GPCR/G Protein

Items 201-250 of 1393

per page
Set Descending Direction
Catalog No.
Product Name
Application
Product Information
Product Citation
  1. 5-HT1A receptor agonist

    Aripiprazole is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM.
  2. adrenergic agonist

    Adrenalone is an adrenergic agonist used as a topical vasoconstrictor and hemostatic, mainly acts on alpha-1 adrenergic receptors.
  3. Prostaglandin E1 (PGE1) is the theoretical cyclooxygenase metabolite of dihomo-γ-linolenic acid (DGLA), but it is virtually undetectable in the plasma of normal humans or other animals. The IC50 of PGE1 for the inhibition of ADP-induced human platelet aggregation is 40 nM.
  4. D2/5-HT2 receptor antagonist

    Blonanserin is a D2/5-HT2 receptor antagonist; atypical antipsychotic.
  5. β2-adrenergic receptor

    Carvedilol is a β1- and β2-adrenergic receptor (AR) agonist with antioxidant properties.
  6. alpha2-adrenoceptor agonist

    Dexmedetomidine hydrochloride is the active isomer of medetomide which acts a potent, highly selective alpha2-AR (alpha2-adrenoceptor) agonist.
  7. COX inhibitor/histamine H1 receptor agonist

    Fexofenadine HCl is an antihistamine that inhibits Cox-1, Cox-2, and is a histamine H1 receptor agonist
  8. Lamotrigine is a novel anticonvulsant drug for inhibition of 5-HT with IC50 of 240 μM and 474 μM in human platelets and rat brain synaptosomes, and also is a sodium channel blocker.
  9. Prostaglandin E2 is a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation.
  10. Procaterol is a short-acting β2-adrenergic receptor agonist with Kp of 8 nM, used for the treatment of asthma
  11. Leukotriene receptor antagonist

    Pranlukast is a selective cysteinyl leukotriene receptor antagonist.
  12. Prazosin HCl is an α1 and α2B-adrenoceptor antagonist. Also a potent antagonist at the melatonin MT3 receptor (Ki = 10.2 nM).
  13. Ropinirole a selective dopamine D2 receptors inhibitor with IC5N/A of 29 nM.
  14. Ropinirole Hydrochloride is a dopamine receptor agonist.
  15. Reboxetine is an antidepressant compound that selectively inhibits norepinephrine uptake (IC50s = 8.2 and 1,070 nM for norepinephrine and serotonin transporters, respectively). It displays greater than 1,000-fold affinity for binding rat norepinephrine receptors compared to serotonin, histamine, acetylcholine, or dopamine receptors (Kis = 1.1, 129, 1,400, 3,900, and >10,000 nM, respectively).
  16. Roxatidine Acetate Hydrochloride is a histamine H2-receptor antagonist used in ulcer treatment. This compound has been found to inhibit platelet function in vitro.
  17. 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.
  18. 5-HT7 receptor antagonist

    SB269970 is a potent and selective 5-HT7 receptor antagonist.
  19. CB receptor agonist

    WIN 55,212-2 is a potent cannabinoid receptor agonist that has been found to be a potent analgesic in a rat model of neuropathic pain. It activates p42 and p44 MAP kinase via receptor-mediated signaling.
  20. DAT and SLC6A2 inhibitor

    GBR-12935 is a piperazine derivative which is a potent and selective dopamine reuptake inhibitor.
  21. CB2 receptor ligand

    BML-190 is a selective inverse agonist of the human cannabinoid CB2 receptor.
  22. CB2 agonist

    MDA 19 is a potent and selective agonist for the cannabinoid receptor CB2, with reasonable selectivity over the psychoactive CB1 receptor.
  23. CB1 antagonist

    CP 945598 is a potent and highly selective CB1 antagonist.
  24. CXCR4 antagonist

    AMD 3465 is a potent, selective CXCR4 antagonist.
  25. GPR40 Inhibitor

    GW 9508 is a cell-permeable aminophenylpropanoate that acts as a potent and selective agonist for the G-protein coupled receptor (GPCR) GRP40/FFA1 receptor (EC50 ?50 nM) with reduced activity towards family members GRP120 (EC50 ?3.5 μM), GRP41/GRP43 (EC50 >50 μM), as well as a panel of eight other free fatty acid (FFA) and prostaglandin receptors.
  26. LPA Receptor antagonist

    Ki16198 is a potent LPA receptor antagonist and inhibits LPA1- and LPA3-induced inositol phosphate production with Ki of 0.34 μM and 0.93 μM, respectively.
  27. CTEP is a highly potent, selective and orally bioavailable allosteric antagonist of mGlu5 receptor with an IC50 of 2.2 nM.
  28. AR antagonist

    Diprophylline is a xanthine derivative with bronchodilator and vasodilator effects.
  29. YIL 781 is a ghrelin receptor antagonist (GHS-R1a) (Ki = 17 nM)
  30. Rotundine (L-tetrahydropalmatine, L-THP) is a selective dopamine D1 receptor antagonist with IC50 of 166 nM.
  31. mGlu4 receptors modulator

    VU 0364770 is a positive allosteric modulator at mGlu4 receptors with EC50 value of 290 nM in mGlu4-expressing HEK 293 cells.
  32. 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.
  33. lysophaphatidic acid 1 (LPA1/Edg-2) receptor inhibitor

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

    BIIE 0246 is a potent, selective and competitive non-peptide antagonist for the neuropeptide Y Y2 receptor (IC50 = 15 nM).
  35. 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.
  36. 5-HT/dopamine D2 antagonist

    Ocaperidone is an effective antipsychotic agent.
  37. 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.

  38. A3 adenosine receptor agonist

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

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

    Aglafoline is an effective PAF antagonist not only in vitro, but also in vivo.
  41. 5-HT2c receptor agonist

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

    TY-52156 is a potent and selective S1P3 receptor antagonist with a Ki value of 110 nM.
  43. 5-HT4 receptor antagonist

    5-HT4 antagonist 1 is a 5-HT4 receptor antagonist with a pKi of 9.6.
  44. 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).
  45. human 5-HT1A receptor agonist

    AP521 is an agonist of human 5-HT1A receptor with an IC50 of 94 nM.
  46. 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.
  47. 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).
  48. cannabinoid CB2 receptor inverse agonist

    CB2R-IN-1 is a potent cannabinoid CB2 receptor inverse agonist with a Ki of 0.9 nM.
  49. σ1 agonist

    4-IBP is a selective ς1 agonist with a high level of affinity for the ς1 receptor (Ki = 1.7 nM) and a moderate affinity for the ς2 receptor (Ki = 25.2 nM) .
  50. Dopamine D2 autoreceptor agonist

    NMI 8739 is a dopamine D2 autoreceptor agonist, which is an amine conjugate of the DHA carrier and the neurotransmitter dopamine.

Items 201-250 of 1393

per page
Set Descending Direction