GPCR/G Protein

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  1. adenylyl cyclase inhibitor

    SQ22536 is an inhibitor of adenylyl cyclase with an IC50 of 1.4 uM. It can inhibit PGE1-stimulated increases in cAMP levels in intact human platelets.
  2. DAT and SLC6A2 inhibitor

    GBR-12935 is a piperazine derivative which is a potent and selective dopamine reuptake inhibitor.
  3. dopamine re-uptake inhibitor

    Vanoxerine (GBR-12909) is a piperazine derivative which is a potent and selective DRI.
  4. human A3 adenosine receptor antagonist /Aurora inhibitor

    Reversine is a potent human A3 adenosine receptor antagonist with Ki of 0.66 μM, and a pan-aurora A/B/C kinase inhibitor with IC50 of 12 nM/13 nM/20 nM, respectively. Also used for stem cell dedifferentiation.
  5. DPP-4 Inhibitor

    Linagliptin is a DPP-4 inhibitor, an enzyme that degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP).
  6. Androgen Receptor inhibitor

    ARN-509 is an androgen receptor antagonist with potential antineoplastic activity. ARN-509 binds to AR in target tissues thereby preventing androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot be translocated to the nucleus. This prevents binding to and transcription of AR-responsive genes.
  7. peptide Oxytocin Receptor Inhibitor

    Atosiban is a peptide Oxytocin Receptor Inhibitor.
  8. Adenosine kinase inhibitor

    5-Iodotubercidin is a potent adenosine kinase inhibitor with IC50 of 26 nM.
  9. CXCL8/CXCR1/2 Inhibitor

    Reparixin is a potent inhibitor of both CXCL8 receptors CXCR1/2, it inhibits weakly CXCR2-mediated cell migration (IC50=100 nM), whereas it strongly blocks CXCR1-mediated chemotaxis (IC50=1 nM).
  10. Serotonin reuptake inhibitor

    Escitalopram oxalate ((S)-(+)Citalopram oxalate) is a selective serotonin reuptake inhibitor (SSRI) with Ki of 0.89 nM.
  11. S1P inhibitor

    PF429242 dihydrochloride is a reversible and competitive S1P inhibitor with an IC50 of 175 nM.
  12. GluR inhibitor

    (-)-Huperzine A is a naturally occurring sesquiterpene alkaloid compound found in the firmoss Huperzia serrata.
  13. Smoothened inhibitor

    BMS-833923 (or XL-139) is an orally bioavailable small-molecule SMO (Smoothened) inhibitor with potential antineoplastic activity.
  14. PAFR inhibitor/H1 receptor inhibitor

    Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 and 102 nM, respectively.
  15. dopamine release inhibitor

    Pentiapine is a novel dopamine release inhibitor.
  16. Adenylyl cyclase inhibitor

    LRE1 is a specific and allosteric inhibitor of soluble adenylyl cyclase.
  17. CXCR4 Inhibitor

    MSX-122 is an orally bioavailable inhibitor of CXCR4 (IC50 = ~10 nM) with potential antineoplastic and antiviral activities. CXCR4 inhibitor MSX-122 binds to the chemokine receptor CXCR4, preventing the binding of stromal derived factor-1 (SDF-1) to the CXCR4 receptor and receptor activation, which may result in decreased tumor cell proliferation and migration.
  18. SphK2 inhibitor

    ABC294640 is an orally available, aryladamantane compound and selective inhibitor of sphingosine kinase-2 (SK2) with potential antineoplastic activity.
  19. Adenosine receptor inhibitor

    N-[(4-Aminophenyl)methyl]adenosine is a adenosine receptor inhibitor, with Ki of 29 nM for Rat ecto-5??-Nucleotidase. IC50 value: 29.0 ± 1.7 nM (Ki) Target: Adenosine Receptor
  20. Smoothened Inhibitor

    LDE225 is an orally bioavailable small-molecule Smoothened (Smo) antagonist with potential antineoplastic activity.
  21. Smoothened Inhibitor

    PF-5274857 is a novel Smo antagonist that specifically binds to Smo with a K(i) of 4.6 ?? 1.1 nmol/L and completely blocks the transcriptional activity of the downstream gene Gli1 with an IC(50) of 2.7 ?? 1.4 nmol/L in cells.
  22. S1PR1/S1PR5 inhibitor

    BAF312 is a next-generation potent sphingosine 1-phosphate (S1P) receptor agonist, selective for S1P1 and S1P5.
  23. PDE inhibitor

    Forskolin is a cell-permeable diterpenoid that possesses anti-hypertensive, positive inotropic, and adenylyl cyclase activating properties.
  24. Smo inhibitor

    Saridegib is a potent and specific inhibitor of Smoothened (Smo), a key signaling transmembrane protein in the Hedgehog (Hh) pathway.
  25. dopamine uptake inhibitor

    GBR 12783 dihydrochloride is a very potent and selective inhibitor of dopamine uptake (IC50 for inhibition of [3H]-dopamine uptake in rat striatal synaptosomes is 1.8 nM).
  26. S1PR1 inhibitor

    KRP-203 is a selective Sphingosine-1-phosphate receptor agonist. It shows to reduce peripheral lymphocyte infiltration and to prolong survival in rat transplant models.
  27. leukotriene biosynthesis inhibitor

    MK-886 is an inhibitor of leukotriene biosynthesis (IC50 = 3 nM in human polymorphonuclear leukocytes).
  28. norepinephrine (NE) transporter inhibitor

    Atomoxetine hydrochloride is a competitive and specific inhibitor of SLC6A2 while demonstrating weak ST and DAT inhibition as studied in synaptosomes of rat hypothalamus.
  29. serotonin uptake inhibitor

    Norfluoxetine is an active metabolite of the antidepressant fluoxetine that inhibits serotonin uptake with a pKi value of 7.35.1 The S-enantiomer of norfluoxetine has 20-times higher serotonin reuptake blocking potency than the R-enantiomer (pKis = 7.86 versus 6.51, respectively).
  30. PAR1 inhibitor

    ML-161 is an inhibitor of protease-activated receptor 1 (PAR1)-mediated platelet activation (IC50 = 0.26 μM for the inhibition of platelet P-selectin expression on human platelets).
  31. Adenylyl Cyclase Inhibitor

    NKY 80 is an inhibitor of adenylyl cyclase (AC). Exhibits greater affinity for AC5 over AC3 and AC2 (IC50 values are 8.3 μM, 132 μM and 1.7 mM respectively).
  32. human 5'-methylthioadenosine phosphorylase inhibitor

    MT-DADMe-ImmA is an inhibitor of human 5'-methylthioadenosine phosphorylase (MTAP) with a Ki of 90 pM.
  33. dopamine β-hydroxylase (DBH) inhibitor

    Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor that could cross the blood-brain barrier (BBB) and cause central as well as peripheral effects.
  34. norepinephrine reuptake inhibitor

    Edivoxetine HCl is a drug which acts as a selective norepinephrine reuptake inhibitor
  35. Smoothened inhibitor

    PF-04449913 is a potent and orally bioavailable inhibitor of smoothened.
  36. Syk inhibitor

    R112 is a Syk inhibitor. R112 inhibited degranulation induced by anti-IgE cross-linking in mast cells and also blocked leukotriene C4 production and all proinflammatory cytokines tested.
  37. angiotensin receptor-neprilysin inhibitor

    LCZ696 is an orally bioavailable, dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) for hypertension and heart failure.
  38. EPAC1/EPAC2 inhibitor

    ESI-09 is a specific exchange protein directly activated by cAMP (EPAC) inhibitor with IC50 of 3.2 uM and 1.4 uM for EPAC1 and EPAC2,
  39. EPAC2 inhibitor

    HJC0350 is a potent and selective EPAC2 inhibitor with IC50 of 0.3 μM, exhibiting no inhibition on Epac1.
  40. serotonin/NE reuptake inhibitor

    Levomilnacipran HCl is a selective serotonin and norepinephrine reuptake inhibitor.
  41. alpha-adrenergic receptor agonist / MAO inhibitor

    Amitraz, also known as Mitaban and Taktic, is an alpha-adrenergic receptor agonist and MAO inhibitor used as an insecticide in prevention of flea and tick infections. It prevents prostaglandin synthesis and may inhibit beta-cell insulin release.
  42. D2DR and D4DR inhibitor

    Loxapine Succinate is a D2DR and D4DR inhibitor and serotonergic receptor antagonist. Loxapine succinate is an antipsychotic agent used in schizophrenia.
  43. Prostaglandin Receptor inhibitor

    Benorilate, also known as Win-11450, is an ester of aspirin and paracetamol with analgesic, antipyretic, and anti-inflammatory activity used in the treatment of rheumatoid diseases. Benorilate has less severe side effects than aspirin.
  44. Prostaglandin Receptor inhibitor

    Dinoprost Tromethamine, also known as Dinoprost Trometamol, is a naturally occurring prostaglandin used in medicine to induce labor and as an abortifacient.
  45. serotonin uptake inhibitor

    Paroxetine Mesylate is a serotonin uptake inhibitor that is effective in the treatment of depression.
  46. 5-HT2 receptors inhibitor

    Nefazodone HCl is an inhibitor of 5-HT2 receptors, SERT, NET, and hERG K+ channels used to treat mood disorders. It decreases immobility time in the forced swim test.
  47. D2DR inhibitor

    Promazine Hydrochloride is a phenothiazine compound and D2DR inhibitor. Promazine Hydrochloride has been employed in studies investigating dopamine-stimulated glycosylation of brain proteins in vitro. It has actions similar to chlorpromazine but with less antipsychotic activity.
  48. MAO inhibitor

    Molindone HCl is a D2 dopamine receptor antagonist. It also acts as a MAO inhibitor.
  49. adrenergic receptor inhibitor

    Asenapine(Org 5222) inhibits adrenergic receptor (α1, α2A, α2B, α2C) with Ki of 0.25-1.2 nM and also inhibits 5-HT receptor (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) with Ki of 0.03-4.0 nM.
  50. D2DR/D4DR inhibitor

    Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.

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