GPCR/G Protein

Items 601-650 of 5455

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  1. glutamate receptors agonist

    (S)-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA).
  2. EGFR inhibitor

    AV-412 (MP412) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively.
  3. serotonin (5-HT)/norepinephrine (NE) reuptake inhibitor

    Desvenlafaxine succinate hydrate is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI).
  4. 5-HT3 receptor antagonist

    Ricasetron is a drug which acts as a selective antagonist at the serotonin 5-HT3 receptor.
  5. 5-HT3 antagonist

    LY278584 is a potent and selective antagonist of 5-HT3 receptors. LY278584 is a useful ligand for studying the localization of 5-HT3 receptors in rat brain
  6. 5HT3 receptor antagonist

    Lerisetron is a serotonin type 3 (5-HT3) receptor antagonist with antiemetic activity.
  7. NA reuptake inhibitor

    MCI-225 is a selective NA reuptake inhibitor with 5-HT3 receptor antagonism.
  8. EP4 receptor antagonist

    GW627368 is a novel, potent and selective competitive antagonist of prostanoid EP4 receptor(Ki= 100 nM) with additional human TP receptor affinity(Ki= 150 nM).
  9. EP4 receptor antagonist

    MF498 is a novel and selective E prostanoid receptor 4 (EP4 receptor) antagonist, displayed strong binding affinity for the EP4 receptor with Ki of 0.7 nM,
  10. 5-HT4 receptor antagonist

    Piboserod is a selective 5-HT(4) receptor antagonist.
  11. 5-HT1E/5-HT1F receptor agonist

    BRL 54443 is a 5-HT1E and 5-HT1F receptor agonist with pKi of 8.7 and 9.25, respectively, with a weak binding affinity for 5-HT1A, 5-HT1B, 5-HT1D receptors.
  12. 5-HT3 receptor inhibitor

    Eucalyptol is a bicyclic monoterpene that has been found in Eucalyptus and other plants. It is an inhibitor of 5-HT3 receptor ,potassium channel, TNF-α and IL-1β.
  13. Buclizine HCl is an antihistamine and anticholinergic of the piperazine derivative family.
  14. 5HT(1A) receptor agonist

    Buspirone is a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect, used for anxiety disorders.
  15. anticancer agent

    Decursin is an anticancer agent, with potential anti-inflammatory activity.
  16. CRTH2 antagonist

    ACT-129968 is a potent and selective CRTH2 antagonist.
  17. vasopressin V1 antagonist

    OPC21268 is a non-peptide AVP Receptor V (Vasopressin Receptor) antagonist that shows 1000-fold selectivity for V1 receptors over V2 receptors.
  18. mGlu2 receptor modulator

    CBiPES hydrochloride is a selective positive allosteric modulator of the mGluR-2 with IC50 value of 98.2 nM
  19. S1PR1 modulators

    RPC1063 is a selective sphingosine 1 phosphate receptor modulators and methods which may be useful in the treatment of S1P1-?associated diseases.
  20. mGluR5 Modulator

    VU0364289 is a novel N-aryl piperazine mGlu5 positive allosteric modulator.
  21. SK2 modulator

    NS13001 is a selective SK2/3 modulator that acts as a potential therapeutic agent for treatment of SCA2 and possibly other cerebellar ataxias.
  22. 5-HT1A/B/D receptor antagonist

    GSK163090 is a potent, selective, and orally active 5-HT1A/B/D receptor antagonist with pKi of 9.4/8.5/9.7, and 6.3/6.7 for 5-HT1A/B/D, and dopamine D2/D3, respectively.
  23. Dopamine Receptor Agonist?€?

    SKF38393 HCl is a D1 agonist with IC50 of 110 nM.
  24. EGFR inhibitor

    Olafertinib (CK-101, RX518) is an epidermal growth factor receptor (EGFR) inhibitor.

     
  25. EP2 Agonist

    C-544326 is a potent and selective prostaglandin E2 receptor agonist with EC50 value of 2.8 nM.
  26. β2 adrenergic receptor antagonist

    ICI-118551 is a selective beta2 adrenergic receptor (adrenoreceptor) antagonist.
  27. Serotonin2A Receptor Inverse Agonist

    Pimavanserin is a potent and selective serotonin 5-HT2A inverse agonist with pIC50 of 8.73, used to treat psychosis associated with Parkinson?€?s disease.
  28. A2A adenosine receptor antagonist

    SCH58261 is a potent and selective A2a adenosine receptor antagonist with Ki of 2.3 nM and 2 nM for rat A2a and bovine A2a, respectively.
  29. sGC activator?€?

    BAY 41-2272 is a direct and NO-independent soluble guanylate cyclase (sGC) stimulator.
  30. ETA receptor antagonist

    BQ-123 is a selective endothelin A receptor (ETA) antagonist with IC50 of 7.3 nM. Phase 2.
  31. 5HT(1A) receptor agonist

    Eptapirone is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential.
  32. Nurr1 activator

    C-DIM12 is a novel synthetic activator of Nurr1. C-DIM12 induces dopaminergic gene expression and protects against 6-hydroxydopamine neurotoxicity in vitro.
  33. CXCR2 antagonist

    AZD-5069 is a potent and selective CXCR2 antagonist with the potential to inhibit neutrophil migration into the airways in patients with COPD.
  34. prostaglandin EP4 receptor antagonist

    Grapiprant is a novel, potent and selective prostaglandin EP4 receptor antagonist with antihyperalgesic properties.
  35. Prostaglandin E2 receptor antagonist

    TG6-10-1 is a potent and selective antagonist for the prostaglandin E2 receptor subtype EP2.
  36. Opioid antagonist

    Naloxegol is a peripherally-selective opioid antagonist for the treatment of opioid-induced constipation.
  37. Orexin 2 receptor agonist

    A potent and selective Orexin2 receptor agonist.
  38. CysLT1 receptor antagonist

    MK-571 is a selective, orally active CysLT1 receptor antagonist. It blocks the binding of LTD4, but not LTC4, to human and guinea pig lung membranes with Ki values of 0.22 nM and 2.1 nM, respectively.
  39. CCK-2 receptor antagonist

    Nastorazepide is a selective, orally available, 1,5-benzodiazepine-derivative gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity.
  40. β2-adrenergic receptor agonist

    Vilanterol is a long-acting beta-2 agonist drug, which in May 2013 was approved in combination with fluticasone furoate for sale as Breo Ellipta by GlaxoSmithKline for the treatment of chronic obstructive pulmonary disease (COPD).
  41. JMV 390-1 is a inhibitor of the major neurotensin and neuromedin N degrading enzymes (IC50 values are 31, 40, 52 and 58 nM for endopeptidase 24.15, endopeptidase 24.11, leucine aminopeptidase and endopeptidase 24.16 respectively).
  42. cAMPS-Sp, triethylammonium salt is a cell-permeable cAMP analog that activates cAMP receptor proteins such as PKA and cAMP-regulated guanine nucleotide exchange factor.
  43. dopaminergic stabilizer

    ACR 16 hydrochloride is a dopaminergic stabilizer (Ki values 17550 nM and 7521 for D2(low) and D2(high), respectively) that state-dependently stabilizes psychomotor activity by the dual actions of functional dopamine D2 receptor antagonism and strengthening of cortical glutamate functions in various settings of perturbed neurotransmission.
  44. dopamine D2 receptor agonist

    UNC 9994 hydrochloride, unique, beta-arrestin-biased functionally selective dopamine D2 receptor (D2R) agonist (Ki value 30 nM; EC50 value 50 nM in ??-arrestin-2 recruitment assay) that exhibits antipsychotic activity in vivo. UNC9994 markedly inhibited PCP-induced hyperlocomotion in wild-type mice, which effect was completely abolished in ??-arrestin-2 knockout mice.
  45. Adenosine A1-R antagonist

    DPCPX, a xanthine derivative, is a very potent and selective Adenosine A1-R antagonist. It displays very modest efficacy against Adenosine A2A-R, Adenosine A2B-R and Adenosine A3-R.
  46. Adenosine A Receptor agonist

    2-Chloroadenosine is a metabolically stable analog of adenosine that behaves as an Adenosine A Receptor agonist (Ki values are 300, 80 and 1900 nM for Adenosine A1-R, Adenosine A2A-R and Adenosine A3-R, respectively).
  47. mGluR agonist

    (S)-3,5-DHPG is an agonist of the group I metabotropic glutamate receptors (mGluRs), binding both mGluR1a and mGluR5a (Ki = 0.9 and 3.9 uM, respectively) but not ionotropic glutamate receptors.
  48. GLP-1 receptor agonist

    Liraglutide is a long-acting glucagon-like peptide-1(GLP-1) receptor agonist.
  49. adenylyl cyclase inhibitor

    SQ22536 is an inhibitor of adenylyl cyclase with an IC50 of 1.4 uM. It can inhibit PGE1-stimulated increases in cAMP levels in intact human platelets.
  50. histamine-H1 receptor blocking agent

    Carbinoxamine maleate is a histamine-H1 receptor blocking agent with antihistamine and anticholinergic properties.

Items 601-650 of 5455

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