GPCR/G Protein

Items 351-400 of 6977

Page
per page
Set Descending Direction
Catalog No.
Product Name
Application
Product Information
Citations
  1. mGlu4 receptor modulator

    Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an IC50 of 500 nM for human mGlu4.
  2. lysophaphatidic acid 1 (LPA1/Edg-2) receptor inhibitor

    SAR-100842 is a lysophaphatidic acid 1 (LPA1/Edg-2) receptor inhibitor.
  3. NPY Y2 receptor antagonist

    BIIE 0246 is a potent, selective and competitive non-peptide antagonist for the neuropeptide Y Y2 receptor (IC50 = 15 nM).
  4. PAR4 antagonist

    BMS-986120 is a first-in-class oral and reversible protease-activated receptor 4 (PAR4) antagonist, with IC50s of 9.5 nM and 2.1 nM in human and monkey blood, respectively.
  5. 5-HT/dopamine D2 antagonist

    Ocaperidone is an effective antipsychotic agent.
  6. FFAR1/GPR40 agonist

    LY2922470 is a potent, selective and orally available agonist of the G protein-coupled receptor 40 (GPR40), with EC50s of 7 nM, 1 nM and 3 nM for human GPR40, mouse GPR40 and rat GPR40, respectively.

  7. A3 adenosine receptor agonist

    AB-MECA is a high affinity A3 adenosine receptor agonist, has high affinity for recombinant A1 and A3 receptors.
  8. LTB4 receptor antagonist

    DW-1350 is a LTB4 receptor antagonist.
  9. PAF antagonist

    Aglafoline is an effective PAF antagonist not only in vitro, but also in vivo.
  10. 5-HT2c receptor agonist

    PRX933 hydrochloride is a 5-HT2c receptor agonist extracted from patent WO 2014140631 A1.
  11. S1P3 receptor antagonist

    TY-52156 is a potent and selective S1P3 receptor antagonist with a Ki value of 110 nM.
  12. 5-HT4 receptor antagonist

    5-HT4 antagonist 1 is a 5-HT4 receptor antagonist with a pKi of 9.6.
  13. 5-HT2A receptor antagonist

    Lumateperone Tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a SERT blocker (Ki = 61 nM).
  14. human 5-HT1A receptor agonist

    AP521 is an agonist of human 5-HT1A receptor with an IC50 of 94 nM.
  15. MCH-1 antagonist

    MCH-1 antagonist 1 is a potent melanin concentrating hormone (MCH-1) antagonist with a Ki of 2.6 nM. MCH-1 antagonist 1 also inhibits CYP3A4 with an IC50 of 10 μM.
  16. 5-HT2C receptor agonist

    YM348 is a potent and orally active 5-HT2C receptor agonist, which shows a high affinity for cloned human 5-HT2C receptor (Ki: 0.89 nM).
  17. PAF receptor antagonist

    Foropafant (SR27417) highly potent, competitive, selective and orally active antagonist of platelet-activating factor (PAF) receptor.
  18. Adrenoceptors antagonist

    BRL 44408 maleate is a high purity Adrenoceptors antagonist. It increases hippocampal noradrenalin release following systemic administration.
  19. β-adrenergic receptors agonist

    Cimaterol is a potent agonist of β-adrenergic receptors (pEC50 = 8.13, 8.78, and 6.62 for human β1, β2, and β3, respectively).
  20. Bisoprolol is a cardioselective β1-adrenergic blocking agent used for secondary prevention of myocardial infarction (MI), heart failure, angina pectoris and mild to moderate hypertension.
  21. Adrenergic α1 Receptor Antagonist

    HEAT hydrochloride is a very selective α1-AR adrenoceptor antagonist, precursor of the 3-[125I]-derivative. Adrenoreceptors (AR) or adrenergic receptors are G-protein coupled receptors involved in a variety of sympathetic nervous system processes.
  22. α2- adrenoceptor antagonist / I2 imidazoline receptor agonist

    Idazoxan hydrochloride is an α2-AR adrenoceptor antagonist and potential I2 imidazoline receptor agonist. Also displays I1 imidazoline receptor antagonist activity. (pKi values are 5.90, 7.22, 8.01, 7.43, and 7.7 for I1, I2, α 2A, α2B, and α 2C receptors respectively).
  23. imidazoline receptor 1 agonist

    Moxonidine hydrochloride is a centrally acting antihypertensive agent.
  24. 5-HT1A receptor antagonist

    NAN-190 is a drug and research chemical widely used in scientific studies. It was previously believed to act as a selective 5-HT1A receptor antagonist, but a subsequent discovery showed that it also potently blocks the α2-adrenergic receptor.
  25. Octopamine hydrochloride is an invertebrate biogenic amine neurotransmitter, related to noradrenalin, that is an adrenoceptor agonist.
  26. α-Adrenergic blocker

    Phentolamine Hydrochloride is an AR (α-Adrenergic) blocker.
  27. Beta adrenergic receptor blocker

    Pindolol is a nonselective beta blocker with partial beta-adrenergic receptor agonist activity.
  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. α2-adrenergic receptor antagonist

    Rauwolscine is a natural alkaloid that acts as a selective and reversible α2-adrenergic receptor antagonist (Ki = 12 nM).
  30. Adrenoceptors antagonist

    S-(-)-Atenolol is the active enantiomer of atenolol that is a cardioselective β-adrenergic blocker.
  31. Adrenoceptors antagonist

    (S)-Timolol maleate is a adrenergic receptor antagonist selective for β1-AR.
  32. Adrenoceptors antagonist

    SR 59230A hydrochloride is a β3-adrenoceptor antagonist.
  33. Adrenergic Receptor agonist

    Tulobuterol is a beta-adrenergic receptor agonist that is related structurally to Terbutaline.
  34. Adrenoceptors agonist

    UK 14,304 tartrate is a water-soluble form UK 14,304. It is a full α2 adrenergic agonist.
  35. Adrenergic Receptor agonist

    Xylazine hydrochloride is an activator of α2A-AR, α2B-AR and α2C-AR.
  36. Histamine H4 receptor antagonist

    A 943931 2HCl is a potent and selective histamine H4 receptor antagonist (pKi values are 7.15 and 8.12 at human and rat receptors respectively).
  37. Somatostatin is an endogenous peptide noted to inhibit the release of growth hormone, insulin and glucagon.
  38. 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).
  39. GPR40/FFA1 agonist

    AMG-837 calcium hydrate is a potent, orally bioavailable GPR40 agonist.
  40. δ opioid receptor agonist

    ADL5747 is a selective, nonpeptidic δ opioid receptor agonist.
  41. Kainate receptor agonist

    Kainate class of ionotropic glutamate receptor agonist. Has been shown to induce seizures and neurodegeneration in vivo and has also been used to induce experimental epilepsy in rodents and to examine excitation-induced neuronal apoptosis mechanisms.
  42. Bombesin is a neuropeptide with many biological effects including hormone release, stimulation of pancreatic enzyme secretion, inhibition of gastric emptying and modulation of gastric acid secretion.
  43. prostanoid DP-receptor (DP1) agonist

    BW 245C is a prostanoid DP-receptor (DP1) agonist, used to treat stroke.
  44. 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).
  45. prostaglandin F2α analog

    Cloprostenol is a synthetic analog of prostaglandin F2α (PGF2α). It is 200 times and 100 times more potent than PGF2α in terminating pregnancy in hamsters and rats, respectively, without the side effects associated with PGF2α.
  46. ETA/ETB antagonist

    PD-159020 is a non-selective ETA/ETB antagonist, with IC50s of 30 and 50 nM for hETA and hETB, respectively.
  47. 5-HT2C agonist

    S 32212 hydrochloride is an inverse agonist of 5-HT2C receptors (pKi = 8.18 at human 5-HT2C INI receptors).
  48. Adenosine A2A receptor antagonist

    Preladenant is a potent and selective antagonist at the adenosine A2A receptor.
  49. Sigma2 antagonist

    UMB24 is a putative sigma2-preferring antagonist.
  50. D2 dopamine partial agonist

    Brexpiprazole is a novel D2 dopamine partial agonist investigational product currently in clinical trials for the treatment of depression, schizophrenia, and attention deficit hyperactivity disorder (ADHD).

Items 351-400 of 6977

Page
per page
Set Descending Direction