Composés et métabolites pharmaceutiques et vétérinaires

7α,24(S)-Dihydroxycholesterol ((3β,7α,24S)-Cholest-5-ene-3,7,24-triol) acts as a ligand for liver X receptors (LXR), specifically binding to the ligand-binding domains of LXRα and LXRβ. This compound is synthesized through the E-α,β-unsaturated ketone process, starting with arsindole and J-secondary-butyl dimethylsiloxy-bis-positive-5-cholestenal as the initial materials. It undergoes a series of transformations to produce 7α,24(S)-dihydroxycholesterol.

Inosine 5'-diphosphate sodium, a purine ribonucleoside diphosphate with inosine as its nucleobase, plays a role in intracellular energy metabolism and signal transduction processes.

3-Ferrocenylpropionic anhydride is extensively used in compound synthesis, serving as an intermediary for producing various bioactive compounds. Additionally, by modulating specific enzyme activities, 3-Ferrocenylpropionic anhydride has demonstrated potential anti-tumor properties.

RO5101576 is a potent antagonist of LTB4 receptor.

2,4-Dihydroxybutanoic acid is typically not found in extracts of normal human urine and is present only in trace amounts in newborns, while cases of succinic semialdehyde dehydrogenase deficiency consistently exhibit elevated levels of this metabolite.

RBM14C12 is a compound known for its cell signaling activity. It plays a crucial role in researching lipid metabolism and cell membrane structure. Additionally, RBM14C12 can be utilized in the development of novel compounds aimed at modulating the biological mechanisms associated with lipid-related diseases.

<p>Morocromen is a 2-benzamidobenzoic acid derivative characterized by its ability to enhance coronary activity.</p>

Slow isomerization of the C-11 double bond of LTE4 leads to the formation of 11-trans LTE4. 11-trans LTE4 is equipotent to LTE4 in contracting guinea pig ileum.

9-cis-β-Carotene, a precursor of retinal, is cleaved by beta-carotene oxygenase 1 (BCMO1) to produce 9-cis-retinal.

<p>6′SLN is a characteristic glycan found on the surface of cancer-related extracellular vesicles (EVs) and serves as the primary form of protein glycosylation within EVs. Additionally, 6′SLN, a derivative of sialic acid, interacts with hemagglutinins (HAs) from both human and avian influenza strains, making it relevant in the study of anti-influenza drugs.</p>

<p>8-Oxo-dATP can be hydrolyzed to its monophosphate form by the oxidation of purine nucleoside triphosphate MTH1, preventing erroneous incorporation during DNA replication or transcription.</p>

LTF4, made in vitro from LTE4 with enzymes, contracts vascular muscle weakly; potency is LTD4 > LTC4 > LTE4 >> LTF4.

(S)-CPP sodium serves as an inhibitor of the branched-chain α-keto acid dehydrogenase complex (BCKDC) kinase, commonly referred to as BDK or keto acid dehydrogenase kinase. As a negative regulator of BCKDC activity, (S)-CPP (IC50 of 6.3 μM) inhibits BDK, which activates the complex, leading to a significant reduction in the levels of leucine/isoleucine and valine in the plasma of wild-type mice.

<p>Homodestcardin: cyclic depsipeptide from T. roseum with immunosuppressant properties; inhibits mouse T cell proliferation.</p>

Diethylumbelliferyl phosphate (DEUP) is a potent and selective inhibitor of cholesterol esterase that does not inhibit protein kinase A activity in vitro. It disrupts steroidogenesis by blocking cholesterol transport to mitochondria in steroidogenic cells, with an IC50 of 11.6 μM. This compound may also limit the absorption of dietary cholesterol.

<p>MRS4458 is an effective inhibitor of the P2Y14 Receptor.</p>

EpoY (SD-142) is an irreversible inhibitor of the primary brain microtubule-associated tyrosine carboxypeptidase (TCP), a complex formed by vasohibin-1 (VASH1) and small vasohibin-binding protein (SVBP). By inhibiting TCP with an IC50 value of approximately 500 nM, EpoY effectively reduces the levels of detyrosinated α-tubulin, which is crucial for microtubule dynamics and neuronal differentiation. This inhibition results in significant differentiation defects and is linked to potential issues related to cancer and cardiomyopathy.

Substituted piperidines-1 can promote the release of growth hormone in humans and animals.

<p>Toladryl is a derivative of Diphenhydramine that can cross the blood-brain barrier and exhibits oral activity, with antihistamine and anticholinergic properties. Its anticholinergic effects are approximately a tenth of those seen with Diphenhydramine, yet it offers 2-4 times the protection against lethal doses of histamine in guinea pigs. The side effects of Toladryl are fewer and milder compared to Diphenhydramine; however, at higher doses, it may cause symptoms such as insomnia, agitation, and disorientation related to the central nervous system. Toladryl is utilized in the research of allergic diseases.</p>

SAR114137 is a highly effective pharmaceutical compound characterized by potent bioactivity. It exhibits variations in its amorphous content during the physical processing of crystalline active pharmaceutical ingredients (APIs). The amorphous API content of SAR114137 significantly decreases when subjected to various jet milling techniques. Additionally, SAR114137 demonstrates good chemical stability in drug formulations.

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

3-Benzylidenecamphor, a UV absorber, is noted for its excellent photostability and antioxidant activity. It is extensively utilized in sunscreen products to shield the skin from UV damage. Additionally, 3-Benzylidenecamphor is used in cosmetics to enhance product shelf life and safety.

<p>Xanthosine 5'-monophosphate is produced from inosine monophosphate (IMP) through the catalytic action of inosine monophosphate dehydrogenase (IMPDH).</p>

<p>Urobilin hydrochloride, a metabolic byproduct of Hemoglobin, is excreted through urine and feces in various mammals. It also serves as an indicator of human waste contamination.</p>

<p>Porphobilinogen act as a phytotoxin, a metabotoxin, and a neurotoxin.</p>

3β,7β-Dihydroxy-5-cholestenoic acid is a C27 acid whose levels are elevated in Niemann-Pick Type C and B diseases, leading to toxicity in ocular motor neurons. It is synthesized by the enzymatic action of hydroxysteroid 11-β dehydrogenase 1 from 3β-hydroxy-7-oxocholest-5-en-(25R)26-enoic acid (3βH,7O-CA).

<p>4-Hexen-3-one inhibits the growth of H. pylori in the ATCC 43526 strain and TDR strain. Additionally, this compound suppresses urease activity.</p>

1,2-Dipentadecanoyl-rac-glycerol (DG(15:0/15:0/0:0)) is a compound referenced in studies examining the effect of insulin on the content of 1,2-diacylglycerol in rat hearts. Insulin is observed to increase the amount of 1,2-diacylglycerol containing specific fatty acid compositions in the heart, which may be linked to cardiac contractility.

c-di-GMP sodium: STING activator, regulates bacteria biofilm, motility, virulence.

15-keto-Prostaglandin E2, an endogenous metabolite, inhibits STAT3 activation through binding to Cys259 and regulates breast cancer cell growth and progression.

Miaosporone A: angucyclic quinone, cytotoxic to MCF-7, NCI-H187, Vero cells; anti-TB and anti-malaria with IC50 of 2.4 μM, 2.5 μM.

D-Citrulline (H-D-Cit-OH), a stereoisomer of L-citrulline, effectively reduces cardiac contractile dysfunction caused by polymorphonuclear leukocyte (PMN) in isolated perfused rat hearts undergoing ischemia/reperfusion. This protective effect is mediated through a non-NO-mediated mechanism.

1-Phenylethanamine, a potential central nervous system stimulant related to β-phenylethylamine (β-phenylethylamine), exhibits diminished glycogenolysis activity in the brain due to its benzene ring being replaced by an indole group. This reduction in activity makes it useful for investigating how the chemical structure of phenylethylamine derivatives influences their effects on the central nervous system. Additionally, 1-Phenylethanamine is also utilized in the synthesis of the tyrosine kinase (tyrosine kinase) inhibitor CLM3.

LXA5 is made from EPA by leukocytes, contracts guinea pig lungs like LXA4/LXB4, but doesn't dilate aorta.

13(R)-HODE, produced from linoleic acid, inhibits platelet aggregation (IC50=2.7μM) and is found in bovine endothelial cells.

22-Hydroxy Mifepristone (RU 42698) is an orally active hydroxylated alcohol metabolite that exhibits both anti-progestational and anti-glucocorticoid activities. This compound contains an alkyne group and is capable of undergoing copper-catalyzed azide-alkyne cycloaddition (CuAAC) with azide-containing molecules. Furthermore, 22-Hydroxy Mifepristone demonstrates a relative binding affinity of 48% to the human glucocorticoid receptor.

RvE4, a bioactive lipid from eicosapentaenoic acid and synthesized by 15-LO, is anti-inflammatory and boosts efferocytosis in human macrophages.

L-Sepiapterin aids in making BH4, a coenzyme essential for eNOS, enhancing artery function and angiogenesis, while suppressing ovarian cancer cell growth.

CS-003 HCl is a TNRA - triple neurokinin receptor antagonist.

4-Amino-3-hydroxyphenylalanine (4-AHP) is a photodegradation product of eumelanin. It can be utilized in research focused on the formation of cutaneous melanoma and age-related macular degeneration.

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.

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

Lichenase, an enzyme, breaks down β-glucans in grains into GOS, aiding polysaccharide degradation in cell walls.

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.

<p>L-Glyceric acid sodium, a urinary metabolite, is predominantly found in individuals with the rare inherited metabolic disorder L-glyceric aciduria. This compound is a diagnostic tool for identifying primary hyperoxaluria type 2 (PH2) and distinguishing it from primary hyperoxaluria type 1 (PH1) based on its excretion pattern.</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.

<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>3-Hydroxy-4-aminopyridine is a natural product for research related to life sciences. The catalog number is T66009 and the CAS number is 52334-53-9.</p>

<p>2-(Methoxycarbonyl)benzoic acid is a natural product for research related to life sciences. The catalog number is T67426 and the CAS number is 4376-18-5.</p>

<p>Vitamin D3 octanoate, an ester derived from vitamin D3, is commonly known as cholecalciferol. Cholecalciferol is a naturally occurring form of vitamin D with notable properties such as inducing cell differentiation and impeding cancer cell proliferation.</p>

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

<p>(S)-3-Hydroxyisobutyric acid is an important interorgan metabolite.</p>

<p>Beta-Cortol is a metabolite of androgen present in adults.</p>

<p>Creatinine-D3 is a deuterium-labeled Creatinine which is a break-down product of creatine phosphate in muscle.</p>

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

L-Cysteine S-sulfate sodium salt sesquihydrate is a useful organic compound for research related to life sciences. The catalog number is T64782 and the CAS number is 150465-29-5.

1-Arachidoyl-sn-glycero-3-phosphocholine is a lysophospholipid (LyP).

<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>

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

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

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

<p>(±)-α-Tocopherol nicotinate is a useful organic compound for research related to life sciences. The catalog number is T64563 and the CAS number is 51898-34-1.</p>

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

GDP-D-mannose disodium is a natural product for research related to life sciences and the catalog number is T65209.

<p>10Z-Nonadecenoic acid is a long-chain fatty acid with anti-tumor activity.</p>

<p>4-Hydroxybenzyl cyanide (4-Hydroxyphenylacetonitrile) shows strong antioxidative activity.</p>

<p>Coumaran (2,3-Dihydrobenzofuran) is an acetylcholinesterase (AChE) inhibitor isolated from leaves of L. camara. Coumaran(2,3-Dihydrobenzofuran) can be used as a biopesticide. 2,3-dihydrobenzofuran is a member of the class of 1-benzofurans that is the 2,3-dihydroderivative of benzofuran. It has a role as a metabolite.</p>

<p>p-Toluic Acid (4-Methylbenzoic acid) belongs to the class of organic compounds known as benzoic acids. 4-Methylbenzoic acid has been primarily detected in saliva. Within the cell, 4-methylbenzoic acid is primarily located in the cytoplasm.</p>

<p>Isonicotinic acid is a metabolite of Isoniazid.Isonicotinic acid is a useful isomer of nicotinic acid. Isoniazid is converted to Isonicotinic acid by hydrazinolysis, with the biotransformation also to be catalyzed by cytochrome P450 enzymes, such as CYP2C.</p>

<p>Applications Derivative of Artemisinin (A777500). Antimalarial, used to treat strains of malaria which are multi-drug resistant.<br>References Hombhanje, F., et al.: Pharma., 3, 3581 (2010), Michael, O., et al.: Malaria J., 9, 335 (2010), Cesar, I., et al.: J. Pharm. Biomed. Anal., 54, 114 (2011),<br></p>

1-Methyladenine is a DNA alkylation product that undergoes damage reversal through oxidative demethylation for repair purposes.