Metabolismo

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

<p>L-690488 has more effective cell penetration than L-690330. L-690488 is a prodrug of L-690330 and is a selective inositol monophosphatase (IMPase) inhibitor.</p>

<p>CAY10435, a β-ketooxazapyridine and selective FAAH inhibitor, exhibits antimicrobial properties. It binds non-competitively to the FAAH of Dictyostelium discoideum, demonstrating a Kd value of 0.57 nM [1] [2].</p>

<p>Sch59498 is a potent phosphodiesterase 1c (Pde1c) inhibitor.</p>

<p>Diethyl-pythiDC is an collagen prolyl 4-hydroxylase inhibitor.</p>

<p>Leukotriene C4 (14,15-LTC4) is an inflammatory mediator synthesized from arachidonic acid through the actions of 15- and 12-lipoxygenases (LOs), involving intermediates such as 15-HpETE and 14,15-LTA4. Unlike the majority of leukotrienes formed via the 5-LO pathway, 14,15-LTC4 is an eoxin predominantly produced by eosinophils, although mast cells and nasal polyps can also synthesize it. While its physiological roles are not well understood, 14,15-LTC4 exhibits limited contractile activity on guinea pig ileum and pulmonary parenchyma. However, it can increase vascular permeability in human endothelial cell monolayers in vitro with potency comparable to 5-LO-derived leukotrienes, contributing to plasma leakage characteristic of inflammation.</p>

<p>PF-04937319 activates glucokinase (EC50=154.4μM) with low hypoglycemia risk, researched for type 2 diabetes treatment.</p>

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

<p>GLUT4 activator 1 is a potent glucose transporter type 4 (GLUT4) translocation activator (EC50: 0.14 μM).</p>

<p>ICMT-IN-5 (compound 46) is an ICMT inhibitor with an IC50 value of 0.3 μM [1].</p>

<p>OSMI-2 is a cell-permeable inhibitor of O-linked N-acetylglucosamine transferase (OGT).</p>

KCA-1490 is an inhibitor of dual PDE3/4.

<p>BMS-185411 is a bio-active chemical.</p>

<p>S-(p-Nitrobenzyl)glutathione acts as a competitive inhibitor of glutathionase.</p>

<p>1,2-Dimyristoyl-3-palmitoyl-rac-glycerol (MMP) is a triacylglycerol comprising myristic acid and palmitic acid [1].</p>

<p>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</p>

<p>ICMT-IN-26 (compound 38) acts as an ICMT inhibitor with an IC50 value of 0.36 μM [1].</p>

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

<p>UCPH-102: Selective EAAT1 inhibitor, IC50 0.43 μM, treats Alzheimer's, ALS, chronic pain, OCD; crosses blood-brain barrier, targets T-ALL cells.</p>

<p>Phenylpyropene C inhibits JAK/STAT and IFN-γ expression (IC50: 5.4-10.8 μM), also blocks acyl CoA (IC50: 16.0 μM).</p>

<p>Monohydroxy melphalan, a degradation product and DNA alkylating agent derived from melphalan, results from melphalan hydrolysis in aqueous solutions such as cell culture medium and human plasma. It enhances DNA adducts in ML-1 myeloblastic leukemia cells based on concentration and induces cytotoxicity with an IC50 value of 28.1 μg/ml.</p>

<p>Glycosidase-IN-1, a D-mannose-derived inhibitor, has hypoglycemic effects and aids in creating immunosuppressants and β-glucosidase blockers.</p>

<p>Selenocystine, a broad-spectrum anticancer agent, effectively induces DNA damage, notably DNA double-strand breaks (DSBs), in HepG2 cells, showcasing</p>

<p>FAS-IN-1 Tosylate is an effective fatty acid synthase inhibitor;Has an IC50 of 10 nM.</p>

<p>ICMT-IN-19 (compound 53) serves as a potent inhibitor of ICMT, demonstrating an IC50 value of 0.026 μM [1].</p>

<p>IDH1 Inhibitor 2 (compound 13) is a potent IDH1 inhibitor via direct covalent modification of His315 (IC50: 110 nM).</p>

<p>12(R)-HEPE, a monohydroxy fatty acid derived from EPA in the eggs of the sea urchin S. purpuratus, has a biological activity that, while not extensively documented, may resemble that of 12(R)-HETE (Catalog No.34560).</p>

<p>GNE-6468 is a potent and selective agonist of RORγ(RORc) (EC50: 13 nM for HEK-293 cell).</p>

<p>Quercetin 7-glucuronide (Quercetin 7-O-β-glucuronide), a Quercetin metabolite found in Madagascarian Uncarina species, has the capability to inhibit LDL</p>

<p>CYP17-IN-1 is an effective oral inhibitor of CYP17 that can inhibit CYP17 in rats and humans with IC50 of 15.8 and 20.1 nM.</p>

<p>PPACK: synthetic peptide, irreversibly inhibits thrombin (Ki = 0.24 nM), prevents platelet activation.</p>

<p>1-Palmitoyl-2-oleoyl-sn-glycero-3-PA (1,2-POPA) is a phospholipid featuring a palmitic acid (16:0) chain that is saturated and an oleic acid (18:1) chain that is monounsaturated, positioned at the sn-1 and sn-2 locations, respectively. This compound is utilized in creating micelles, liposomes, and various artificial membrane forms.</p>

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

<p>Quizalofop (Xylafop) is a reagent of biochemical.</p>

<p>7,7-Dimethyl-(5Z,8Z)-eicosadienoic acid (DEDA, 5 μM) significantly impacts the response to βA(25-35) stimulation. It reduces the formation of ROS.</p>

<p>Miglustat hydrochloride (N-Butyldeoxynojirimycin hydrochloride) is an inhibitor of glucosylceramide synthase and can be used for studies about Type I Gaucher</p>

FM26, an isoxazole-based RORγt inverse agonist, cuts EL4 IL-17a mRNA; potent with 264 nM IC50.

<p>15-PGDH-IN-1: potent oral 15-PGDH inhibitor, IC50=3nM, useful for tissue repair research.</p>

<p>ICMT-IN-50 (compound 3) serves as an inhibitor of ICMT with an IC50 value of 0.31 µM [1].</p>

<p>Potent LXR agonist; AC50: 1.5 nM (LXR-α), 12 nM (LXR-β); potential in atherosclerosis research.</p>

<p>Fasidotril inhibits NEP/ACE, treats high blood pressure in rats, effective in humans with hypertension.</p>

<p>LX-1031 is an effective inhibitor of tryptophan 5-hydroxylase. LX-1031 decreases serotonin (5-HT) synthesis peripherally.</p>

<p>GSK3987 is an LXR ligand. GSK3987 recruits the steroid receptor coactivator-1 to human LXRalpha and LXRbeta with EC50s of 40 nM.</p>

<p>13-OAHSA, a branched fatty acid ester of hydroxy fatty acids (FAHFAs), results from the esterification of oleic acid to 13-hydroxy stearic acid. It represents a significant component of the FAHFA family, most abundantly expressed in the serum of glucose-tolerant AG4OX mice that exhibit adipose tissue-specific overexpression of the Glut4 glucose transporter. Similar to other FAHFAs which are known to enhance glucose tolerance, stimulate insulin secretion, and exert anti-inflammatory effects, 13-OAHSA may play a pivotal role in managing metabolic syndrome and inflammation.</p>

<p>MγLnFP, an analog of methyl arachidonyl fluozophosphonate (MAFP), holds significance in pharmacological research due to its potential as an inhibitor of phospholipases, FAAH, and its role as a CB receptor ligand. However, the properties and effects of the γ-linolenyl variant of MAFP remain to be fully explored.</p>

<p>GPX4-IN-4 (Compound 24) serves as a potent inhibitor of GPX4, applicable in cancer research [1].</p>

<p>LFHP-1c, a neuroprotective PGAM5 inhibitor, demonstrates efficacy in preserving blood-brain barrier integrity following ischemic stroke.</p>

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

<p>DMPA, a derivative of phosphatidic acid (PA), constitutes a significant component of cellular membranes.</p>

<p>Ionizable Lipid-2 (Compound 1) serves as an ionizable lipid, essential for nucleic acid delivery and the construction of lipid nanoparticles (LNPs) [1].</p>

<p>Siguazodan (SKF 94836) is an effective, selective, orally active phosphodiesterase III ((PDE-III)) inhibitor with an IC50 of 117 nM.</p>

<p>Oxalomalic acid (Oxalomalate) trisodium, an inhibitor of aconitase and NADP-dependent isocitrate dehydrogenase, suppresses nitrite production and inducible nitric oxide synthase (iNOS) protein expression in lipopolysaccharide-activated J774 macrophages [1].</p>

<p>GIV3727, a bitter taste receptor hTAS2R antagonist, inhibits the activation of hTAS2R31 by saccharin and acesulfame potassium, effectively diminishing the</p>

<p>1,2-Dioleoyl-3-docosohexaenoyl-rac-glycerol, a triacylglycerol, consists of oleic acid at the sn-1 and sn-2 positions and docosahexaenoic acid at the sn-3 position. This compound has been identified in human breast milk.</p>

<p>Prostaglandin H2 (PGH2), initially isolated from the incubation of arachidonic acid with ovine seminal vesicle microsomes, acts as a potent vasoconstrictor. It serves as the precursor for all 2-series prostaglandins (PGs) and thromboxanes (TXs). Moreover, as a TP receptor agonist, PGH2 irreversibly aggregates human platelets at concentrations of 50-100 ng/ml.</p>

<p>QH536 degrades HMGCR (EC50: 0.22 μM), has anti-inflammatory properties, and avoids cholesterol buildup; useful for cardiovascular and NASH research.</p>

<p>FR-190809 is a nonadrenotoxic and orally efficacious inhibitor of acyl-CoA:cholesterol O-acyltransferase (ACAT) (IC50: 45 nM).</p>

<p>Hemipyocyanine (528-71-2) is the virulence factor of Gram-negative, aerobic rod bacterium Pseudomonas aeruginosa. Hemipyocyanine is an α-Amylase inhibitor.</p>

<p>Aladotril is an inhibitor of neutral endopeptidase. Its prodrug is aladotrilat.</p>

<p>1-Oleoyl-2-hydroxy-sn-glycero-3-PG (sodium salt), a lysophospholipid with oleic acid (18:1) at the sn-1 position, finds application in creating micelles, liposomes, and various artificial membranes, notably in lipid-based drug delivery systems.</p>

<p>ICMT-IN-52 (compound 44) serves as an ICMT inhibitor with an IC50 value of 0.052 μM [1].</p>

<p>DPM-1001 is an orally bioavailable and non-competitive protein-tyrosine phosphatase (PTP1B) inhibitor (IC50: 100 nM) with the anti-diabetic property.</p>

<p>ML395 is a potent, selective PLD2 allosteric inhibitor with potent antiviral activity (IC50 =360 nM).</p>

<p>LNP Lipid-8 (11-A-M), an ionizable lipid, is utilized in lipid nanoparticles (LNP) for siRNA delivery to T cells without ligand targeting. When loaded with GFP siRNA (siGFP), it significantly silences the GFP gene in a mouse model [1].</p>

<p>cKK-E15, a peptide-lipid, is instrumental in formulating LNP3 alongside C14PEG2000, unmodified cholesterol, and DOPE [1].</p>

<p>Nampt-IN-10 TFA, a NAMPT inhibitor, shows potency in A2780 (IC50: 5 nM) and CORL23 (IC50: 19 nM), suitable for ADC payloads.</p>

<p>TMP778 is an effective and selective RORγt inverse agonist (IC50: 7 nM in FRET assay).</p>

<p>11-Dehydro-2,3-Dinor Thromboxane B2 is a metabolite of Thromboxane B2 (TXB2), formed by the oxidation of TXB2 via 11-Hydroxy Thromboxane Dehydrogenase.</p>

<p>FXa-IN-1, an FXa blocker: IC50=3 nM, Ki=0.7 nM, orally available, long half-life, for thrombosis research.</p>

<p>14,15-Epoxyeicosatrienoic acid (14,15-EET), derived from Arachidonic acid metabolism, significantly inhibits platelet aggregation in vivo and enhances</p>

<p>1-Myristoyl-2-linoleoyl-3-oleoyl-rac-glycerol, a triacylglycerol, features myristic acid, linoleic acid, and oleic acid at the sn-1, sn-2, and sn-3 positions, respectively. This compound is prevalent in mature human milk, infant formula fats, and butterfat.</p>

<p>(Rac)-Lonafarnib is a racemic FTase inhibitor, effective against H-ras, K-ras, N-ras (IC50: 1.9, 5.2, 2.8 nM), and has anti-HDV properties.</p>

<p>N-Methyl Palbociclib is an impurity of the orally active selective CDK4 and CDK6 inhibitor Palbociclib (PD 0332991).</p>

<p>FR-234938 is a non-nucleoside adenosine deaminase inhibitor with anti-inflammatory activity.</p>

<p>GNE-618 is a potent and orally active inhibitor of nicotinamide phosphoribosyltransferase (IC50: 6 nM).</p>

<p>Kelatorphan is an enkephalin degrading enzyme full inhibitor.</p>

<p>KH064 is a sPLA2-IIA inhibitor of oral activity.</p>

<p>Glycosidase-IN-2 is a glycosidase inhibitor with hypoglycemic activity.</p>

<p>1,2-Dipalmitoyl-sn-glycero-3-N,N-dimethyl-PE is a derivative of 1,2-dipalmitoyl-sn-glycero-3-PE (1,2-DPPE) with two added methyl groups on its sn-3 moiety, which in aqueous suspensions, reduces the phase transition temperature relative to those of 1,2-DPPE and 1,2-dipalmitoyl-sn-glycero-3-N-methyl-PE (1,2-NMeDPPE). It is utilized in creating liposomes and monolayers for investigating membrane permeability and monolayer viscosity.</p>

<p>Iomazenil is an antagonist and partial inverse agonist of benzodiazepine and potential therapy for alcohol abuse.</p>

<p>M5N36: selective Cdc25C inhibitor, IC50: 0.15µM A, 0.19µM B, 0.06µM C; halts cell growth, boosts p-CDK1/2.</p>

<p>ICMT-IN-12 (compound 78) serves as an ICMT inhibitor, demonstrating an IC50 value of 0.42 μM [1].</p>

<p>A 62198 is a potent and selective renin inhibitor with potential as a hypotensive agent.</p>

<p>Gisadenafil (UK-369003) is a selective inhibitor of phosphodiesterase 5 (PDE5) with an IC50 of 3.6 nM and prevents degradation of cGMP.</p>

<p>SHP2-IN-17 (compound 192) is a potent inhibitor of SHP2, exhibiting an IC50 of 2 nM and holds potential for use in glioblastoma research [1].</p>

<p>ICMT-IN-31 (compound 68) serves as an ICMT inhibitor, demonstrating significant potency with an IC50 value of 0.0038 μM [1].</p>

<p>NUCC-0223619 is an IDO1 inhibitor that induces the degradation of IDO protein and can be involved in the synthesis of PROTAC.</p>

<p>1-Palmitoyl-2-oleoyl-3-stearoyl-rac-glycerol, a primary triacylglycerol in cocoa butter, features palmitic acid (at the sn-1 position), oleic acid (at the sn-2 position), and stearic acid (at the sn-3 position).</p>

<p>ATX inhibitor 15, an indole-based carbamate, has a 2.17 nM IC50 against ATX, suppresses pro-fibrotic genes, and protects against mouse lung fibrosis.</p>

<p>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.</p>

<p>Mitochondria degrader-1, a potent autophagy inducer, aids in neurodegenerative, cancer, and aging disease research.</p>

<p>H2-003 is a selective inhibitor of diacylglycerol acyltransferase 2 (DGAT2).</p>

<p>SREBP/SCAP-IN-2 (compound 13) acts as a selective inhibitor of SREBP/SCAP [1].</p>

<p>1,2-Dilauroyl-sn-glycero-3-phospho-(2R)-glycerol is a type of phosphoglycerol characterized by the presence of lauric acid at the sn-1 and sn-2 positions. [Matreya, LLC. Catalog No. 1443]</p>

<p>ICMT-IN-33 (compound 73) functions as an ICMT inhibitor with an IC50 value of 0.46 μM [1].</p>

<p>Hypusine is an N-terminal amino alcohol derivative of Lys occurring in bovine brain &amp;</p>

<p>Lp-PLA2-IN-9, a tetracyclic pyrimidinone, inhibits rhLp-PLA2 (pIC50: 10.1), promising for neurodegenerative research.</p>

<p>6β-hydroxy Testosterone （4-Androsten-6β,17β-diol-3-one） is a 17β-hydroxy steroid, an androgen and endogenous metabolite.</p>

<p>RORγt agonist 2 is a potent agonist of RORγt.</p>

<p>YM17E is an inhibitor of ACAT with IC50 of 44 nM in rabbit liver microsomes in vitro.</p>