Metabolism

Items 2501-2550 of 6503

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  1. picomolar PDE1 inhibitor

    ITI-214 (free base) is a picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activity (Ki = 58 pM).
  2. LOXL2 inhibitor

    PAT-1251 Hydrochloride is a potent, selective and oral lysyl oxidase-like 2 (LOXL2) inhibitor, with IC50s of 0.71 and 1.17 μM for hLOXL2 and hLOXL3, respectively, and also potently inhibits mouse, rat, and dog LOXL2 (IC50s, 0.10, 0.12, and 0.16 μM, respectively).
  3. PDEδ inhibitor

    Deltasonamide 2 is a competitive, high affinity PDEδ inhibitor with a Kd of ~385 pM.
  4. all-trans-4-Oxoretinoic acid, an active metabolite of vitamin A, induces gene transcription via binding to nuclear retinoic acid receptors (RARs).
  5. PDEδ inhibitor

    Deltasonamide 2 TFA is competitive, high affinity PDEδ inhibitor with a Kd of ~385 pM.
  6. Sevelamer is a phosphate binding drug used to treat hyperphosphatemia in patients with chronic kidney disease; consists of polyallylamine that is crosslinked with epichlorohydrin.
  7. AHR antagonist

    BAY 2416964 is a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018146010A1, example 192, has an IC50 of 341 nM. BAY 2416964 has the potential for solid tumors treatment.
  8. succinate dehydrogenase (SQR) enzyme inhibitor

    Fluxapyroxad, a broad-spectrum fungicide, is an inhibitor of the succinate dehydrogenase (SQR) enzyme.
  9. MAO-B inhibitor

    PF9601N is a selective and potent monoamine oxidase B inhibitor that exhibit anti-Parkinsonian effects in several models of PD.
  10. Autotaxin Inhibitor IV

    HA155, also known as Autotaxin Inhibitor IV, is a boronic acid-based compound that inhibits autotaxin (IC50 = 5.7 nM) by selectively binding to its catalytic threonine.
  11. RARβ agonist

    BMS453 (BMS-189453), a synthetic retinoid, is a RARβ agonist and a RARα/RARγ antagonist.
  12. Phospholipase D2 (PLD2) inhibitor

    ML298 (CID53393915) is a potent, specific inhibitor of Phospholipase D2 (PLD2) with IC50 of 355 nM.
  13. rabbit platelet sPLA2 inhibitor

    YM-26734 is a rabbit platelet sPLA2 inhibitor that has been used to ameliorate local inflammatory responses in TPA-induced mouse ear edema.
  14. AhR modulator

    SGA360 is a selective modulator of aryl hydrocarbon (Ah) receptor that exhibits anti-inflammatory properties.
  15. urinary metabolite

    Creatine riboside is a urinary metabolite and is a diagnostic and prognostic biomarker of lung cancer.
  16. activator and non-inhibitory chaperone of glucocerebrosidase

    ML198 is a novel activator and non-inhibitory chaperone of glucocerebrosidase.
  17. noninhibitory chaperone of glucocerebrosidase (Gcase)

    NCGC607 is a a noninhibitory chaperone of glucocerebrosidase (GCase).
  18. LDHA inhibitor

    GNE-140 racemic is a novel potent lactate dehydrogenase (LDHA) inhibitor.
  19. SCAP inhibitor

    Lycorine is a natural alkaloid extracted from the Amaryllidaceae plant. Lycorine is a potent and orally active SCAP inhibitor with a Kd value 15.24 nM.
  20. Eurycomanone could increases spermatogenesis by inhibiting the activity of phosphodiesterase and aromatase in steroidogenesis.
  21. Cytochrome P450 hibitor

    Gentiopicroside, a naturally occurring iridoid glycoside, inhibits P450 activity, with an IC50 and a Ki of 61 ?M and 22.8 ?M for CYP2A6; Gentiopicroside has antianti-inflammatoryand antioxidative effects.
  22. Hsp70 activator

    ML346 is an activator of Hsp70 expression and HSF-1 activity, with an EC50 of 4.6 μM for Hsp70.
  23. NNMT inhibitor

    JBSNF-000088 (6-Methoxynicotinamide), a analog of nicotinamide (NA), is a potent Nicotinamide N-methyltransferase (NNMT) inhibitor with IC50s of 1.8 ?M, 2.8 ?M, and 5.0??M for human NNMT, monkey NNMT and mouse NNMT, respectively.
  24. enpp-1 inhibitor

    Enpp-1-IN-1 is a Ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1) inhibitor extracted from patent WO2019046778, Example 55.
  25. PPAR alpha agonist

    Pemafibrate, also known as (R)-K 13675, is a PPAR alpha agonist.
  26. OXPHOS inhibitor

    VLX600 is an iron-chelating inhibitor of oxidative phosphorylation (OXPHOS).
  27. Ticlopidine (Yuclid, Ticlopidinum, Ticlopidina) is an orally active inhibitor of platelet aggregation induced by adenosine diphosphate (ADP).
  28. electron transport chain inhibitor

    HQNO, secreted by P. aeruginosa, is a potent electron transport chain inhibitor with a Kd of 64 nM for complex III.
  29. mutant IDH-1 inhibitor

    DS-1001b is a mutant IDH-1 (Isocitrate Dehydrogenase-1) inhibitor extracted from patent WO2016052697A1, Example 168, and has antitumor activity.
  30. GCase activator

    ML266 (CID-46943215) is a activator of glucocerebrosidase (GCase) that does not inhibit the enzyme??s action but can still facilitates its translocation to the lysosome.
  31. marine xenobiotic metabolite

    Imidacloprid-urea with a role as a marine xenobiotic metabolite, is the primary imidacloprid soil metabolite, whereas imidacloprid-olefin is the main plant-relevant metabolite and is more toxic to insects than imidacloprid.
  32. ALDH1A1 inhibitor

    Propachlor is a specific ALDH1A1 inhibitor. It is sometimes used as an herbicide.
  33. glutathione-independent inhibitor

    iFSP1 is a potent, selective and glutathione-independent inhibitor of ferroptosis suppressor protein 1 (FSP1) (AIFM2) with an EC50 of 103 nM.
  34. epigenetic modifier

    L-2-Hydroxyglutaric acid disodium ((S)-2-Hydroxyglutaric acid disodium, L-2-Hydroxyglutarate disodium, LGA, L-2HG) is an epigenetic modifier and a putative oncometabolite in kidney cancer that inhibits histone demethylases and hence promotes histone methylation.
  35. Autophagy inducer

    Tomatidine hydrochloride acts as an anti-inflammatory agent by blocking NF-κB and JNK signaling. Tomatidine hydrochloride activates autophagy either in mammal cells or C elegans.
  36. NF-κB inhibitor

    Urolithin B is one of the gut microbial metabolites of ellagitannins, and has anti-inflammatory and antioxidant effects. Urolithin B is also a regulator of skeletal muscle mass.
  37. Pyruvic acid (Acetylformic acid) is an important organic chemical intermediate that plays a role in cardiomyocyte pathophysiology and therapy.
  38. Palmitoleic acid, a composition of fatty acid, is implicated in the prevention of death from cerebrovascular disorders in SHRSP rats.
  39. immunomodulatory agent

    3-Hydroxyanthranilic Acid (3-HAA, 3-HANA), a tryptophan metabolite, has an immunomodulatory effect that may result from inhibition of PI3K/Akt/mTOR and NF-κB activity, thereby decreasing the production of pro-inflammatory mediators.
  40. GK activator

    Dorzagliatin (HMS5552), a dual-acting glucokinase (GK) activator, improves glycaemic control and pancreatic β-cell function in type 2 diabetes.
  41. GLUT1 inhibitor

    Lavendustin B is an inhibitor of HIV-1 integrase interaction with LEDGF/p75 with an IC50 of 94.07 μM. Lavendustin B is an ATP-competitive GLUT1 inhibitor with a Ki of 15 ?M. Lavendustin B is also a weak inhibitor of tyrosine kinases.
  42. PASK inhibitor

    BioE-1115 is a highly selective and potent PAS kinase (PASK) inhibitor with an IC50 of ~4 nM. BioE-1115 is also a potent casein kinase 2α inhibitor with an IC50 of ~10 μM.
  43. antioxidant

    2-Phospho-L-ascorbic acid trisodium acts as an antioxidant and a stimulator of hepatocyte growth factor (HGF) production.
  44. DCLK1 domain probe

    DCLK1-IN-1 is a selective, oral bioavailability in vivo-compatible chemical probe of the doublecortin like kinase 1 (DCLK1 kinase) domain.
  45. Antioxidant agent

    Dihydrocaffeic acid is a phenolic acid found in Gynura bicolor, reduces phosphorylation of MAPK p38 and prevent UVB-induced skin damage. Antioxidant potential and anti-inflammatory activity.
  46. sEH inhibitor

    AUDA (compound 43) is a potent soluble epoxide hydrolase (sEH) inhibitor with IC50s of 18 and 69 nM for the mouse and human sEH, respectively. AUDA has anti-inflammatory activity.
  47. antifungal

    The compound 7,4'-Di-O-methylapigenin may be partly responsible for the reported antifungal activity of C. zeyheri, and may serve as a potential source of lead compounds that can be developed as antifungal phytomedicines.
  48. antioxidant agent

    Pyridoxine (Pyridoxol) is a pyridine derivative. Pyridoxine exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
  49. PKM2 activator

    Mitapivat is a pyruvate kinase isoenzyme M2 (PKM2) activator.
  50. uPA inhibitor

    UK-371804 is a potent and selective urokinase-type plasmogen activator (uPA) inhibitor with excellent enzyme potency (Ki=10 nM) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin).

Items 2501-2550 of 6503

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