortical neurons following oral or intraperitoneal administration

AGN 196996: strong RARα inhibitor (Ki: 2 nM), weak for RARβ/γ (Ki: 1087/8523 nM).

Xanthine oxidoreductase-IN-3, an oral XOR inhibitor with IC50 of 26.3 nM, is useful for acute hyperuricemia research.

NG-497, a selective inhibitor of human ATGL, blocks lipolysis in adipocytes and aids cancer research.

SBI-425: orally available TNAP inhibitor, enhances cardiovascular health & survival, no bone impact.

Orellanine, from Cortinarius orellanus, is nephrotoxic and hinders macromolecule synthesis in kidney cells and liver mitochondria.

PDE4B-IN-2 (A 33), an oral PDE4B inhibitor, IC50: 15 nM; less potent on PDE4D (IC50: 1.7 µM), has anti-inflammatory properties.

AZ3976 is an inhibitor of PAI-1 with an IC50 of 16 μM in a plasma clot lysis assay. AZ3976 displays profibrinolytic activities.

ALDH1A3-IN-2 is a potent ALDH1A3 inhibitor with an IC50 of 0.30 μM.ALDH1A3-IN-2 has potential for cancer disease research.

5-ALA benzyl ester hydrochloride: a photodetection agent that promotes PPIX in colon cancer cells.

Carbazeran (UK-31,557) is an inhibitor of PDE2 and PDE3 and can be used for studies about metabolic diseases.

Salnacedin (G-201) treats immune, skin, and musculoskeletal issues, suitable for acne, dermatitis, and psoriasis research.

Lonapalene is a topically effective inhibitor of 5-lipoxygenase.

CYP1B1-IN-4: 2,4-diarylthiazole, selective CYP1B1 inhibitor (IC50=0.2 nM), low cytotoxicity, stable in liver microsomes.

Allopurinol riboside, an allopurinol metabolite, inhibits purine nucleoside phosphorylase in parasites with a Ki of 277 μM.

Nanterinone: oral phosphodiesterase inhibitor, improves acute heart failure hemodynamics.

PF-04447943, a selective PDE9A inhibitor (IC50=12nM), may aid sickle cell anemia research with its anti-inflammatory properties.

Dasantafil (SCH446132) is a small molecule phosphodiesterase-5A (PDE5A) inhibitor used to treat genitourinary disorders and study erectile dysfunction.

Phosphatase-IN-1 is a phosphatidic acid phosphatase (Pah) inhibitor with antifungal activity for the study of rice blast and ruderalia.

AZD-0284 is an inverse agonist of the nuclear receptor RORγ. In development for the treatment of plaque psoriasis vulgaris and respiratory tract disorders[1].

Ladostigil is an oral cholinesterase & MAO-B inhibitor used for depression and Alzheimer's studies.

BMS641 (BMS-209641) is a RARβ agonist with affinity for RARβ that synergistically activates RARβ and RARgamma to induce cell maturation.

5(R)-HETE, a chemotactic for neutrophils, is a potent rare arachidonic acid derivative confirmed in S. solidissima oocytes.

IDH889: Brain-penetrant, mutant-specific IDH1 inhibitor; selective for IDH1 R132* mutations. IC50: 0.02μM (R132H), 0.072μM (R132C), 1.38μM (wild-type).

FXIa-IN-1 is a potent β-lactam covalent heparin-derived factor XIa (fXIa) inhibitor.

Cholesterol 24-hydroxylase-IN-2 is a potent inhibitor of cholesterol 24-hydroxylase (CH24H or CYP46A1), exhibiting an IC50 value of 5.4 nM, and has potential

IA1-8H2, a non-covalent, non-competitive inhibitor of PHPT1 with an IC50 of 3.4 μM, is utilized in the study of lung cancer, hepatocarcinoma, and renal cancer [

N-didesmethyl Loperamide, an active metabolite of the peripheral μ1-opioid receptor agonist loperamide, impedes electrically induced contractions in isolated

γ-CEHC, a metabolite of γ-tocopherol, is predominantly excreted through urine, primarily in its conjugated form as glucuronide [1], rather than through bile.

3-Hydroxy Medetomidine, a metabolite of the α2-adrenergic receptor agonist Medetomidine, is actively involved in the biochemical pathways following the administration of Medetomidine.

TP-1454 is an activator against PKM2 with a biochemically determined AC50 of 10 Nm. It can regulate tumor immune responses by acting on T regulatory cells.

1,2-Dipalmitoleoyl-3-oleoyl-rac-glycerol, a triacylglycerol, features palmitoleic acid at the \(sn-1\) and \(sn-2\) positions, and oleic acid at the \(sn-3\) position. It is present in the fat body of bumblebees.

GSK1842799, a selective S1P1 agonist for MS, shows >1000x selectivity over S1P3 & good oral bioavailability.

ICMT-IN-39, also known as compound 18, functions as an inhibitor of ICMT with an IC50 value of 0.031 µM [1].

Cyclophellitol aziridine, an analogue of cyclophenol, serves as a potent inhibitor of β-glucosidase [1].

Pentadecanoyl ethanolamide, a derivative of the endogenous lipid amides (N-acylethanolamines), demonstrates anticonvulsant efficacy in electroshock-induced seizures in mice, exhibiting minimal toxicity [1].

GLX481304 is a selective Nox-2 and Nox-4 inhibitor, exhibiting IC50 values of 1.25 μM.

S-(N-Methylsulfinylbutylthiocarbamoyl)-L-cysteine (SFN-Cys) is an isothiocyanate derivative, functioning as an active metabolite of sulforaphane, a class I and

ICMT-IN-27, also known as compound 64, is an inhibitor of the enzyme ICMT, demonstrating potent activity with an IC50 value of 0.1 µM [1].

ICMT-IN-28 (compound 65) serves as an inhibitor of ICMT, exhibiting significant potency with an IC50 value of 0.008 μM [1].

N-Acyl taurines, such as N-lignoceroyl taurine, alongside various arachidonoyl amino acid conjugates like N-arachidonoyl dopamine and N-arachidonoyl-L-serine, have been identified in bovine brain and through mass spectrometry lipidomic studies in the brain and spinal cord of both wild-type and FAAH knockout mice. Notably, N-lignoceroyl taurine levels were found to be 23-26 times higher in FAAH knockout mice than in wild types, suggesting its degradation by FAAH, despite in vitro evidence showing FAAH hydrolyzes N-lignoceroyl taurine significantly slower than oleoyl ethanolamide. Additionally, N-acyl taurines with polyunsaturated acyl chains are known to activate TRPV1 and TRPV4 channels within the transient receptor potential (TRP) family of calcium channels.

1,2-Dinonadecanoyl-sn-glycero-3-PC (DNPC), a saturated phospholipid, serves as a standard in quantifying phosphatidylcholines in human synovial fluid and has been utilized in researching lipid bilayer phase transition dynamics.

Hydroxy lenalidomide, a metabolite of the thalidomide analog and anticancer agent lenalidomide, is a derivative substance involved in the metabolic process of its parent compound.

19(R)-hydroxy PGF2α, an ω-1 hydroxylase metabolite of PGF2α present in human semen, exhibits a concentration of approximately 20 µg/ml for both 19(R)-hydroxy PG compounds (F2α and F1α) in fresh samples. This compound demonstrates no activity at the FP receptor of the cat iris sphincter muscle at concentrations up to 1 µM.

GSK321 is an IDH1 inhibitor that prevents cytoplasmic glutamine reductive carboxylation.GSK321 is used in the study of leukemia.

OSMI-1: cell-permeable OGT inhibitor, blocks O-GlcNAcylation (IC50: 2.7 μM), no effect on other cell glycans.

Compound 144 (also known as Anticancer Agent 144) is a potent inhibitor of both PTPN2 and PTP1B, exhibiting IC50 values of less than 2.5 nM, making it suitable

Compound 1e, also known as ALP/Carbonic anhydrase-IN-1, is a dual inhibitor targeting both carbonic anhydrase (CA) isozymes II, IX, and XII, as well as alkaline

"9322-O16B, an ionizable cationic lipid, facilitates the generation of lipid nanoparticles (LNPs) [1]."

DSTAP chloride (CDESA), a cationic lipid, is utilized in the formation of lipid nanoparticles (LNPs) and exhibits high transfection efficiency [1].

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