GPCR/G Protein

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  1. CB1/CB2 agonist

    NMP-7 is a non-selective agonist of the CB1 and CB2 cannabinoid receptors that acts by blocking T-type calcium channels.
  2. alpha2-Adrenergic receptor agonist

    Flutonidine is an alpha2-Adrenergic receptor agonist.
  3. mGlu1 receptorsant agonist

    YM 298198 is a non-competitive antagonist with high affinity and selectivity for mGlu1 receptors (Ki = 19 nM).

  4. Galanin receptors GALR agonist

    Galnon is a selective, non-peptide agonist at the galanin receptors GALR.
  5. prostanoid agonist

    QCC-374 is prostanoid agonist potentially for the treatment of pulmonary arterial hypertension.
  6. central alpha 2-adrenoceptor agonist

    Guanabenz (GBZ, GA, Wytensin, Wy-8678) is an orally active central alpha 2-adrenoceptor (α2 adrenergic receptor) agonist with antihypertensive action.
  7. Tirzepatide (LY3298176, GIP/GLP-1 RA, TZP) is a dual GIP/GLP-1 receptor agonist. Tirzepatide differentially induces internalization of the GIP and GLP-1 receptors with EC50 values of 18.2 nM and 18.1 nM, respectively.
  8. Glucagon receptor agonist

    Retatrutide (LY3437943) is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). Retatrutide binds human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643 and 0.775 nM, respectively. Retatrutide can be used for the research of obesity.
  9. GLP-1 receptor agonist

    Oxyntomodulin (bovine, porcine), a 37-amino acid peptide hormone, is a glucagon-like peptide 1 (GLP-1) receptor agonist.
  10. GLP-1 agonist

    Lixisenatide acetate is a glucagon-like peptide-1 (GLP-1) receptor agonist that can be used in the treatment of type 2 diabetes mellitus (T2DM).
  11. μ-opioid receptor agonist

    Dermorphin is a natural heptapeptide μ-opioid receptor (MOR) agonist found in amphibian skin. Inhibition of neuropathic pain.
  12. PAR-1 agonist

    Protease-Activated Receptor-1, PAR-1 Agonist is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor.
  13. CRFR agonist

    Urocortin, rat (Urocortin (Rattus norvegicus)) is a neuropeptide and a potent endogenous CRFR agonist with Kis of 13 nM, 1.5 nM, and 0.97 nM for human CRF1, rat CRF2α and mouse CRF2β, respectively.
  14. neuropeptide Y (NPY) Y5 receptor agonist

    [D-Trp34]-Neuropeptide Y is a potent and selective neuropeptide Y (NPY) Y5 receptor agonist. [D-Trp34]-Neuropeptide Y is a significantly less potent agonist at the NPY Y1, Y2, Y4, and y6 receptors. [D-Trp34]-Neuropeptide Y markedly increases food intake in rats.
  15. opioid κ-receptor agonist

    Dynorphin B (1-13) acts as an agonist on opioid κ-receptor.
  16. neurokinin (NK)-1 receptor agonist

    [Sar9] Substance P is a potent and selective neurokinin (NK)-1 receptor agonist.
  17. PAR-1 agonist

    iso-TRAP-6 (iso-SFLLRN) is a PAR-1 agonist that can activate platelets. iso-TRAP-6 is an analog of TRAP-6 that refers to the use of isoserine instead of serine as first amino acid.
  18. VPAC2 agonist

    Bay 55-9837 is a potent and highly selective agonist of VPAC2, with a Kd of 0.65 nM. Bay 55-9837 may be a useful therapy for the research of type 2 diabetes.
  19. CXCR4 agonist

    CTCE-0214 is a chemokine CXC receptor 4 (CXCR4) agonist, SDF-1α (stromal cell-derived factor-1α) peptide analog. CTCE-0214 shows anti-inflammatory activity, and can be used in inflammation sepsis and systemic inflammatory syndromes research.
  20. PAR2 agonist

    AY254 is an analogue of AY77. AY254 is ERK-biased PAR2 agonist with an EC50 of 2 nM. AY254 relieves cytokine-induced caspase 3/8 activation. AY254 also promotes scratch-wound healing and induced IL-8 secretion via PAR2-ERK1/2 signaling.
  21. PAR2 agonist

    AY77 is a calcium-biased PAR2 agonist. AY77 shows an EC50 of 0.17 and 2 nM in PAR2-mediated the activation in the Gq pathway and recruitment of β-arrestin-2, respectively. AY77 potently induces intracellular Ca2+ release.

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