GPCR/G Protein

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Citations
  1. prostacyclin receptor agonist

    NS-304 is a selective prostacyclin IP1 receptor agonist (Ki values are 260 and 2100 nM and for human and rat IP receptors, and >10 μM for EP1-4, DP, FP, and TP receptors).
  2. NMDA& mGlu receptor agonist

    Ibotenic acid is a neuroexcitatory amino acid originally isolated from Amanita species that functions as a NMDA and metabotropic glutamate receptor agonist.
  3. GLP-1 receptor agonist

    ixisenatide inhibit glucagon release, markedly reduce postprandial glucago. have a promoting effct in diabetes mellitus (T2DM).
  4. Adenosine Receptor agonist

    Capadenoson is a selective agonist of adenosine-A1 receptor.
  5. 5-HT6 agonist

    WAY 181187 is a high affinity and selective 5-HT6 agonist with Ki value of 2.2 nM.
  6. dopaminergic agonist

    Pergolide mesylate is a dopaminergic agonist that also decrease plasma prolactin concentrations.
  7. κ1-opioid receptor agonist

    U-69593 is a potent, selective κ1-opioid receptor agonist (EC50 = 80-109 nM). Active in vivo. Antinociceptive.
  8. CB2 receptor agonist

    Tedalinab (GRC-10693) is a drug developed for the treatment of osteoarthritis and neuropathic pain, which acts as a potent and selective cannabinoid CB2 receptor agonist. It has a very high selectivity of 4700x for CB2 over the related CB1 receptor, has good oral bioavailability and has shown promising safety results and effective analgesic and antiinflammatory actions in early clinical trials.
  9. β2-adrenoceptor agonist

    Salmeterol Xinafoate is a long-acting β2-adrenergic receptor agonist with anti-inflammatory effect.
  10. β-adrenoceptor agonist

    Bambuterol HCl is a potent β-adrenoceptor agonist, used in the treatment of asthma.
  11. I(1) imidazoline receptor agonist

    Rilmenidine Phosphate is a selective I(1) imidazoline receptor agonist.
  12. Dopamine receptor agonist

    (+)-PD 128907 hydrochloride is a potent D3DR (dopamine receptor) agonist (Ki = 2.3 nM).
  13. 5-HT2A receptor agonist

    Pimavanserin is a potent and selective 5-HT2A receptor inverse agonist with mean pIC50 of with 8.7 in the cell-based functional assay.
  14. FFA4/GPR120 agonist

    GSK137647A is a selective FFA4 agonist, with pEC50 of 6.3, 6.2, and 6.1 for human, Mouse and Rat FFA4, respectively.
  15. 5-HT1F receptor agonist

    LY 344864 racemate is a 5-HT1F receptor agonist.
  16. CNS penetrant mGlu7/8 receptor agonist

    VU6005649 is a CNS penetrant mGlu7/8 receptor agonist with EC50s of 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively.
  17. GPR39 agonist

    TM N1324 is an agonist of G-Protein-Coupled Receptor 39 (GPR39) with EC50s of 9 nM/5 nM in the presence of Zn2+, and 280 nM/180 nM in the absence of Zn2+ for human/murine GPR39.
  18. 5-HT(2A) receptor agonist

    Temanogrel, also known as APD791, is a highly selective 5-hydroxytryptamine2A receptor inverse agonist under development for the treatment of arterial thrombosis.
  19. Rev-Erbα agonist

    GSK4112 is a selective Rev-Erbα agonist with EC50 value of 250 nM.
  20. sigma1 receptor agonist

    Anavex2-73 is a muscarinic/moderate sigma1 receptor agonist that alleviated the scopolamine- and dizocilpine-induced learning impairments. CAS: 195615-83-9 (Free base) 195615-84-0 (HCl)
  21. histamine H3 receptors agonist

    S38093 is an inverse agonist at histamine H3 receptors. CAS: 862896-30-8 (Free base) 1222097-72-4 (HCl)
  22. α-adrenoceptor agonist

    Xylometazoline hydrochloride is an α-adrenoceptor agonist commonly used as nasal decongestant.
  23. MT1 and MT2 receptor agonist

    Tasimelteon is a melatonin MT1 and MT2 receptor agonist.
  24. β2AR agonist

    Metaproterenol hemisulfate (Orciprenaline hemisulfate) is a direct-acting sympathomimetic and a β2-adrenergic receptor (β2AR) agonist with an IC50 of 68 nM. Metaproterenol hemisulfate also has anti-inflammatory activity.
  25. alpha-1 adrenergic agonist

    Methoxamine Hydrochloride is an alpha-1 adrenergic agonist that causes prolonged peripheral vasoconstriction.
  26. beta-Adrenergic agonist

    Ractopamine HCl is a beta-Adrenergic agonist. It acts by being a full agonist at the TAAR1.
  27. Adrenergic alpha-1 agonist

    Midodrine hydrochloride is an ethanolamine derivative that is an adrenergic alpha-1 agonist. It is used as a vasoconstrictor agent in the treatment of hypotension. It improves clinical outcome of chronic hypotension.
  28. adrenergic alpha-1 agonist

    Midodrine is an ethanolamine derivative that is an adrenergic alpha-1 agonist. It is used as a vasoconstrictor agent in the treatment of HYPOTENSION.
  29. Serotonin receptors agonist

    Dihydroergotamine Mesylate, also known as DHE or Migranal, is an ergot alkaloid used to treat migraines. It has similar actions to the triptans, acting as an agonist to the serotonin receptors and causing vasoconstriction of the intracranial blood vessels, but also interacts centrally with dopamine and adrenergic receptors.
  30. Beta 2 adrenergic agonist

    Fenoterol is a Beta 2 adrenergic agonist designed to open up the airways to the lungs. It is classed as sympathomimetic beta agonist and asthma medication.
  31. α2-adrenergic receptor agonist

    Brimonidine (UK 14304) is a full α2-adrenergic receptor (α2-AR) agonist.
  32. beta-adrenergic agonist

    Nylidrin hydrochloride is a beta-adrenergic agonist. Nylidrin hydrochloride is shown to be an effective inhibitor of IgE-mediated release of histamine from human basophils, and thus can be used as antiallergic agent.
  33. dopamine D2 receptor agonist

    Quinagolide hydrochloride is a selective dopamine D2 receptor agonist, also is a prolactin inhibitor.
  34. peripheral oxytocin receptors agonist

    Carbetocin (Lonactene; Duratocin) is an obstetric drug used to control postpartum hemorrhage and bleeding after giving birth; an agonist at peripheral oxytocin receptors.
  35. μ- opioid receptor agonist

    Trimebutine Maleate is a drug with antimuscarinic and weak mu opioid agonist effects. Trimebutine Maleate modulates the calcium and potassium channels, relieves abdominal pain in patients with irritable bowel syndrome.
  36. α2-receptor agonist

    Lofexidine is a selective α2-receptor agonist, commonly used to alleviate the physical symptoms of heroin and other types of opioid withdrawal.
  37. β2-adrenergic receptor agonist

    Tulobuterol Hydrochloride is a long-acting beta2-adrenergic receptor agonist.
  38. Somatostatin Receptor agonist

    Pasireotide(SOM 230) is a stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9 respectively).
  39. selective IP receptor agonist

    MRE-269 is an active metabolite of selexipag, and acts as a selective IP receptor agonist.
  40. FFA4/GPR120 agonist

    TUG-891 is a potent and selective agonist of the free fatty acid receptor 4 (FFA4/GPR120), which demonstrates both potential opportunity and possible challenges to therapeutic agonism.
  41. 5-HT1A receptor agonist

    Eptapirone is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential. The affinity of F 11440 for 5-HT1A binding sites (pKi, 8.33) was higher than that of buspirone (pKi, 7.50), and somewhat lower than that of flesinoxan (pKi, 8.91). In vivo, F 11440 was 4- to 20-fold more potent than flesinoxan, and 30- to 60-fold more potent than buspirone.
  42. EP4 agonist

    KAG-308, a newly-identified EP4-selective agonist shows efficacy for treating ulcerative colitis and can bring about lower risk of colorectal carcinogenesis by oral administration.
  43. S1P agonist

    ASP1126 is a selective and orally active sphingosine-1-phosphate (S1P) agonist, with EC50 values of 7.12 nM, 517 nM for hS1P1 and hS1P3, respectively.
  44. mGluR agonist

    L-Cysteinesulfinic acid is a potent agonist at several rat metabotropic glutamate receptors (mGluRs) with pEC50s of 3.92±0.03, 4.6±0.2, 3.9±0.2, 2.7±0.2, 4.0±0.2, and 3.94±0.08 for mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, respectively.
  45. μ opioid receptor agonist

    PZM21 is a potent and selective μ opioid receptor agonist with an EC50 of 1.8 nM.
  46. EP2 receptor agonist

    Taprenepag isopropyl is a highly selective EP2 receptor agonist.
  47. mGluR5 agonist

    CHPG is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells.
  48. 5-HT3 partial agonist

    Pumosetrag Hydrochloride (MKC-733; DDP-733) is an orally available 5-HT3 partial agonist developed for the treatment of irritable bowel syndrome and gastroesophageal reflux disease.
  49. dual FPR1/FPR2/ALX agonist

    FPR Agonist 43 (compound 43) is a dual formyl peptide receptor 1 (FPR1) and formyl peptide receptor 2 (FPR2)/ALX agonist.
  50. adenosine A1 receptor agonist

    GR79236 is a highly potent and selective adenosine A1 receptor agonist (Ki = 3.1 nM) that has analgesic and anti-inflammatory actions in humans and animals.

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