GPCR/G Protein

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Product Name
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Product Information
Product Citation
  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. peptide Oxytocin Receptor Inhibitor

    Atosiban is a peptide Oxytocin Receptor Inhibitor.
  4. serotonin/NE reuptake inhibitor

    Levomilnacipran HCl is a selective serotonin and norepinephrine reuptake inhibitor.
  5. adrenergic receptor/5-HT receptor inhibitor

    Asenapine hydrochloride 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.
  6. Dopamine reuptake inhibitor

    Phenylpiracetam is a phenylated derivative of the nootropic drug piracetam. It is used as a stimulant nootropic drug that can be up to 30-60 times more potent than piracetam.
  7. CXCL8 receptor inhibitor

    Reparixin L-lysine salt is an inhibitor of CXCL8 receptor, also inhibit CXCR1 and CXCR2 activation,which has been shown to attenuate inflammatory responses in various injury models.
  8. LTA4 hydrolase Inhibitor

    SC 57461A is a potent and competitive inhibitor of recombinant human leukotriene A4 hydrolase in vitro (Askonas et al., 2002).
  9. serotonin (5-HT)/norepinephrine (NE) reuptake inhibitor

    Desvenlafaxine succinate hydrate is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI).
  10. NA reuptake inhibitor

    MCI-225 is a selective NA reuptake inhibitor with 5-HT3 receptor antagonism.
  11. 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.
  12. NDR Inhibitor

    Bupropion is a medication primarily used as an antidepressant and smoking cessation aid.
  13. 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.
  14. 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.
  15. SMO inhibitor

    Jervine is a naturally occuring steroidal alkaloid that causes cyclopia by blocking sonic hedgehog(Shh) signaling; Jervine is an inhibitor of Smo.
  16. 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.
  17. Histamine H1 receptor inhibitor

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

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

    CCG 50014 is a potent and selective inhibitor of RGS4 with IC50 of 30 nM.
  20. Serotonin reuptake inhibitor

    Escitalopram oxalate ((S)-(+)Citalopram oxalate) is a selective serotonin reuptake inhibitor (SSRI) with Ki of 0.89 nM.
  21. 5-HT1A receptor antagonist/COMT inhibitor

    Flopropione is a 5-HT1A receptor antagonist and also a catechol-o-methyltransferase (COMT) inhibitor.
  22. 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.
  23. 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.
  24. 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.
  25. 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.
  26. serotonin uptake inhibitor

    Paroxetine Mesylate is a serotonin uptake inhibitor that is effective in the treatment of depression.
  27. 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.
  28. 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.
  29. 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.
  30. D2DR/D4DR inhibitor

    Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.
  31. alpha-1 adrenergic receptors / mAChRs inhibitor

    Anisodamine is an inhibitor of alpha-1 adrenergic receptors and mAChRs isolated from Chinese solanacea plant.
  32. 5-Lipoxygenase (5-LO) inhibitor

    Atreleuton (ABT-761) is a selective, reversible, and orally bioavailable 5-Lipoxygenase (5-LO) inhibitor. Atreleuton (ABT-761) exhibits potent and selective inhibition of leukotriene formation.
  33. LTC4S inhibitor

    TK05 is a potent and selective inhibitor of leukotriene C4 synthase (LTC4S) with an IC50 of 95 nM.
  34. LTC4S inhibitor

    AZD9898 is an orally active leukotriene-C4 synthetase (LTC4S, glutathione S-transferase II) inhibitor, with an IC50 of 0.28 nM. AZD9898 mitigates the GABA binding and hepatic toxicity signal. AZD9898 has the potential to treat asthma.
  35. triple reuptake inhibitor/5-HT2A/5-HT2C/5-HT3/α1A-adrenergic receptor antagonis

    Tedatioxetine hydrobromide acts as a triple reuptake inhibitor and 5-HT2A, 5-HT2C, 5-HT3 and α1A-adrenergic receptor antagonist.
  36. LTB4 receptor inhibitor

    LY223982 is a potent and specific inhibitor of leukotriene B4 receptor, with an IC50 of 13.2 nM against [3H]LTB4 binding to LTB4 receptor.
  37. 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.
  38. 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).
  39. adenylate cyclase inhibitor

    CB-7921220 is an adenylate cyclase inhibitor.
  40. 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.
  41. 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.
  42. CBP inhibitor

    GNE-049 is a highly potent and selective CBP inhibitor with an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC50s of 12 nM and 4200 nM, respectively.
  43. AC1 inhibitor

    ST034307 is a potent and selective adenylyl cyclase 1 (AC1) inhibitor, with IC50 of 2.3 μM.
  44. 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.
  45. 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.
  46. 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.
  47. GRK2 inhibitor

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

    Acebilustat (CTX-4430) is a leukotriene A4 hydrolase inhibitor, used for an oral antiinflammatory drug.
  49. 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.
  50. Smo inhibitor

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

Items 51-100 of 119

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