Métabolisme

IDX375 is a non-nucleoside inhibitor that selectively targets the HCV NS5B enzyme. It shows promising selectivity for genotypes 1a and 1b. The structure and binding sites of IDX375 have been confirmed through X-ray co-crystallization studies.

<p>PNPLA3 Modifier 1 (Compound 10), a modifier of patatin-like phospholipase domain-containing protein 3 (pnpla3), exhibits a geometric mean EC50 of 4.9 nM.</p>

Docosapentaenoic acid (22n-3) sodium is a component of phospholipids. It exhibits inhibitory activity against α-amylase and α-glucosidase, with IC50 values of 17 μg/mL and 22 μg/mL, respectively. Additionally, Docosapentaenoic acid 22n-3 sodium enhances cell viability and has mild anti-inflammatory effects.

BRD7539B: PfDHODH inhibitor, IC50 0.033μM; selective vs HsDHODH, IC50 >50μM.

Ketomethylenebestatin, a weaker carba-analog of aminopeptidase inhibitor bestatin, is 10x less potent.

<p>Dopaminechrome (DACHR) is an oxidation product of dopamine that promotes the generation of H2O2 at mitochondrial complex I in the brain in a concentration- and respiration-dependent manner. It possesses neurotoxic properties and can be utilized in Parkinson's disease research.</p>

<p>Lipid 11 (Compound Lipid 1) is a cationic lipid designed for nucleic acid delivery. It forms lipid nanoparticles (LNPs) through electrostatic interactions with nucleic acids, such as ceDNA. By using its cationic amine groups, Lipid 11 complexes with negatively charged nucleic acids, enabling cellular uptake and release of the nucleic acid cargo. Lipid 11 shows potential for use in the development of gene therapy drug delivery systems.</p>

<p>ROR1-IN-1 (Compound 19h) is an inhibitor of receptor tyrosine kinase-like orphan receptor 1 (ROR1) with a Ki of 0.10 μM. It inhibits the proliferation of cancer cell lines H1975, A549, and MDA-MB-231, with IC50 values of 0.36 μM, 1.37 μM, and 0.47 μM, respectively. In mice, ROR1-IN-1 demonstrates antitumor efficacy and exhibits favorable pharmacokinetic properties in a rat model.</p>

FABP1-IN-1 (44) is a selective FABP1 inhibitor with an IC50 value of 4.46 μM. It is applicable in research related to alcoholic fatty liver disease.

<p>The PKR Inhibitor, negative control, is an inactive structural analog of RNA-dependent protein kinase (PKR) inhibitors, serving as a negative control. Additionally, it can inhibit LK-induced neuronal death, demonstrating significant neuroprotective properties.</p>

<p>Carbonic anhydrase inhibitor 17 (compound 7c) is a pyrazine-based sulfonamide that acts as a carbonic anhydrase II inhibitor, with an IC50 value of 0.63 nM.</p>

<p>CIT-ALD is an aldehyde intermediate formed during the metabolism of Citalopram. It has potential applications in the research of neurological disorders.</p>

9(S)-HEPE is a monohydroxy fatty acid derived from EPA. The biological activity of 9(S)-HEPE has not been documented.

Lumirubin is a water-soluble photoproduct of bilirubin formed in vivo during phototherapy.

<p>DC360 is a synthetic analog of all-trans retinoic acid (ATRA) that can induce the expression of RARβ. It is useful for studies characterizing the retinoic acid signaling pathway.</p>

<p>α-Amylase/α-Glucosidase-IN-7 (Compound 3f) serves as a competitive inhibitor for the enzymes α-glucosidase and α-amylase, exhibiting IC50 values of 18.52 µM and 20.25 µM, respectively. Additionally, it effectively inhibits AChE and BChE, with IC50 values of 9.25 µM and 10.06 µM, respectively. This compound is useful in research related to diabetes and Alzheimer's [1].</p>

<p>LXRα agonist 1 (Compound 40) is a selective activator of LXRα, with an EC50 of 42 nM, and also demonstrates some activation effects on LXRβ, with an EC50 of 266 nM. It promotes target gene transcription by stabilizing the ligand-binding domain (LBD) of LXRα. When combined with the Raf inhibitor Sorafenib, LXRα agonist 1 shows significant antitumor activity in liver cancer cells. This compound is applicable in research focused on lipotoxicity-related cancers.</p>

<p>Quinapril is an orally active, non-peptide, and non-thiol angiotensin-converting enzyme (ACE) inhibitor. It primarily blocks the conversion of angiotensin I to angiotensin II in both plasma and tissues. Upon enzymatic hydrolysis, Quinapril is converted into the pharmacologically active Quinaprilat and is effective in hypertension models.</p>

<p>Bestatin methyl ester (600, 900 µM; 24 h) inhibits spore cell differentiation in Dictyostelium discoideum.</p>

<p>CGS-24592 is an orally active, selective, and potent inhibitor of neutral endopeptidase 24.11 (NEP), with an IC50 value of 1.6 nmol/L. It reduces the degradation of atrial natriuretic peptide (ANP), thereby increasing plasma ANP concentration and lowering blood pressure. CGS-24592 shows potential for research in cardiovascular diseases such as hypertension and congestive heart failure.</p>

<p>LTA4H-IN-2 (compound (S)-2) acts as an orally active inhibitor targeting Leukotriene A4 Hydrolase, exhibiting potent activity with an IC 50 of less than 3 nM [1].</p>

PDE4-IN-6: Potent PDE4 inhibitor, IC50 - 0.125μM (B), 0.43μM (D), anti-inflammatory, for arthritis research.

<p>EC33, a selective aminopeptidase A (APA) inhibitor, blocks the pressor response of exogenous Ang II and does not cross the blood-brain barrier, making it a potential candidate for salt-dependent hypertension research [1].</p>

<p>Glucosylceramide Synthase-IN-4 (compound 12) serves as a potent inhibitor of glucosylceramide synthase (GCS), exhibiting an IC50 of 6.8 nM. It demonstrates superior pharmacokinetic properties and robust stability in human hepatocytes. Additionally, this compound is noted for its effective CNS penetration and acceptable PXR selectivity [1].</p>

Nampt activator-4, a positive allosteric modulator (N-PAM) of nicotinamide phosphoribosyltransferase (NAMPT), has an EC50 of 0.058 μM and can enhance nicotinamide adenine dinucleotide (NAD+) levels in cells [1].

<p>α-Glucosidase-IN-63 (Compound 4d) serves as an α-Glucosidase inhibitor with an IC 50 value of 0.44 μM. Additionally, it exhibits inhibitory activity against hCA II, demonstrating a K i of 7.0 nM. The compound is also effective when administered orally. [1]</p>

<p>ABCB1-IN-4 (Compound C6z) is an orally active inhibitor of α-amylase and α-glucosidase, with IC50 values of 1.63 μM and 0.14 μM, respectively. It holds potential for diabetes research.</p>

<p>CK1δ-IN-3 (compound 376) is a CK1δ (casein kinase 1δ) inhibitor that can be used to study neurodegenerative diseases such as Alzheimer's disease.</p>

<p>8-Hydroxychlorpromazine is a metabolite of Chlorpromazine that can enhance the hyperglycemic response following glucose loading, suggesting a possible synergistic role in Chlorpromazine-induced glucose metabolism disorders. It holds potential for research into metabolic diseases.</p>

<p>AXKO-0046 is an indole derivative and small-molecule LDHB selective inhibitor.</p>

<p>Lp(a)-IN-5 (Compound A) is an orally active inhibitor of lipoprotein (a) [Lp(a)]. It effectively inhibits the assembly of Apo(a) and ApoB proteins, with an IC50 value of 0.41 nM. Lp(a)-IN-5 shows potential for research into diseases associated with elevated plasma Lp(a) levels, such as cardiovascular diseases.</p>

<p>BI-4916 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor that inhibits SSP and reduces cancer cell migration.</p>

<p>TMX-4113 has potential to be used in cancer that is a phosphodiesterase 6D(PDE6D) and casein kinase 1α(CK1α) degrader [1].</p>

<p>IRX5010 (IRX4647F), an analogue of IRX4647, serves as a highly selective RARγ nuclear receptor agonist. It effectively inhibits the growth of EMT-6 triple-negative breast cancer.</p>

<p>CK1δ-IN-7 (Compound 488) is an inhibitor of casein kinase 1δ (CK1δ).</p>

<p>DDO-3055 is an orally active PHD2 inhibitor utilized in studies related to anemia associated with chronic kidney disease.</p>

<p>WAY-606344 (Compound 97) is an inhibitor of Casein kinase 1δ and shows potential for Alzheimer's disease research.</p>

HSD17B13-IN-17 (compound 9) serves as a potent inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13). It demonstrates inhibitory efficacy with IC50 values of ＜0.1 μM for estradiol and ＜1 μM for Leukotriene B3 as substrates. This compound is significant in the management of nonalcoholic fatty liver diseases (NAFLDs), including nonalcoholic steatohepatitis (NASH) [1].

MAO-B-IN-17 is a selective and potent monoamine oxidase B (MAO-B) inhibitor (IC50: 5.08 μM) for the study of central nervous system disorders like Parkinson's.

JX237 is an SLC6A19 inhibitor, a transporter protein that neutralizes amino acid uptake by the liver, and can be used in the study of cardiovascular disease.

<p>Obicetrapib (AMG-899) is an inhibitor of cholesteryl ester transfer protein.</p>

FABPs ligand 6 (MF6) is an inhibitor of FABP5 and FABP7.

Lapaquistat acetate (TAK-475) is a squalene synthase inhibitor that reduces the cytotoxicity induced by statins in human skeletal muscle cells.

<p>Aleglitazar (R1439) (R1439) is a potent dual PPARα/γ agonist, with IC50s of 38 nM and 19 nM for human PPARa and PPARγ, respectively.</p>

Moiramide B is an acetyl coenzyme A carboxylase inhibitor with antimicrobial activity, strongly inhibiting Gram-positive bacteria.

<p>Glycosyltransferase-IN-1 is a glycosyltransferase inhibitor with bacteriostatic activity, inhibiting MSSA, MRSA, Bacillus subtilis, and Enterobacteriaceae.</p>

<p>WAY-213613 hydrochloride: potent, selective GLT-1/EAAT2 inhibitor (IC50 85 nM); weaker for EAAT1/3; inactive at glutamate receptors; research tool for CNS.</p>

<p>Etamicastat hydrochloride (BIA 5-453 hydrochloride) is a peripherally selective dopamine beta-hydroxylase inhibitor that reduces hypertension.</p>

DRB18 inhibits GLUT proteins, altering glucose metabolism and inducing cancer cell death by G1/S arrest and oxidative stress.

<p>STK-15 is a candidate for use as a fatty acid binding protein 5 (FABP5) inhibitor.</p>

<p>CP-642931 (Sorbitol dehydrogenase-IN-1) is a sorbitol dehydrogenase inhibitor used in the study of diabetes mellitus and cardiovascular disease.</p>

JNJ-6204 is a deuterated compound that efficiently inhibits CSNK1D and CSNK1E.

<p>BE1218 is a liver X receptor (LXR) inverse agonist active on LXRα and LXRβ with an IC50 of 9 nM and 7 nM, respectively.</p>

BMS453 (BMS-189453), a synthetic retinoid, is a potent and selective agonist of RARβ and a potent testicular toxin.

PREP inhibitor-1 is a prolyl oligopeptidase (PREP) inhibitor for the study of Alzheimer's disease.

<p>Dual FAAH/sEH-IN-1 inhibits both sEH (IC50: 9.6 nM) and FAAH (IC50: 7 nM), offering potent anti-inflammatory effects.</p>

ALOX15-IN-2: Potent ALOX15 inhibitor. IC50: 1.55 μM for LA; 2.79 μM for AA. Stops linoleic/arachidonic acid oxidation.

(S)-GNE-140 is the less active enantiomer of GNE-140.

TC-F 2 is a FAAH inhibitor.

6-Hydroxybentazon is a phase I metabolite of bentazon, a herbicide.

<p>GNE-140 is a potent inhibitor of lactate dehydrogenase A (LDHA). GNE-140 is a racemate mixture of (R)-GNE-140 and (S)-GNE-140.</p>

MK-0941 is an orally active and allosteric glucokinase activator, has potential in the treatment of type 2 diabetes.

SMND-309, a metabolite of salvianolic acid B, exhibits neuroprotective effects in cultured neurons and in rats subjected to permanent middle cerebral artery occlusion.

PF-06747711 is an effective and selective retinoic acid receptor-related orphan C2 inverse agonist (IC50: 4.1 nM). PF-06747711 also has anti-skin inflammatory activity.

β-Apo-13-carotenone is a naturally occurring β-apocarotenoid, and is a RXRα antagonist.

<p>8-Dehydrocholesterol is a compound whose elevated concentration is a diagnostic biochemical hallmark of classical Smith-Lemli-Opitz syndrome.</p>

4-Hydroxyacetophenone oxime is an impurity of Acetaminophen (Paracetamol), a potent COX-2 and hepatic NAT2 inhibitor used as an antipyretic and analgesic drug.

N3PT is a potent and selective inhibitor of transketolase(TK) with IC50 of 22 nM for Apo-TK)

Modecainide is metabolite of Encainide, is an antiarrhythmic agent.

PS10 is a broad-spectrum PDK inhibitor that inhibits PDK2 and significantly increases the activity of the pyruvate dehydrogenase complex.

Calcitriol Impurities A refers to the contaminants found in Calcitriol, the hormonally active metabolite of vitamin D3, which serves to activate the vitamin D receptor.

BI-2545 is a potent and selective autotaxin (ATX) inhibitor with IC50 values of 2.2 nM and 3.4 nM for human and rat ATX, reduces plasma LPA levels.

<p>This assay employs the competitive inhibition enzyme immunoassay technique. The microtiter plate provided in this kit has been pre-coated with Mouse MDA protein. Standards or samples are added to the appropriate microtiter plate wells then with a biotin-conjugated antibody specific to Mouse MDA. Next, Avidin conjugated to Horseradish Peroxidase (HRP) is added to each microplate well and incubated. After TMB substrate solution is added. The enzyme-substrate reaction is terminated by the addition of sulphuric acid solution and the color change is measured spectrophotometrically at a wavelength of 450nm ± 10nm. The concentration of Mouse MDA in the samples is then determined by comparing the OD of the samples to the standard curve.</p>

<p>The test principle applied in this kit is Sandwich enzyme immunoassay. The microtiter plate provided in this kit has been pre-coated with an antibody specific to Rat VLDL. Standards or samples are added to the appropriate microtiter plate wells then with a biotin-conjugated antibody specific to Rat VLDL. Next, Avidin conjugated to Horseradish Peroxidase (HRP) is added to each microplate well and incubated. After TMB substrate solution is added, only those wells that contain Rat VLDL, biotin-conjugated antibody and enzyme-conjugated Avidin will exhibit a change in color. The enzyme-substrate reaction is terminated by the addition of sulphuric acid solution and the color change is measured spectrophotometrically at a wavelength of 450nm ± 10nm. The concentration of Rat VLDL in the samples is then determined by comparing the OD of the samples to the standard curve.</p>

4-Nitrophenyl N-acetyl-β-D-galactosaminide is a useful organic compound for research related to life sciences. The catalog number is T67691 and the CAS number is 14948-96-0.

Valiolamine is a useful organic compound for research related to life sciences. The catalog number is T65494 and the CAS number is 83465-22-9.

2-Methylcitric acid trisodium (Methylcitric acid) is an endogenous metabolite in the 2-methylcitric acid cycle, which accumulates in methylmalonic and propionic acidemias.

<p>O-Allylvanillin, an O-allylchalcone derivative, exhibits anti-cancer properties by inhibiting the growth of THP-1, HL60, Hep-G2, and MCF-7 cells with IC50 values of 74.76 μM, 63.52 μM, 90.99 μM, and 90.11 μM, respectively [1].</p>

<p>WAY-339495 may have anti-tumor, anti-inflammatory and analgesic activity and can be used to study obesity, cardiovascular disease, diabetes, neurodegenerative diseases, Alzheimer's disease and stroke.</p>

<p>Cefadroxil is a first generation aminocephalosporin with good patient compliance, a long-acting therapeutic effect, high solubility and relatively broad spectrum of anti-bacterial activity. Cefadroxil is also a substrate of the intestinal peptide transporter PepT1, which is primarily responsible for the drug's uptake across the apical membrane of small intestine.</p>

<p>11β-HSD1-IN-8 is a useful organic compound for research related to life sciences. The catalog number is T65743 and the CAS number is 386704-15-0.</p>

PF-06445974 has good selectivity for PDE4D, excellent brain permeability, and has a high level of specific binding in the "cold tracer" study.

<p>MB07803 is an orally available prodrug of an effective, noncompetitive inhibitor of fructose 1,6-bisphosphatase (FBPase) (EC50: 140 nM and t1/2 of 7.6±2.9 h).</p>

Dichloroiodomethane is a natural compound found in human beings[1].

Z-D-Trp-OH has a wide range of applications in life science related research.

<p>L-N-Benzylserine is a useful organic compound for research related to life sciences. The catalog number is T65056 and the CAS number is 17136-45-7.</p>

R-18986 is a biochemical substance.

<p>1-(2,3-Dichlorphenyl)-piperazine (DCPP) is a potent DHCR7 inhibitor. DHCR7 is the last enzyme in cholesterol biosynthesis.</p>

RORγt Inverse agonist 10 is a highly potent, orally bioavailable compound that acts as an antagonist for the retinoic acid receptor-related orphan nuclear receptor gamma t (RORγt). With an IC50 of 51 nM, it effectively inhibits RORγt activity, a key transcription factor regulating genes linked to psoriasis pathogenesis, including [IL-17A], [IL-22], and [IL-23R].

1-Trityl-1H-imidazole is a useful organic compound for research related to life sciences. The catalog number is T66710 and the CAS number is 15469-97-3.

N1,N8-Diacetylspermidine hydrochloride is a polyamine found in human urine.

<p>4-Phenyl-1H-1,2,3-triazole, an inhibitor of the enzyme IDO1 (IC50: 60 µM), is utilized in cancer research [1].</p>

MRS2802 is a P2Y14 receptor agonist, its EC50 value for P2Y14 receptor is 63 nM.

FFPM is a novel PDE4 inhibitor (IC50: 6 nM) and good selectivity over other PDEs. The drug also penetrates the blood brain barrier well.

3,5-Dibromotyrosine is a useful organic compound for research related to life sciences. The catalog number is T65914 and the CAS number is 300-38-9.

Boc-His(Boc)-OH.DCHA, an amino acid derivative, has a wide range of applications in life science research.

DSR-141562 is a new compound that can be taken orally and has a specific ability to inhibit phosphodiesterase 1 (PDE1) in the brain. This compound exhibits a preference for inhibiting human PDE1B, with an IC50 value of 43.9 nM. It also shows moderate inhibition of human PDE1A (IC50 = 97.6 nM) and PDE1C (IC50 = 431.8 nM). DSR-141562 is particularly useful in the study of positive symptoms, negative symptoms, and cognitive impairments associated with schizophrenia.

<p>Neuraminic acid: acidic amino sugar, 9 carbon chain, from pyruvic acid + D-mannosamine, in active mucoproteins.</p>

<p>3-Deoxy-galactosone, a 1,2-dicarbonyl compound, originates from the degradation of galactose. It forms in food during Maillard and caramelization reactions.</p>