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Pathways Recommended: GPCR/G Protein
Results for "

Gαs protein

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-112461A
    NF449 octasodium
    4 Publications Verification

    		 P2X Receptor Cardiovascular Disease
    NF449 octasodium is a highly potent P2X1 receptor antagonist, with IC50s of 0.28, 0.69, and 120 nM for rP2X1, rP2X1+5, P2X2+3, respectively. NF449 octasodium is a Gsα-selective G Protein antagonist. NF449 octasodium suppresses the rate of GTP[γS] binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks the coupling of β-adrenergic receptors to Gs .
    NF449 octasodium
  • HY-171978
    LM-189

    		Adrenergic Receptor Cardiovascular Disease
    LM-189 is a β2-adrenergic receptor (β2AR) ligand and G protein-biased modulator with a human β2AR Ki of 0.063 nM.LM-189 promotes β2AR coupling to Gαs and Gαi heterotrimers, stabilizes distinct β2AR conformations including a TM6 outward state, and increases β2AR ICL2 dynamics.LM-189 restricts β2AR ligand-binding pocket conformational heterogeneity, stabilizes polar ligand-receptor interaction networks, and exhibits bias toward Gαi signaling over Gαs signaling.LM-189 enabled cryo-EM structural characterization of the β2AR-Gi complex.LM-189 can be used for the research of congestive heart failure .
    LM-189
  • HY-162734
    BRD5075

    		GPR65 Inflammation/Immunology
    BRD5075 is a selective GPR65 activator. BRD5075 enhances GPR65 activity under acidic conditions, promotes Gαs-dependent signaling pathways, including cAMP production and G protein recruitment. BRD5075 regulates the cytokine and chemokine expression network in dendritic cells, and inhibits the expression of pro-inflammatory cytokines and chemokines in a GPR65-dependent manner. BRD5075 is applicable to research related to inflammatory bowel disease .
    BRD5075
  • HY-112461
    NF449

    		P2X Receptor Cardiovascular Disease
    NF449 is a highly potent P2X1 receptor antagonist, with IC50s of 0.28, 0.69, and 120 nM for rP2X1, rP2X1+5, P2X2+3, respectively. NF449 is a Gsα-selective G Protein antagonist. NF449 suppresses the rate of GTP[γS] binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks the coupling of β-adrenergic receptors to Gs .
    NF449
  • HY-162735
    BRD5080

    		GPR65 Inflammation/Immunology
    BRD5080 is a GPR65 agonist. BRD5080 activates GPR65 to enhance the cAMP signaling pathway, reduce the expression of inflammatory cytokines and chemokines in dendritic cells, enhance the activity of human wild-type, mouse wild-type, and human GPR65 I231L variant receptors in a pH-dependent manner, and mediate the recruitment of Gαs protein. BRD5080 can be used in the research of inflammatory bowel disease .
    BRD5080
  • HY-182271
    GPR61 Inverse agonist 3

    		Orphan GPCR GABA Receptor Phosphodiesterase (PDE) Metabolic Disease
    GPR61 Inverse agonist 3 is a selective and brain-penetrant GPR61 inverse agonist with human IC50 of 4.0 nM, mouse IC50 of 8.8 nM, human Ki of 0.34 nM, mouse Ki of 1.1 nM. GPR61 Inverse agonist 3 disrupts GPR61-Gαs protein interactions to abolish GPR61 constitutive activity. GPR61 Inverse agonist 3 moderately inhibits GABAA chloride channel and PDE3A1 with IC50 values of 4.6 and 8.9 μM. GPR61 Inverse agonist 3 shows no functional effect on food intake in adult mice co-administered with a pan-CYP inhibitor. GPR61 Inverse agonist 3 can be used for the research of cachexia/sarcopenia .
    GPR61 Inverse agonist 3

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