GPCR/G Protein

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Catalog No.
Product Name
Application
Product Information
Product Citation
  1. REV-ERBα/β agonist

    SR9011 is the agonist for REV-ERB-α with IC50 of 670 nM and REV-ERB-β with IC50 of 800 nM.
  2. CB1/CB2 receptor agonist

    Bay 59-3074 is a novel, selective CB1/CB2 receptor partial agonist with Ki values of 48.3 and 45.5 nM at human CB1 and CB2 receptors respectively .
  3. 5-HT1A receptor agonist/serotonin reuptake inhibitor

    YL0919, a novel antidepressant candidate with dual activity as a 5-HT1A receptor agonist and a selective serotonin reuptake inhibitor,the IC50 values of YL-0919 inhibiting the uptake of 5-HT into rat cerebral cortical synaptosomes and human recombinant cells were 1.78??0.34 nM and 1.93??0.18 nM respectively.
  4. CXCR4 agonist

    ATI-2341, pepducin targeting the C-X-C chemokine receptor type 4 (CXCR4) (EC50 = 194 nM, is an allosteric agonist activating the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization.
  5. CB2 receptor agonist

    AM1241 is a selective cannabinoid CB2 receptor agonist with Ki of 3.4 nM, exhibits 82-fold selectivity over CB1 receptor.
  6. Adenosine A2 receptor agonist

    CGS 21680 HCl is an adenosine A2 receptor agonist with IC50 of 22 nM, exhibits 140-fold over A1 receptor.
  7. β2-adrenergic receptor agonist

    Clorprenaline HCl is a β2-receptor agonist, it has a significant expansion of the bronchial effect.
  8. GPR35/CXCR8 agonist

    Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8.
  9. β-adrenoceptor agonist

    Indacaterol (QAB149) maleate is an ultra-long-acting β-adrenoceptor agonist.
  10. β3-AR agonist

    L755507 is a potent, selective agonist of β3-AR with an IC50 of 35 nM.
  11. GLP-1 agonist

    Albiglutide is a glucagon-like peptide-1 agonist (GLP-1 agonist).
  12. adenosine A2B receptor agonist

    MRS1706 is a selective adenosine A2B receptor inverse agonist with Ki values of 1.39, 157, 112, and 230 nM for human A2B, A1, A2A, and A3 receptors, respectively.
  13. Endogenous galanin receptor agonist

    Galanin (1-30) (human) is an endogenous peptide with multiple endocrine, metabolic and behavioral effects
  14. 5-HT7 receptor agonist

    LP-211 is a a selective agonist of the serotonin 5-HT7 receptor with a Ki value of 0.58 nM at rat cloned 5-HT7 receptors, and >300-fold selectivity over the 5-HT1A receptor.
  15. MOR agonist

    SR17018 is an mu-opioid-receptor (MOR) agonist with an EC50 of 97 nM.
  16. KOR agonist

    Asimadoline is a potent κ-opioid receptor (KOR) agonist (IC50s = 5.6 and 1.2 nM for guinea pig and human receptors, respectively).
  17. NK3 receptor agonist

    Senktide is a potent, selective agonist of the neuromedin K3 (NK3) receptor (EC50 = 0.5-3 nM).
  18. Adenosine receptor agonist

    NECA is a high-affinity adenosine receptor agonist (Ki values are 6.2, 14, and 20 nM for human A3, A1 and A2A receptors respectively; EC50 = 2.4 μM for human A2B).
  19. GLP-1 receptor agonist

    Dulaglutide is a glucagon-like peptide-1 (GLP-1) receptor agonist.
  20. CaSR agonist

    Evocalcet is a calcium-sensing receptor agonist. The calcium-sensing receptor (CaSR) is a Class C G-protein coupled receptor which senses extracellular levels of calcium ion.
  21. 5-HT1F receptor agonist

    LY 344864 racemate is a 5-HT1F receptor agonist.
  22. 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.
  23. 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.
  24. 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.
  25. Rev-Erbα agonist

    GSK4112 is a selective Rev-Erbα agonist with EC50 value of 250 nM.
  26. 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)
  27. histamine H3 receptors agonist

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

    Xylometazoline hydrochloride is an α-adrenoceptor agonist commonly used as nasal decongestant.
  29. 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.
  30. MT1 and MT2 receptor agonist

    Tasimelteon is a melatonin MT1 and MT2 receptor agonist.
  31. 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.
  32. alpha-1 adrenergic agonist

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

    Ractopamine HCl is a beta-Adrenergic agonist. It acts by being a full agonist at the TAAR1.
  34. 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.
  35. 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.
  36. 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.
  37. 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.
  38. α2-adrenergic receptor agonist

    Brimonidine (UK 14304) is a full α2-adrenergic receptor (α2-AR) agonist.
  39. 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.
  40. dopamine D2 receptor agonist

    Quinagolide hydrochloride is a selective dopamine D2 receptor agonist, also is a prolactin inhibitor.
  41. 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.
  42. 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.
  43. 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.
  44. β2-adrenergic receptor agonist

    Tulobuterol Hydrochloride is a long-acting beta2-adrenergic receptor agonist.
  45. 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).
  46. selective IP receptor agonist

    MRE-269 is an active metabolite of selexipag, and acts as a selective IP receptor agonist.
  47. 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.
  48. 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.
  49. 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.
  50. 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.

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