Metabolism

Items 851-900 of 6503

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  1. Perindopril Butylamine Salt is an angiotensin-converting enzyme (ACE) inhibitor.
  2. PDE inhibitor

    Pimobendan (Vetmedin) is a calcium sensitizer with positive inotropic and vasodilator effects. It is also a selective inhibitor of phosphodiesterase III (PDE3).
  3. CYP3A4 inhibitor

    Posaconazole is an inhibitor primarily of CYP3A4, but it does not inhibit the activity of other CYP enzymes; Also an inhibitor of sterol C14?? demethylase inhibitor with IC50 of 0.25 μM. Posaconazole has a median terminal elimination half-life of 15-35 hours.
  4. Prednisolone is a glucocorticoid with the general properties of the corticosteroids.
  5. MAO-B inhibitor

    Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C.
  6. ACE inhibitor

    Ramipril is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 5 nM.
  7. Ranolazine is a partial fatty acid oxidation inhibitor, shifts ATP production from fatty acid to more oxygen-efficient carbohydrate oxidation.
  8. Ranolazine dihydrochloride (CVT 303 dihydrochloride) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP).
  9. HMG-CoA reductase inhibitor

    Rosuvastatin (Crestor) is a member of the drug class of statins, used to treat high cholesterol and related conditions, and to prevent cardiovascular disease. Rosuvastatin is a competitive inhibitor of the enzyme HMG-CoA reductase, having a mechanism of action similar to that of other statins.
  10. mitochondrial electron transport chain complex I inhibitor

    Rotenone is an mitochondrial electron transport chain complex I inhibitor. Rotenone induces apoptosis through enhancing mitochondrial reactive oxygen species production.
  11. PDE4 inhibitor

    (S)-(+)-Rolipram ((+)-Rolipram) is a cyclic AMP(cAMP)-specific phosphodiesterase 4 (PDE4) inhibitor, with an IC50 of 1100 nM. (S)-(+)-Rolipram can suppresse tumor necrosis factor-alpha (TNFα) production by human mononuclear cells.
  12. MAO Inhibitor

    Safinamide Mesylate is mesylate salt of Safinamide, which selectively and reversibly inhibits MAO-B with IC50 of 0.45 μM.
  13. PDE5 inhibitor

    Sildenafil citrate is a potent phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 5.22 nM.
  14. HMG-CoA reductase inhibitor

    Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.
  15. Sodium danshensu is a sodium salt of danshensu from the widely used Chinese herb Danshen (Salvia miltiorrhiza Bunge). In vitro and in vivo studies revealed that danshensu possessed diverse pharmacological effects, including relaxation of coronary artery, anticoagulation, protection of myocardial ischemia-reperfusion injury, and antiarrhythmia activities
  16. HDAC inhibitor

    Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2.
  17. Sulfasalazine is a drug for the treatment of rheumatoid arthritis and ulcerative colitis. Sulfasalazine is reported to suppress NF-κB activity.
  18. PDE5 inhibitor

    Tadalafil is a PDE5 inhibitor with an IC50 value of 1.8 nM.
  19. Tazarotene is a prodrug and a member of the acetylenic class of retinoids.
  20. Hydroxylase inhibitor

    Tetrahydropapaverine, one of the TIQs and an analogue of salsolinol and tetrahydropapaveroline, has been reported to have neurotoxic effects on dopamine neurons.
  21. RAR agonist

    Tretinoin is an endogenous agonist for retinoic acid receptors with IC50 value of 14 nM for RAR-alpha, RAR-beta and RAR-gamma receptors).
  22. Procollagen C-proteinase inhibitor

    UK-383367 is a procollagen C-proteinase inhibitor with IC50 of 44 nM, has excellent selectivity over MMPs.
  23. PDE-5 Inhibitor

    Vardenafil is a PDE5 inhibitor used for treating erectile dysfunction.
  24. CYP17 inhibitor

    Voriconazole (Vfend) is a triazole antifungal agent that is available as a lyophilized powder for solution for intravenous infusion.
  25. 5-lipoxygenase inhibitor

    Zileuton is a potent and selective inhibitor of 5-lipoxygenase with antiasthmatic properties.
  26. CYP17A1 inhibitor

    TAK-700 (Orteronel) is an oral, non-steroidal androgen synthesis inhibitor that selectively inhibits the 17,20 lyase enzyme.
  27. CYP17 inhibitor

    Abiraterone acetate (CB7630) is an orally active acetate ester of the steroidal compound Abiraterone with antiandrogen activity. Abiraterone inhibits 17 α-hydroxylase/C17,20 lyase (CYP17A1).
  28. PDE Inhibitor

    GSK256066 is an exceptionally high affinity and selective inhibitor of PDE4 that inhibits PDE4 isoforms A-D with equal affinity and has a high HARBS (High-Affinity Rolipram Binding Site) ratio (>17).
  29. CETP inhibitor

    Anacetrapib (MK-0859) is a CETP inhibitor being developed to treat hypercholesterolemia (elevated cholesterol levels) and prevent cardiovascular disease.
  30. Retinoid X Receptor Ligand

    Bexarotene is a highly selective retinoid X receptor (RXR) agonist.
  31. Monoacylglycerol lipase inhibitor

    URB754 was originally reported to be a potent, noncompetitive inhibitor of monoacylglycerol lipase.
  32. MAO B inhibitor

    Rasagiline is a selective irreversible inhibitor of MAO-B (monoamine oxidase-B).
  33. Phoenixin-20 (PNX-20) is a bioactive peptide with hormone-like actions in vertebrates, and can stimulates hypothalamo-pituitary-gonadal hormones and regulate reproductive processes in mammals. Phoenixin-20 promotes neuronal mitochondrial biogenesis via CREB-PGC-1α pathway. Phoenixin-20 has anxiolytic effect.
  34. Rimtoregtide is a polypeptide compound which significantly reduces the increase in the levels of amylase and lipase in the blood caused by acute pancreatitis. Rimtoregtide has the potential for the research of pancreatitis and acute pancreatitis (extracted from patent WO2018205233A1).
  35. anti-inflammatory agent

    Delmitide (RDP58) acetate is an orally active d-isomer decapeptide with potent anti-inflammatory activity. Delmitide acetate inhibits production of TNF-α, IFN-γ, and interleukin (IL)-12, and up-regulates heme oxygenase 1 activity. Delmitide acetate can be used for the research of ulcerative colitis.
  36. Xenin is a 25-amino acid peptide initially isolated from human gastric mucosa. Xenin is a gut hormone that can reduce food intake.
  37. Meldonium is a cardioprotective agent. It inhibits γ-butyrobetaine hydroxylase (BBOX) and carnitine/organic cation transporter type 2 (OCTN2).

  38. PAI-1 inhibitor

    Angstrom6 (A6 Peptide) is an 8 amino-acid peptide derived from single-chain urokinase plasminogen activator (scuPA) and interferes with the uPA/uPAR cascade and abrogates downstream effects. Angstrom6 binds to CD44 resulting in the inhibition of migration, invasion, and metastasis of tumor cells, and the modulation of CD44-mediated cell signaling.
  39. N-Acetyloxytocin is isolated and characterized in the neurointermediate lobe of the rat pituitary (NIL) and their presence in several brain areas of the rat.
  40. γ-Glu-Gly, a γ-glutamyl dipeptide, is a human lipid metabolite.γ-Glu-Gly has a similar structure to GABA (γ-aminobutyric acid) and can act as an antagonist of excitatory amino acids.
  41. ACE inhibitor

    Bradykinin potentiator B (Bradykinin potentiating peptide B) is venom of Agkistrodon halys blomhoffi. Bradykinin potentiator B is a potent ACE inhibitor. Bradykinin potentiator inhibits the activity of bradykinin inhibitory peptidase.
  42. H-Tyr-Phe-OH (L-Tyrosyl-L-phenylalanine) is an orally active inhibitor of Angiotensin converting enzyme (ACE), with an inhibiton rate of 48% at 50 μM. H-Tyr-Phe-OH can be used as an biomarker for differentiating benign thyroid nodules (BTN) from thyroid cancer (TC). H-Tyr-Phe-OH exhibits xanthine oxidase inhibition (uric acid lowering) activity and serves as regulator in IL-8 production in neutrophil-like cells.
  43. Hsp70-derived octapeptide is a conserved octapeptide of the C-terminal end of Hsp70, which physically interacts with tetratricopeptide repeat (TPR) motifs.
  44. Ac-SVVVRT-NH2 is a PGC-1α modulator that modulates the activity of the human PGC-1α promoter (114%). Ac-SVVVRT-NH2 increases PGC-1α mRNA (125%) and accumulation of intracellular lipids (128%) in subcutaneous human adipocytes. Ac-SVVVRT-NH2 can be used in the research of diseases which is modulated by PGC-1α.
  45. L-LEUCINE-13C6, also known as 13C6-D-Leucine or L-Leucine-1,2,3,4,5,5'-13C6, is a fully 13C labelled D-Leucine. L-Leucine is an essential branched-chain amino acid (BCAA), which activates the mTOR signaling pathway.

  46. hCA II inhibitor

    EMAC10101d is a potent and selective inhibitor of Carbonic Anhydrase Isoform toward hCA II with an inhibitory activity in the low nanomolar range. Ki of 8.1 nM
  47. mGluR II agonist

    Xanthurenic acid is a putative endogenous Group II metabotropic glutamate receptor agonist, on sensory transmission in the thalamus.
  48. IDO1 inhibitor

    IDO-IN-13 is a potent indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an EC50 of 17 nM, extracted from patent WO2019040102A1, example 43.
  49. uPA inhibitor

    ZK824190 is an orally available and selective urokinase plasminogen activator (uPA) inhibitor as a potential treatment for multiple sclerosis. IC50s of 237, 1600 and 1850 nM for uPA, tPA, and Plasmin, respectively.
  50. PDE4 inhibitor

    Lotamilast (RVT-501; E6005) is a selective phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 2.8 nM.

Items 851-900 of 6503

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