Métabolisme

1-(2,3-Dichlorophenyl)piperazine hydrochloride, with CAS No. 119532-26-2, is a fragment molecule that serves as an important scaffold for molecular linking, expansion, and modification. 1-(2,3-Dichlorophenyl)piperazine hydrochloride provides a structural basis and research tool for the design and screening of novel drug candidates, and is commonly used in drug discovery, drug synthesis, and related research.

NY-ESO-1 (157–165) peptide is a peptide derived from the NY-ESO-1 protein and has the ability to activate the immune system. It is particularly effective in individuals positive for HLA-A2, as it can be recognized by CD8+ T cells, thus triggering an immune response. The presence of NY-ESO-1 (157–165) peptide in various tumors makes it a potential target for cancer immunotherapy. This peptide is also utilized in research focusing on cancer immunotherapy.

PKM2 activator 7 (Compd B4) is a PKM2 activator with an AC50 value of 0.144 μM. It functions by inhibiting the growth of T cells, thereby alleviating DSS-induced colitis in mice.

WAY-639921 treats cardiovascular and respiratory conditions by inhibiting PDE1c.

Carbonic anhydrase inhibitor24 (Compound 11) is an inhibitor of human carbonic anhydrase. It exhibits Ki values of 10.7 nM and 7.5 nM against hCAs IX and XII, respectively.

CP-346086 dihydrate is a strong oral MTP inhibitor with 2.0 nM IC50, reducing cholesterol and triglycerides in vivo.

Sorafenib N-oxide, active sorafenib metabolite, inhibits FLT3-ITD (Kd=70 nM), targets AML, selectivity for FLT3-ITD+, also mixes CYP3A4 inhibitor (Ki=15 μM).

N-4′-(p-Trifluoromethylphenyl)butyl-DAB (compound 5g) acts as an agonist for lysosomal acid α-glucosidase (GAA).

All-trans-13,14-Dihydroretinol, a metabolite of all-trans-retinoic acid, is synthesized through the enzymatic action of retinol saturase on all-trans-retinoic acid.

Butafosfan, often with cyanocobalamin, boosts lipid metabolism in livestock to prevent/treat deficiencies and ketosis.

The synthetic compound me4 Peptide, designed from the microexon me4 sequence of the neuronal CPEB4 protein, can inhibit the aggregation of CPEB4 and is applicable in research on autism spectrum disorder-related conditions.

E-76 is a peptide with anticoagulant activity that inhibits blood coagulation by specifically binding to the exogenous coagulation factor VIIa (FVIIa). It is utilized in the study of blood coagulation-related diseases.

Naphthacene (Benz[b]anthracene) is a useful life science reagent for biochemical experiments and organic synthesis.

Cartilostatin 1, an anti-angiogenic peptide, has potential applications in research focused on angiogenesis inhibition [1].

G43 inhibits glucosyltransferase GtfB (Kd 3.7μM) and GtfC (Kd 46.9nM), and fights Streptococcus mutans in caries research.

hCAXII-IN-9 (Compound 3I) is a selective hCAXII inhibitor with Ki values of 28 nM for hCAXII, 7192.6 nM for hCAI, 188.6 nM for hCAII, and greater than 100000 nM for hCAIX. This compound may be utilized in anti-tumor research.

Lipoxygenase (LOX) is a dioxygenase that catalyzes the peroxidation of linoleic acid (LA) or arachidonic acid (AA) in the presence of molecular oxygen.

Thymoctonan, as a synthetic octapeptide thymic hormone, can repair immunodeficiency of mice cured of plasmacytoma by melphalan.

S-Phenylmercapturic acid is a metabolite of benzene that can be used as a biomarker to assess benzene exposure.

Vitamin B12a monohydrochloride (Hydroxocobalamin) is an essential water-soluble vitamin.a cyanide detoxifier and nutritional supplement, injection, inhalation.

N-Lactylleucine is an endogenous metabolite detectable in patients with intermediate maple syrup urine disease.

α-Glycosidase-IN-2 (compound 8b) is an inhibitor of α-glycosidase, displaying Ki values of 74.16 nM and 6.09 nM for aldose reductase and α-glycosidase, respectively. This compound is utilized in research related to diabetes.

sPLA2 inhibitor 3 (Compound 6c) functions as a potent α-glucosidase inhibitor (IC50= 0.0953 µM) and has potential applications in diabetes research.

Guanosine triphosphate tritris (GTP tritris) serves as a crucial enhancer in myocyte differentiation, playing an essential role in regulating miRNA-muscle regulatory factors. It promotes the release of exosomes rich in guanine and guanine-derived molecules, and is considered an activation precursor for RNA synthesis. In mitochondrial functionality, GTP is involved in the entry of proteins into the matrix, which is vital for various regulatory pathways. It initiates peptide synthesis by facilitating the binding of formylmethionine-tRNA to the ribosome, and aids in polypeptide chain elongation. Additionally, GTP acts as a carrier for phosphates and pyrophosphates, channeling chemical energy into specific biosynthetic pathways. It activates signal transduction G proteins, regulates cellular processes such as proliferation and differentiation, and its hydrolysis by small GTPases (including Ras and Rho) is indispensable for both proliferation and apoptosis. Furthermore, the small GTPase Rab assists in vesicle docking, fusion, and formation. Beyond signal transduction, GTP is also an energy-rich precursor in the biosynthesis of DNA and RNA enzymes.

α-Glucosidase-IN-75 (compound 13) is an inhibitor of α-glucosidase, exhibiting an IC50 value of 3.81 μM. It is employed in the study of cardiovascular diseases induced by high glucose levels.

Triletide is a thromboxane A2 antagonist agent.

N-Lactylvaline is an endogenous metabolite detectable in patients with intermediate maple syrup urine disease.

BuChE-IN-15, a chemical compound, exhibits potent inhibitory activity with IC50 values of 81 nM and 400 nM, respectively. It also demonstrates good blood-brain barrier permeability and neuroprotective properties, making it suitable for research in Alzheimer's disease.

AV22-149 (compound 22) is an inhibitor of Carbonic Anhydrase .

LQ-38 is an orally active, soluble epoxide hydrolase (sEH) inhibitor with an IC50 value of 5.2 nM. It has shown anti-inflammatory activity in rat foot edema models and in mouse models of acute pancreatitis, and exhibits analgesic effects in acetic acid-induced mouse writhing models.

Compound 6T, designated as Carbonic anhydrase inhibitor26, acts as an inhibitor of Carbonic Anhydrase II (Carbonic AnhydraseII), exhibiting an IC50 value of 9.10 ± 0.26 μM.

2-Deoxy-2-fluoro-L-fucose is a fucosylation inhibitor that inhibits the proliferation of human cancer, and inhibits root growth and cell elongation.

CAIX-IN-4 (Compound 8b) is a selective inhibitor of carbonic anhydrase IX (CAIX) with an IC50 value of 0.32 μM. It holds potential for research in cancer, such as renal cell carcinoma.

N-Acylated ethanolamines (NAEs) are bioactive lipids; AEA activates CB1/CB2 receptors; PEA, an anti-inflammatory, doesn't bind well to them.

Zuretinol is a oral retinoid.

Phospho-L-Arginine (lithium salt hydrate) is a L-arginine derivative suitable for biochemical experiments and drug synthesis research.

1-Benzyl-3-Phenylthiourea (1-Benzyl-3-Phenyl-2-Thiourea) can be used as a sensing material for the detection of nerve agents and related stimulants.

Bilirubin conjugate is a stable, water-soluble ditaurate derivative of bilirubin meant to mimic endogenous bilirubin glucuronide derivatives.

sPLA2 inhibitor 2 (compound 6a) is an sPLA2 inhibitor with an IC50 value of 0.0475 μM, making it valuable for diabetes research.

CK1δ-IN-6: potent, selective CK-1δ inhibitor, IC50 23 nM, neuroprotective, anti-inflammatory, for neurodegenerative research.

Desmethyl bosentan, bosentan's active metabolite, activates PXR in CV-1 cells at 25 μM.

CSNK2-IN-2 (compound 2) is an orally active inhibitor of CSNK2. It is utilized in antiviral research.

Ercalcidiol is a metabolite of vitamin D2 and can be used in monitoring vitamin D therapy.

Bam 12P acetate is the putative enkephalin precursor in bovine adrenal, pituitary, and hypothalamus.

CK2-IN-14 (Compound 10b) is an inhibitor of cyclin-dependent kinase 2α with an IC50 of 36.7 nM. It effectively hinders the growth of cancer cell lines 786-O and U937, with GI50 values of 7.3 μM and 7.5 μM, respectively.

Lofacimig is a bispecific antibody of VH-VH-G1(h-CH2-CH3) dimer type that targets FXI/PTA.

sEH-degrader-1 (Compound 8) acts as an effective inhibitor of sEH, exhibiting IC50 values of 3.8 nM for hsEH and 210 nM for msEH. Additionally, it proficiently degrades sEH in both mouse liver and brown adipose tissue.

TBCA: selective CK2 inhibitor, IC50=110 nM, Ki=77 nM, favors CK2 over CK1, DYRK1A, and 27 other kinases.

Casein kinase 1δ-IN-8 is an inhibitor of casein kinase 1δ and is used to treat neurodegenerative diseases such as Alzheimer's disease type.

Ledelabricin alfa, an isoform A variant of human proteoglycan 4 (PRG4), functions as a lubricant for joints and boundaries.