GPCR/G Protein

Shop By

Items 51-100 of 663

Page
per page
Set Descending Direction
Catalog No.
Product Name
Application
Product Information
Citations
  1. EPAC1/EPAC2 inhibitor

    ESI-09 is a specific exchange protein directly activated by cAMP (EPAC) inhibitor with IC50 of 3.2 uM and 1.4 uM for EPAC1 and EPAC2,
  2. EPAC2 inhibitor

    HJC0350 is a potent and selective EPAC2 inhibitor with IC50 of 0.3 μM, exhibiting no inhibition on Epac1.
  3. serotonin/NE reuptake inhibitor

    Levomilnacipran HCl is a selective serotonin and norepinephrine reuptake inhibitor.
  4. 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.
  5. D2DR and D4DR inhibitor

    Loxapine Succinate is a D2DR and D4DR inhibitor and serotonergic receptor antagonist. Loxapine succinate is an antipsychotic agent used in schizophrenia.
  6. Prostaglandin Receptor inhibitor

    Benorilate, also known as Win-11450, is an ester of aspirin and paracetamol with analgesic, antipyretic, and anti-inflammatory activity used in the treatment of rheumatoid diseases. Benorilate has less severe side effects than aspirin.
  7. Prostaglandin Receptor inhibitor

    Dinoprost Tromethamine, also known as Dinoprost Trometamol, is a naturally occurring prostaglandin used in medicine to induce labor and as an abortifacient.
  8. serotonin uptake inhibitor

    Paroxetine Mesylate is a serotonin uptake inhibitor that is effective in the treatment of depression.
  9. 5-HT2 receptors inhibitor

    Nefazodone HCl is an inhibitor of 5-HT2 receptors, SERT, NET, and hERG K+ channels used to treat mood disorders. It decreases immobility time in the forced swim test.
  10. D2DR inhibitor

    Promazine Hydrochloride is a phenothiazine compound and D2DR inhibitor. Promazine Hydrochloride has been employed in studies investigating dopamine-stimulated glycosylation of brain proteins in vitro. It has actions similar to chlorpromazine but with less antipsychotic activity.
  11. MAO inhibitor

    Molindone HCl is a D2 dopamine receptor antagonist. It also acts as a MAO inhibitor.
  12. adrenergic receptor inhibitor

    Asenapine(Org 5222) inhibits adrenergic receptor (α1, α2A, α2B, α2C) with Ki of 0.25-1.2 nM and also inhibits 5-HT receptor (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) with Ki of 0.03-4.0 nM.
  13. D2DR/D4DR inhibitor

    Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.
  14. DOPA decarboxylase inhibitor

    Methyldopa Sesquihydrate is a DOPA decarboxylase inhibitor and indirect α2-adrenergic receptor agonist used to treat hypertension.
  15. alpha-1 adrenergic receptors / mAChRs inhibitor

    Anisodamine is an inhibitor of alpha-1 adrenergic receptors and mAChRs isolated from Chinese solanacea plant.
  16. EGFR inhibitor

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

     
  17. GRK2/5 inhibitor

    CCG215022 is a potent GRK2 and GRK5 inhibitor. CCG215022 exhibited nanomolar IC50 values against both GRK2 and GRK5 and good selectivity against other closely related kinases such as GRK1 and PKA.
  18. SMO inhibitor

    Jervine is a naturally occuring steroidal alkaloid that causes cyclopia by blocking sonic hedgehog(Shh) signaling; Jervine is an inhibitor of Smo.
  19. 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.
  20. Histamine H1 receptor inhibitor

    Antazoline HCl is a first generation antihistamine, binding to the histamine H1 receptor and blocking the action of endogenous histamine.
  21. Histamine/cholinergic inhibitor

    Azatadine is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively.
  22. RGS4 inhibitor

    CCG 50014 is a potent and selective inhibitor of RGS4 with IC50 of 30 nM.
  23. 5-HT1A receptor antagonist/COMT inhibitor

    Flopropione is a 5-HT1A receptor antagonist and also a catechol-o-methyltransferase (COMT) inhibitor.
  24. sGC inhibitor

    NS-2028 is a highly selective soluble Guanylyl Cyclase (sGC) inhibitor with IC50 values of 30 nM and 200 nM for basal and NO-stimulated enzyme activity.
  25. triple reuptake inhibitor

    Dasotraline hydrochloride (SEP-225289 hydrochloride) is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.
  26. SSR inhibitor / 5-HT1A receptor partial agonist

    Vilazodone D8 is the a deuterium labeled vilazodone, which is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist.
  27. leukotriene A4 hydrolase inhibitor

    DG051 is a potent leukotriene A4 hydrolase inhibitor of leukotriene B4 biosynthesis in the enzyme assay with an IC50=47 nM.
  28. DPP4 inhibitor

    Vildagliptin (LAF237 dihydrate;NVP-LAF 237 dihydrate) is a dipeptidyl peptidase 4 (DPP4) inhibitor that delays the degradation of glucagon-like peptide-1 (GLP-1).
  29. dopamine reuptake inhibitor

    Vanoxerine (GBR-12909) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM).
  30. LTC4 inhibitor

    Nedocromil sodium suppresses the action or formation of multiple mediators, including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2).
  31. dopamine reuptake inhibitor

    GBR 12935 is a potent, and selective dopamine reuptake inhibitor.
  32. serotonin reuptake inhibitor/5-HT2A receptor antagonist

    Eplivanserin mixture is a selective serotonin reuptake inhibitor and a 5-HT2A receptor antagonist, extracted from patent WO 2005/002578 A1.
  33. bovine tubulin oxidation inhibitor

    Takeda103A is a potent GRK2-dependent bovine tubulin oxidation inhibitor.
  34. allosteric inhibitor of CXCR1 and CXCR2

    SX-682 is an orally bioavailable, potent allosteric inhibitor of CXCR1 and CXCR2.
  35. ODQ

    soluble guanylyl cyclase inhibitor

    ODQ is a potent and selective soluble guanylyl cyclase (sGC, nitric oxide-activated enzyme) inhibitor. ODQ enhances the pro-apoptotic effects of Cisplatin in human mesothelioma cells.
  36. glucagon receptor inhibitor

    GRA Ex-25 is an inhibitor of glucagon receptor, with IC50 of 56 and 55 nM for rat and human glucagon receptors, respectively.
  37. thromboxane A2 synthase inhibitor

    Terbogrel is an orally available thromboxane A2 receptor antagonist and a thromboxane A2 synthase inhibitor, with both IC50s of about 10 nM.
  38. thromboxane synthesis inhibitor

    Ro-24-0238 is an antagonist of platelet activating factor (PAF) and inhibitor of thromboxane synthesis, used for lessening the inflammation and damage resulting from a local release of PAF.
  39. GRK2 inhibitor

    GSK180736A is a G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.
  40. leukotriene A4 hydrolase inhibitor

    Acebilustat (CTX-4430) is a leukotriene A4 hydrolase inhibitor, used for an oral antiinflammatory drug.
  41. monoamine reuptake inhibitor

    Diclofensine hydrochloride (Ro-8-4650 hydrochloride) is a potent inhibitor of monoamine reuptake, blocking the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3, and 3.7 nM, respectively.
  42. Smo inhibitor

    LEQ506 is a second-generation inhibitor of smoothened (Smo) with IC50s of 2 and 4 nM in human and mouse, respectively.
  43. dual NE/DA transporter inhibitor

    Centanafadine is dual norepinephrine (NE)/dopamine (DA) transporter inhibitor, also inhibits serotonin transporter, with IC50s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively.
  44. AC1 inhibitor

    NB001 (HTS 09836) is an adenylcyclase 1 (AC1) inhibitor which has effect on neural and non-neural pain by modulating AC1 activity.
  45. 5-HT1A/5-HT1B/5-HT3A/5-HT7 receptor/SERT inhibitor

    Vortioxetine is a inhibitor of 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT, with Ki values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.
  46. KH7

    sAC-specific inhibitor

    KH7 is a soluble adenylyl cyclase (sAC)-specific inhibitor, with IC50s of 3-10 μM toward both recombinant purified human sACt protein and heterologously expressed sACt in cellular assays.
  47. GRK2/GRK3 inhibitor

    CMPD101, is a novel membrane-permeable, small-molecule inhibitor of both GRK2 and GRK3 with IC50s of 18 nM and 5.4 nM. CMPD101 also inhibits ROCK-2 and PKCα (IC50s=1.4 μM and 8.1 μM, respectively).
  48. adenylate cyclase inhibitor

    CB-7921220 is an adenylate cyclase inhibitor.
  49. SERT inhibitor

    DSP-1053 is a potent Serotonin Transporter (SERT) (Ki=1.02 nM) inhibitor with partial 5-HT1A receptor (Ki=5.05 nM) agonistic activity.
  50. AChE /M1/M2/5HT4/I2 inhibitor

    MHP 133 is a drug with multiple CNS targets, and inhibits acetylcholinesterase (AChE) with Ki of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors.

Items 51-100 of 663

Page
per page
Set Descending Direction