GPCR/G Protein

Items 5501-5550 of 6977

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Catalog No.
Product Name
Application
Product Information
Citations
  1. group III mGluR antagonist

    MSOP is a selective group III metabotropic glutamate receptor antagonist with apparent KD of 51 μM for the L-AP4-sensitive presynaptic mGluR.
  2. Sigma-1 receptor antagonist

    Sigma-1 receptor antagonist 3 (compound135) is a potent and selective Sigma-1 (??1) receptor antagonist with a Ki of 1.14 nM.
  3. sigma 1 receptor antagonist

    Sigma-1 receptor antagonist 2 is a potent and selective sigma 1 receptor (??1 R) antagonist with Kis of 3.88 and 1288 nM for ??1 and ??2 receptor, respectively.
  4. CCKA receptor antagonist

    Dexloxiglumide is a selective cholecystokinin type A (CCKA) receptor antagonist. Dexloxiglumide, the active enantiomer of Loxiglumide, inhibits smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8).
  5. PPARγ and CB2 receptor dual agonist

    VCE-004.8, a semi-synthetic multitarget cannabinoquinoid, is a specific PPARγ and CB2 receptor dual agonist with potent anti-inflammatory activity.
  6. Thyrotropin receptor modulator

    D3-βArr is a positive allosteric modulator for thyrotropin receptor (TSHR), which initiates translocation of β-Arr 1 by direct TSHR activation and potentiates TSH-mediated preosteoblast differentiation in vitro.
  7. Oxytocin receptor antagonist

    SHR1653 is a highly potent, selective and brain penetrated oxytocin receptor (OTR) antagonist, with an IC50 of 15 nM for hOTR.
  8. κ opioid receptor antagonist

    BTRX-335140 (CYM-53093) is a potent and selective, orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively.
  9. CRTH2/DP2 receptor antagonist

    CAY10595 is a potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki of 10 nM.
  10. 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.
  11. LPA2 agonist

    Radioprotectin-1 is a potent and specific nonlipid agonist of lysophosphatidic acid receptor 2 (LPA2), with an EC50 value of 25 nM for murine LPA2 subtype.
  12. PAR2 antagonist

    I-191 is a potent, selective protease-activated receptor 2 (PAR2) antagonist.
  13. LPA5 antagonist

    AS2717638 is an oral active and selective lysophosphatidic acid receptor 5 (LPA5) antagonist, with an IC50 of 38 nM for hLPA5. AS2717638 also significantly improves PGE2-, PGF2α-, and AMPA-induced allodynia.
  14. Rev-Erbα/β agonist

    SR10067 is a potent, selective and brain penetrant Rev-Erbα/β agonist, with IC50 values are 160 and 170 nM for Rev-Erbβ and Rev-Erbα, respectively. SR10067 has anxiolytic activity.
  15. β2 adrenergic receptor agonist

    BI-167107 is a high affinity, full agonist that binds to the β2 adrenergic receptor (β2AR) with a dissociation constant Kd of 84 pM.
  16. Smo mutant antagonist

    ALLO-2 is a potent drug-resistant Smoothened (Smo) mutant antagonist that inhibits Smo agonist Hh-Ag1.5-induced luciferase expression in TM3-Gli-Luc cells with IC50 of 6 nM.
  17. neuropeptide Y1 receptor antagonist

    BMS-193885 is a potent, competitive neuropeptide (NPY) Y1 antagonist (Ki = 3.3 nM, IC50 = 5.9 nM) that displays > 47, > 100, > 160, > 160 and > 160-fold selectivity over ??1, α1, Y2, Y4 and Y5 receptors respectively.
  18. non-peptide PAR2 agonist

    GB110 is a Novel potent non-peptide PAR2 agonist. GB-110 selectively induces PAR2-mediated intracellular Ca2+ release in HT29 cells with an EC50 of 0.28 μM.
  19. LPA1 receptor antagonist

    ASP6432 is a potent and selective Type 1 Lysophosphatidic Acid (LPA1) receptor antagonist.
  20. LTC4S inhibitor

    TK05 is a potent and selective inhibitor of leukotriene C4 synthase (LTC4S) with an IC50 of 95 nM.
  21. CXCR4 receptor antagonist

    USL311 is a CXCR4 receptor antagonist which prevents the binding of stromal-cell derived factor-1 (SDF-1 or CXCL12) to CXCR4.
  22. PAR2 antagonist

    GB-88 is a novel selective, orally available PAR2 antagonist, inhibits PAR2 activated Ca2+ release with an IC50 of 2 ?M.
  23. Dopamine D4 receptor antagonist

    A-381393 is a potent and selective agonist of the dopamine D4 receptor.
  24. GLP-1R modulator

    VU0453379 is a CNS-penetrant glucagon-like peptide 1 receptor (GLP-1R) positive allosteric modulator (PAM) with an EC50 of 1.3 μM.
  25. SSTR5 antagonist

    SSTR5 antagonist 2 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential to treat type 2 diabetes mellitus (T2DM).
  26. CB1 antagonist

    CB1 antagonist 2 is caimabinoid 1 (CB1) antagonist extracted from patent WO2016184310A1, compound 3, inhibits CB1 in vivo with an IC50 of 25.5 nM.
  27. E1R

    sigma-1 receptors modulator

    E1R is a novel positive allosteric modulator of sigma-1 receptors.
  28. PAR4 antagonist

    UDM-001651 is a potent , selective and orally active Protease-Activated Receptor 4 (PAR4) Antagonist with in Vivo Antithrombotic Efficacy (IC50 = 2.4 nM).
  29. GPRC6A agonist

    DJ-V-159 is an agonist for G protein-coupled receptor family C group 6 member A (GPRC6A).
  30. non-peptide MAS agonist

    AR234960, a non-peptide MAS (a G protein-coupled receptor) agonist, increases both mRNA and protein levels of CTGF via ERK1/2 signaling in HEK293-MAS cells and adult human cardiac fibroblasts.
  31. D1 receptor agonist

    PF-06256142 is a potent and selective orthosteric agonist of the D1 receptor, with D1 EC50=30 nM and D1 binding Ki = 12 nM.
  32. mGlu5 modulator

    VU0652835 is a metabotropic glutamate receptor subtype 5 (mGlu5) negative allosteric modulator with an IC50 of 81 nM.
  33. GLP-1R modulator

    NNC0640 is a negative allosteric modulator of glucagon-like peptide-1 receptor (GLP-1R).
  34. CRTH2 antagonist

    BI-671800 is a CRTH2 antagonist that treats patients with asthma.
  35. GLP-1 receptor agonist

    Semaglutide, a long-acting GLP-1 analogue, is a glucagon-like peptide-1 (GLP-1) receptor agonist that can be used in the treatment of type 2 diabetes.
  36. TSHR agonist

    ML-109 is a potent and full thyroid stimulating hormone receptor (TSHR) agonist, with an EC50 of 40 nM.
  37. Dopamine receptor blocker

    Dicarbine blocks dopamine receptors in various brain parts and prevents the depression of the conditioned defence reflexes caused by stimulation of the mesencephalic portion of the reticular formation. Dicarbine could be used to treat patients with schizophrenia and alcoholic psychosis in clinical.
  38. histamine H4 receptor inverse agonist

    H4 Receptor antagonist 1 is a potent and selective histamine H4 receptor inverse agonist, with an IC50 of 19 nM.
  39. angiotensin 1 (AT1) and AT2 receptor agonist

    Angiotensin III is an angiotensin 1 (AT1) and AT2 receptor agonist.
  40. 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.
  41. μ-opioid receptor antagonist

    GSK1521498 free base is a potent and selective μ-opioid receptor (MOR) antagonist. GSK1521498 free base is being used for the treatment of disorders of compulsive consumption of food, alcohol, and drugs.
  42. apelin agonist

    Apelin agonist 1 is an oral selective apelin agonist AM-2995, a agonist of the APJ (APLNR, angiotensin receptor like-1) receptor, may be used in the treatment of cardiovascular conditions.
  43. NOP receptor antagonist

    LY-2940094 is a potent, selective and orally available nociceptin receptor (NOP receptor) antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY-2940094 reduces ethanol self-administration in animal models.
  44. mGlu3 receptor agonist

    LY2794193 is a highly potent and selective mGlu3 receptor agonist (hmGlu3 Ki=0.927 nM??EC50=0.47 nM; hmGlu2 Ki=412 nM??EC50=47.5 nM).
  45. mGlu2/3 antagonist

    LY3020371 hydrochloride is a potent, selective metabotropic glutamate 2/3 receptor (mGlu2/3) antagonist with Ki of 5.3 and 2.5 nM, potently blocks cAMP formation with IC50 of 16.2 nM.
  46. mu-opioid receptor agonist

    CYT-1010 is a mu-opioid receptor agonist extracted from patent WO2013173730A2, with EC50s of 13.1 nM and 0.0053 nM on beta-arrestin recruitment and inhibition of cAMP production, respectively.
  47. FFA2 agonist

    TUG-1375 is an agonist of free fatty acid receptor 2 (FFA2/GPR43), with a pKi of 6.69. TUG-1375 is inactive on FFA3, FFA4, PPARα, PPARγ, PPARδ, LXRα or LXRβ.
  48. GPR40 full agonist

    GPR40 agonist 1 is a potent and novel GPR40 full agonist with an EC50 of 2 nM and 17 nM for hGPR40 and rGPR40, respectively.
  49. dopamine D2/D3 receptor antagonist

    Raclopride is a dopamine D2/D3 receptor antagonist, which binds to D2 and D3 receptors with dissociation constants (Kis) of 1.8 nM and 3.5 nM, respectively, but has a very low affinity for D1 and D4 receptors with Kis of 18000 nM and 2400 nM, respectively.
  50. PAF antagonist

    Tulopafant is a platelet activating factor (PAF) antagonist.

Items 5501-5550 of 6977

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