GPCR/G Protein

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Catalog No.
Product Name
Application
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Product Citation
  1. dopamine beta-hydroxylase inhibitor

    Nepicastat is an inhibitor of dopamine beta-hydroxylase, an enzyme that catalyzes the conversion of dopamine to norepinephrine.
  2. Serotonin reuptake inhibitor

    Vilazodone acts as a serotonin reuptake inhibitor (IC50 = 0.5 nM) and 5-HT1A receptor partial agonist (IC50 = 0.2 nM; IA = ~60-70%).
  3. RGS inhibitor

    CCG-63808 is a reversible inhibitor of regulator of G-protein signaling (RGS) proteins.
  4. DP1 inhibitor

    Laropiprant is used in combination with niacin to reduce blood cholesterol. Laropiprant acts as a DP1 antagonist, reducing the vasodilation.
  5. DAT and SLC6A2 inhibitor

    GBR-12935 is a piperazine derivative which is a potent and selective dopamine reuptake inhibitor.
  6. CXCL8/CXCR1/2 Inhibitor

    Reparixin is a potent inhibitor of both CXCL8 receptors CXCR1/2, it inhibits weakly CXCR2-mediated cell migration (IC50=100 nM), whereas it strongly blocks CXCR1-mediated chemotaxis (IC50=1 nM).
  7. Adenosine receptor inhibitor

    N-[(4-Aminophenyl)methyl]adenosine is a adenosine receptor inhibitor, with Ki of 29 nM for Rat ecto-5??-Nucleotidase. IC50 value: 29.0 ± 1.7 nM (Ki) Target: Adenosine Receptor
  8. leukotriene biosynthesis inhibitor

    MK-886 is an inhibitor of leukotriene biosynthesis (IC50 = 3 nM in human polymorphonuclear leukocytes).
  9. serotonin uptake inhibitor

    Norfluoxetine is an active metabolite of the antidepressant fluoxetine that inhibits serotonin uptake with a pKi value of 7.35.1 The S-enantiomer of norfluoxetine has 20-times higher serotonin reuptake blocking potency than the R-enantiomer (pKis = 7.86 versus 6.51, respectively).
  10. human 5'-methylthioadenosine phosphorylase inhibitor

    MT-DADMe-ImmA is an inhibitor of human 5'-methylthioadenosine phosphorylase (MTAP) with a Ki of 90 pM.
  11. peptide Oxytocin Receptor Inhibitor

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

    Levomilnacipran HCl is a selective serotonin and norepinephrine reuptake inhibitor.
  13. 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.
  14. 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.
  15. 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.
  16. NA reuptake inhibitor

    MCI-225 is a selective NA reuptake inhibitor with 5-HT3 receptor antagonism.
  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. serotonin uptake inhibitor

    Paroxetine Mesylate is a serotonin uptake inhibitor that is effective in the treatment of depression.
  20. 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.
  21. 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.
  22. 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.
  23. 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.
  24. prostaglandin synthase inhibitor

    Pizuglanstat is a hematopoietic prostaglandin synthase inhibitor.

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