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GPCR/G protein

G-protein-coupled receptors (GPCRs) mediate a wide range of physiological responses to environmental stimulants, neurotransmitters, hormones cytokines and lipid signaling molecules. As a result, GPCRs play a significant role in biological processes such as vision, olfaction, the autonomic nervous system, and behavior.

All GPCRs share a common seven trans-membrane structure. GPCRs are associated with heterotrimeric G-proteins which are GTP-binding proteins made of alpha, beta, and gamma subunits. When a ligand binds to GPCR, it activates the attached G-protein, the GDP is replaced with GTP. The activated G-protein then dissociates into an alpha and a beta-gamma complex which activates downstream signaling pathways. These intracellular signaling pathways include cAMP/PKA, calcium/NFAT, phospholipase C, protein tyrosine kinases, MAP kinases, PI-3-kinase, nitric oxide/cGMP, Rho, and JAK/STAT.

GPCRs are one of the most important therapeutic targets for various diseases, over 30% of all modern medicinal drugs target this family. Aberrant GPCR functions are involved in pathological conditions such as neurological, immunological and hormonal disorders. A large number of GPCRs have been identified, but whose ligands are not known, are classified as orphan receptors.

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  1. UNBS 5162
    Catalog No. :
    A8886
    A pan-antagonist of CXCL chemokines
    UNBS5162 is a pan-antagonist of CXCL chemokines.
  2. K-Ras(G12C) inhibitor 12
    Catalog No. :
    B4876
    allosteric inhibitor of K-Ras(G12C)
    K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of K-Ras(G12C) [1].
  3. p-iodo-Clonidine (hydrochloride)
    Catalog No. :
    C5822
    partial agonist of the α2-adrenergic receptor
  4. ONO-8130
    Catalog No. :
    C5743
    orally bioavailable antagonist of the prostaglandin E2 (PGE2) receptor EP
  5. GPR120 Compound A
    Catalog No. :
    C5824
    orally available, high-affinity agonist of GPR120
  6. Carazolol
    Catalog No. :
    C5802
    high-affinity, lipophilic, non-selective ligand of the β-adrenergic receptors
  7. Fendiline (hydrochloride)
    Catalog No. :
    C5675
    α2-adrenergic receptor antagonist
  8. γ-Linolenic Acid
    Catalog No. :
    C5518
    weak LTB4 receptor antagonist
  9. REV 5901
    Catalog No. :
    C5416
    antagonist of cysteinyl-leukotriene receptors
  10. S-2 Methanandamide
    Catalog No. :
    C5513
    potent CB1 receptor agonist

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