GPCR/G Protein

Items 1101-1150 of 6966

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  1. angiotensin II receptor type 1 antagonist

    Azilsartan medoxomil monopotassium is an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM, which used in the treatment of adults with essential hypertension.
  2. 5-HT1A/5-HT1B/5-HT1C agonist

    Eltoprazine(DU28853) is a serenic or antiaggressive agent which as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor.
  3. β2-adrenergic receptor agonist

    Levosalbutamol tartrate(levalbuterol) is the R-enantiomer of the short-acting β2-adrenergic receptor agonist salbutamol.
  4. leukotriene A4 hydrolase inhibitor

    Acebilustat (CTX-4430) is a leukotriene A4 hydrolase inhibitor, used for an oral antiinflammatory drug.
  5. angiotensin II and endothelin A receptor antagonist

    Sparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively.
  6. thromboxane-prostaglandin receptor antagonist

    Terutroban is a thromboxane-prostaglandin receptor antagonist.
  7. REV-ERBα/β agonist

    SR9009 is a REV-ERBα/β agonist with IC50s of 670 nM and 800 nM for REV-ERBα and REV-ERBβ, respectively.
  8. REV-ERBα/β agonist

    SR9011 is a REV-ERBα/β agonist with IC50s of 790 nM and 560 nM for REV-ERBα and REV-ERBβ, respectively.
  9. GPR119 receptors agonist

    PSN632408 is an optimized agonist of GPR119 receptors that shows similar potency to OEA at both recombinant mouse and human GPR119 receptors, exhibiting EC50 values of 5.6 and 7.9 uM, respectively.
  10. CRTH2 antagonist

    MK-7246 is a potent and selective CRTH2 antagonist with a Ki of 2.5??0.5 nM.
  11. S1P1 agonist

    Cenerimod (ACT-334441) is a potent and orally available sphingosine 1-phosphate 1 receptor (S1P1) agonist extracted from patent WO 2016184939 A1 and WO 2011007324 A1, example 1, with an EC50 of 2.7 nM.
  12. mGluR4 PAM

    ADX88178 is a potent metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 4 nM for human mGluR4.
  13. monoamine reuptake inhibitor

    Diclofensine hydrochloride (Ro-8-4650 hydrochloride) is a potent inhibitor of monoamine reuptake, blocking the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3, and 3.7 nM, respectively.
  14. Smo inhibitor

    LEQ506 is a second-generation inhibitor of smoothened (Smo) with IC50s of 2 and 4 nM in human and mouse, respectively.
  15. mGlu5 antagonist

    Auglurant (VU0424238) is a novel and selective mGlu5 antagonist with an IC50 value of 11 nM (rat) and an IC50 value of 14 nM (human). Auglurant (VU0424238) has an acceptable CNS penetration.
  16. histamine 1 receptor antagonist

    Decloxizine(UCB-1402; NSC289116) is a histamine 1 receptor antagonist.
  17. angiotensin-(1-7) receptor agonist

    AVE 0991 is a nonpeptide and orally active angiotensin-(1-7) receptor agonist with an IC50 of 21 nM.
  18. group II (mGlu2/3) receptor agonist

    Eglumegad (LY354740) is a highly potent and selective group II (mGlu2/3) receptor agonist with IC50s of 5 and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively.
  19. A1 receptor agonist

    N6-Cyclohexyladenosine is a selective A1 receptor agonist (EC50 = 8.2 nM).
  20. Smo antagonist

    MRT-83 is a potent antagonist of Smo, with an IC50 in the nanomolar range. MRT-83 also blocks Hedgehog (Hh) signaling.
  21. CysLT1/CysLT2 antagonist

    Gemilukast is an orally active and potent dual cysteinyl leukotriene 1 and 2 receptors (CysLT1 and CysLT2) antagonist, with IC50s of 1.7, 25 nM for human CysLT1 and CysLT2, respectively.
  22. guanylate cyclase stimulator

    Vericiguat (BAY1021189) is a potent, orally available and soluble guanylate cyclase stimulator.
  23. DP1/EP2 agonist

    Treprostinil sodium is a potent DP1 and EP2 agonist with EC50 values of 0.6??0.1 and 6.2??1.2 nM, respectively.
  24. histamine H4 receptor antagonist

    Toreforant is a potent and selective histamine H4 receptor (H4R) antagonist, with a Ki at the human receptor of 8.4 nM.
  25. A2AR/ENT1 agonist

    A2AR-agonist-1 is a potent A2AR and ENT1 agonist with Ki of 4.39 and 3.47 for A2AR and ENT1.
  26. IP receptor agonist

    Ralinepag is a potent, orally bioavailable and non-prostanoid prostacyclin (IP) receptor agonist, with EC50s of 8.5 nM, 530 nM and 850 nM for human and rat IP receptor and human DP1 receptor, respectively.
  27. endothelin receptor type B (ETB) agonist

    IRL-1620 is a potent and selective endothelin receptor type B (ETB) agonist with a Ki of 16 pM.
  28. Sigma-1 receptor agonist/muscarinic M1 agonist

    Blarcamesine, also known as AVex-73 and AE-37, is a muscarinic M1 agonist potentially for the treatment of Alzheimer's disease. It is an ς receptor ligand.
  29. dual NE/DA transporter inhibitor

    Centanafadine is dual norepinephrine (NE)/dopamine (DA) transporter inhibitor, also inhibits serotonin transporter, with IC50s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively.
  30. mGlu2 receptor agonist

    LY2812223 is a highly potent, functionally selective mGlu2 receptor agonist with mGlu2 binding affinity for mGlu2 and mGlu3 (Ki=144 nM and 156 nM, respectively).
  31. endothelin (ET) receptor antagonist

    Tezosentan (RO 610612) is an endothelin (ET) receptor antagonist, with pA2s of 9.5, 7.7 for ETA and ETB receptors, respectively.
  32. PGE2 agonist

    Evatanepag (CP-533536) is an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation with EC50 of 0.3 nM.
  33. sigma 1 receptor agonist

    Cutamesine (SA4503; AGY-94806) is a selective sigma 1 receptor(??1R) agonist; high affinity for the sigma 1 receptor subtype labeled by (+)-[3H]pentazocine (IC50= 17.4??1.9 nM); 100-fold less affinity for the sigma 2 receptor.
  34. FFAR1/GPR40 activator

    GPR40 Activator 1 is a potent GPR40 activator for treatment of type 2 diabetes.
  35. CXCR3 antagonist

    NBI-74330 is a potent antagonist for CXCR3, and exhibits potent inhibition of (125I)CXCL10 and (125I)CXCL11 specific binding with Ki of 1.5 and 3.2 nM, respectively.
  36. group III mGluR receptors agonist

    O-Phospho-L-serine is the immediate precursor to L-serine in the serine synthesis pathway, and an agonist at the group III mGluR receptors (mGluR4, mGluR6, mGluR7, and mGluR8); O-Phospho-L-serine also acts as a weak antagonist for mGluR1 and a potent antagonist for mGluR2.
  37. FFAR1/GPR40 agonist

    AMG 837 is a potent GPR40 agonist (EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.

  38. CXCR3 antagonist

    AMG 487 is an orally active and selective antagonist of CXC chemokine receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively.
  39. TGR5 agonist

    INT-777 is a potent TGR5 agonist with an EC50 of 0.82 μM.
  40. Calcium-sensing receptor (CaR) antagonist

    SB-423557 is an orally active calcium-sensing receptor (CaR) antagonist (IC50=520 nM), precursor of SB-423562 (IC50=73 nM).
  41. NK3R antagonist

    Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist.
  42. AC1 inhibitor

    NB001 (HTS 09836) is an adenylcyclase 1 (AC1) inhibitor which has effect on neural and non-neural pain by modulating AC1 activity.
  43. 5-HT1A receptor agonist

    Befiradol (NLX-112) is a selective 5-HT1A receptor agonist.
  44. NPY Y5 receptor antagonist

    Velneperit (S-2367) is a novel neuropeptide Y (NPY) Y5 receptor antagonist.
  45. mGlu4 receptor modulator

    TCN238 is a positive allosteric mGlu4 receptor modulator with an EC50 of 1 μM.
  46. D3 receptor and D2 receptor partial agonist

    Cariprazine is a novel antipsychotic drug candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
  47. A2B receptor antagonist

    LAS101057 is a potent, selective, and orally efficacious A2B receptor antagonist.
  48. B1 receptor antagonist

    ELN-441958 is a potent, neutral antagonist of B1 receptor, inhibits the binding of the B1 agonist ligand [3H]DAKD to IMR-90 cells with Ki of 0.26 nM.
  49. PAR2 agonist

    AC-55541 is a highly selective protease-activated receptor 2 (PAR2) agonist (pEC50=6.7), displays no activity at other PAR subtypes or at over 30 other receptors involved in nociception and inflammation.
  50. BRS-3 agonist

    MK-5046 is a novel BRS-3 agonist, binds to BRS-3 with high affinity (mouse Ki = 1.6 nM, human Ki = 25 nM).

Items 1101-1150 of 6966

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