GPCR/G Protein

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  1. A1 adenosine receptor agonist

    Tecadenoson (CVT-510) is a selective A1 adenosine receptor agonist.
  2. 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).
  3. 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).
  4. imidazoline receptor 1 agonist

    Moxonidine hydrochloride is a centrally acting antihypertensive agent.
  5. Adrenergic Receptor agonist

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

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

    Xylazine hydrochloride is an activator of α2A-AR, α2B-AR and α2C-AR.
  8. GPR40/FFA1 agonist

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

    ADL5747 is a selective, nonpeptidic δ opioid receptor agonist.
  10. 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.
  11. prostanoid DP-receptor (DP1) agonist

    BW 245C is a prostanoid DP-receptor (DP1) agonist, used to treat stroke.
  12. 5-HT2C agonist

    S 32212 hydrochloride is an inverse agonist of 5-HT2C receptors (pKi = 8.18 at human 5-HT2C INI receptors).
  13. 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).
  14. NTR1 agonist

    ML-314 is a brain penetrant nonpeptidic β-arrestin biased ggonist of the neurotensin NTR1 receptor, which exhibits full agonist behavior against NTR1 (EC50 = 2.0 μM) in the primary assay and selectivity against NTR2.
  15. 2A-AR adrenergic agonist

    Guanabenz acetate is an a2A-AR adrenergic agonist and IGRS (imidazoline I2 binding site) selective ligand.
  16. EDG-1 (S1P1) agonist

    CYM 5442 HCl is a potent and selective EDG-1 (S1P1) agonist in vitro (EC50 = 1.35 nM).
  17. histamine H3 receptor agonist

    Immethridine hydrobromide is a strong and highly selective histamine H3 receptor agonist (pEC50 = 9.74) that displays 300-fold selectivity over the H4 receptor (pKi values are 9.07 and 6.61 respectively).
  18. β3 adrenergic agonist

    CL 316243 disodium salt, a beta-3 adrenergic agonist, was developed as an anti-obesity and diabetes drug, and causes rapid decreases in blood glucose levels in mice.
  19. β3-adrenergic receptors agonist

    BRL-37344 is a b3-AR (b 3-adrenoceptor) selective agonist with lipolytic activity.
  20. opioid receptors agonist

    DPI-3290 (Org 41793) is a potent and specific opioid receptors agonist with Ki values of 0.18 nM, 0.46 nM, and 0.62 nM for δ-, μ-, and κ-opioid receptors, respectively.
  21. dopamine D2 receptor agonist

    Bromocriptine mesylate is a potent dopamine receptor agonist that binds the D2 receptor with highest affinity (Ki = 2.5 nM).1,2 As a result, it has found applications in combination therapy for Parkinsonism.
  22. GPR119 agonist

    AR-231453 is a potent and selective small molecule agonis of GPR119 that enhances glucose dependent insulin secretion and glucagon like peptide-1 (GLP-1) release.
  23. TGR5(GPCR19) agonist

    TGR5 Receptor Agonist is a potent TGR5(GPCR19) agonist, showed improved potency in the U2-OS cell assay (pEC50 = 6.8) and in melanophore cells (pEC50 = 7.5).
  24. adrenergic alpha-2 receptor agonist

    Medetomidine Hydrochloride is an adrenergic alpha-2 receptor agonist, which is used in veterinary medicine for its analgesic and sedative properties.
  25. GLP-1 receptor agonist

    BETP is a selective positive allosteric modulator and partial agonist of the glucagon-like peptide 1 (GLP-1) receptor.
  26. 5-HT1A/1B and 5-HT2C agonist

    RU 24969 succinate is a potent 5-HT1A/1B and moderate 5-HT2C agonist that may also release 5-HT.

  27. Dopamine receptor agonist

    Cabergoline, a lysergic acid amide derivative, is a potent dopamine D2 receptor agonist.
  28. 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).
  29. 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.
  30. GLP-1 receptor agonist

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

    Capadenoson is a selective agonist of adenosine-A1 receptor.
  32. 5-HT6 agonist

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

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

    U-69593 is a potent, selective κ1-opioid receptor agonist (EC50 = 80-109 nM). Active in vivo. Antinociceptive.
  35. 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.
  36. β2-adrenoceptor agonist

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

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

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

    (+)-PD 128907 hydrochloride is a potent D3DR (dopamine receptor) agonist (Ki = 2.3 nM).
  40. 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.
  41. 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.
  42. 5-HT1F receptor agonist

    LY 344864 racemate is a 5-HT1F receptor agonist.
  43. 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.
  44. 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.
  45. 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.
  46. Rev-Erbα agonist

    GSK4112 is a selective Rev-Erbα agonist with EC50 value of 250 nM.
  47. 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)
  48. histamine H3 receptors agonist

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

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

    Tasimelteon is a melatonin MT1 and MT2 receptor agonist.

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