GPCR/G Protein

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  1. Dopamine D2 Receptor Antagonist

    SB269652 is a new chemical probe that can differentiate D2R monomers from dimers or oligomers depending on the observed pharmacology.
  2. CXCR2 antagonist

    SB 265610 is a nonpeptide, allosteric, inverse agonist of CXCR2 (Kd = 2.51 nM) that prevents receptor activation by binding to a region distinct from the agonist binding site. It does not bind to the related CXCR1 receptor.1 It has been shown to prevent neutrophil chemotaxis both in vitro and in a rat model of hyperoxia-induced lung injury.
  3. angiotensin receptor-neprilysin inhibitor

    LCZ696 is an orally bioavailable, dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) for hypertension and heart failure.
  4. CXCR2 antagonist

    SB225002 is a potent, and selective CXCR2 antagonist with IC50 of 22 nM for inhibiting interleukin IL-8 binding to CXCR2, > 150-fold selectivity over the other 7-TMRs tested.
  5. β2-adrenoceptor agonist

    Salmeterol Xinafoate is a long-acting β2-adrenergic receptor agonist with anti-inflammatory effect.
  6. EPAC1/EPAC2 inhibitor

    ESI-09 is a specific exchange protein directly activated by cAMP (EPAC) inhibitor with IC50 of 3.2 uM and 1.4 uM for EPAC1 and EPAC2,
  7. Histamine H1 receptor antagonist

    Promethazine HCl is a potent histamine H1 receptor antagonist.
  8. β-adrenoceptor agonist

    Bambuterol HCl is a potent β-adrenoceptor agonist, used in the treatment of asthma.
  9. 5-HT2 receptor antagonist

    Cyclobenzaprine HCl is a muscle relaxant by blocking pain sensations.
  10. I(1) imidazoline receptor agonist

    Rilmenidine Phosphate is a selective I(1) imidazoline receptor agonist.
  11. β-adrenoceptor antagonist

    Carteolol HCl is a β-adrenoceptor antagonist
  12. EPAC2 inhibitor

    HJC0350 is a potent and selective EPAC2 inhibitor with IC50 of 0.3 μM, exhibiting no inhibition on Epac1.
  13. Adenosine A Receptor antagonist

    CGS 15943 is a potent, non-selective Adenosine A Receptor antagonist. It is orally active in vivo.
  14. mGluR-2 modulator

    JNJ-42153605 is a positive allosteric modulator of the metabotropic glutamate 2 receptor.
  15. neuropeptide Y Y2 receptor antagonist

    JNJ-31020028 is a novel, selective, brain-penetrant neuropeptide Y Y2 receptor antagonist
  16. Capromorelin functions as a growth hormone secretagogue and ghrelin mimetic which causes the body to secrete human growth hormone in a way usually seen at puberty and in young adulthood.
  17. 5-HT6 receptor antagonist

    LuAE58054 is a potent and selective 5-HT6 receptor antagonist under development by Lundbeck as an augmentation therapy for the treatment of cognitive deficits associated with Alzheimer's disease and schizophrenia.
  18. ETBR antagonist

    BQ-788 sodium salt is a selective ETBR (Endothelin receptor B ) antagonist.
  19. 5-HT3 receptor antagonist

    Tropisetron is a selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ?? 0.9 nM for 5-HT3 receptor.
  20. Dopamine receptor agonist

    (+)-PD 128907 hydrochloride is a potent D3DR (dopamine receptor) agonist (Ki = 2.3 nM).
  21. serotonin/NE reuptake inhibitor

    Levomilnacipran HCl is a selective serotonin and norepinephrine reuptake inhibitor.
  22. Adenosine A3 receptor agonist

    CF-102 is an orally bioavailable, synthetic, highly selective adenosine A3 receptor (A3AR) agonist with potential antineoplastic activity.
  23. CCR1 antagonist

    BX471 is a potent, selective non-peptide CCR1 antagonist (Ki = 1 nM for human CCR1), exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.
  24. NK1 receptor antagonist

    Netupitant is a selective neurokinin 1 (NK1) receptor antagonist. It competitively binds to and blocks the activity of the human substance P/NK1 receptors in the central nervous system (CNS), thereby inhibiting NK1-receptor binding of the endogenous tachykinin neuropeptide substance P (SP), which may result in the prevention of chemotherapy-induced nausea and vomiting (CINV).
  25. 5-HT2A receptor agonist

    Pimavanserin is a potent and selective 5-HT2A receptor inverse agonist with mean pIC50 of with 8.7 in the cell-based functional assay.
  26. FFA4/GPR120 agonist

    GSK137647A is a selective FFA4 agonist, with pEC50 of 6.3, 6.2, and 6.1 for human, Mouse and Rat FFA4, respectively.
  27. 5-HT1F receptor agonist

    LY 344864 racemate is a 5-HT1F receptor agonist.
  28. CNS penetrant mGlu7/8 receptor agonist

    VU6005649 is a CNS penetrant mGlu7/8 receptor agonist with EC50s of 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively.
  29. 5-HT1F antagonist

    LY 334370 hydrochloride is a selective 5-HT1F receptor agonist (Ki values are 1.87, 16.4, > 100 (IC50)). CAS: 199673-74-0(LY 334370 hydrochloride); 182563-08-2 (LY 334370 Free Base)
  30. H4 receptor antagonist

    JNJ-39758979 is histamine H4 receptor antagonists with a Ki of 12.5 nM.
  31. GPR39 agonist

    TM N1324 is an agonist of G-Protein-Coupled Receptor 39 (GPR39) with EC50s of 9 nM/5 nM in the presence of Zn2+, and 280 nM/180 nM in the absence of Zn2+ for human/murine GPR39.
  32. α1 adrenoreceptor antagonist

    Urapidil is an α1 adrenoreceptor antagonist and a 5-HT1A receptor agonist.
  33. 5-HT(2A) receptor agonist

    Temanogrel, also known as APD791, is a highly selective 5-hydroxytryptamine2A receptor inverse agonist under development for the treatment of arterial thrombosis.
  34. EP1 receptor antagonist

    GSK-269984A is a novel EP1 receptor antagonist.
  35. opioid receptor antagonis

    Bevenopran, also known as CB-5945, ADL-5945, MK-2402, OpRA III, is a peripherally selective μ- and δ-opioid receptor antagonist.
  36. Neuronostatin-13 human is a 13-amino acid peptide hormone encoded by the somatostatin gene and plays an important role in the regulation of hormonal and cardiac function.
  37. Rev-Erbα agonist

    GSK4112 is a selective Rev-Erbα agonist with EC50 value of 250 nM.
  38. OX2 receptor antagonist

    TCS-OX2-29 is a selective OX2 receptor antagonist with IC50 value of 40 nM. CAS: 1610882-30-8 (HCl) 372523-75-6 (Free Base)
  39. IP (prostacyclin) receptor antagonist

    RO-1138452 is a potent and selective IP (prostacyclin) receptor antagonist with high affinity for IP receptors.
  40. sigma1 receptor agonist

    Anavex2-73 is a muscarinic/moderate sigma1 receptor agonist that alleviated the scopolamine- and dizocilpine-induced learning impairments. CAS: 195615-83-9 (Free base) 195615-84-0 (HCl)
  41. histamine H3 receptors agonist

    S38093 is an inverse agonist at histamine H3 receptors. CAS: 862896-30-8 (Free base) 1222097-72-4 (HCl)
  42. CXCR4 Antagonist

    MSX-130 is CXCR4 antagonist.
  43. CXCR4 receptor modulator

    NSC-23026 is a CXCR4 receptor modulator.
  44. GPCR19 antagonist

    SBI-115 is a TGR5 (GPCR19) antagonist. SBI-115 decreases hepatic cystogenesis with polycystic liver diseases via inhibiting TGR5.
  45. CRTh2 receptor antagonist

    Fevipiprant, also known as NVP-QAW039 or QAW039, is an oral active and potent CRTh2 receptor antagonist and potentially useful for asthma treatment.
  46. beta-adrenergic receptor antagonist

    Nifenalol, also known as INPEA, is a new beta-adrenergic receptor antagonist.
  47. α-adrenoceptor agonist

    Xylometazoline hydrochloride is an α-adrenoceptor agonist commonly used as nasal decongestant.
  48. alpha-adrenergic receptor agonist / MAO inhibitor

    Amitraz, also known as Mitaban and Taktic, is an alpha-adrenergic receptor agonist and MAO inhibitor used as an insecticide in prevention of flea and tick infections. It prevents prostaglandin synthesis and may inhibit beta-cell insulin release.
  49. 5-HT2 antagonist

    Sarpogrelate hydrochloride (MCI-9042), a selective 5-HT2 antagonist, has been widely used as an anti-platelet agent for the treatment of PAD.
  50. D2DR and D4DR inhibitor

    Loxapine Succinate is a D2DR and D4DR inhibitor and serotonergic receptor antagonist. Loxapine succinate is an antipsychotic agent used in schizophrenia.

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