Home >> Research Area >> GPCR/G protein

GPCR/G protein

G protein–coupled receptors (GPCRs) which are also known as seven-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptor, and G protein–linked receptors (GPLR), constitute a large protein family of receptors, that detect molecules outside the cell and activate internal signal transduction pathways and, ultimately, cellular responses. Coupling with G proteins, they are called seven-transmembrane receptors because they pass through the cell membrane seven times.

Products for GPCR/G protein

  1. Cat.No. Product Name Information
  2. BCC6049 Lys-γ3-MSH Lys-γ3-MSH
  3. BCC7350 SNAP 5089 SNAP 5089
  4. BCC4494 Bosentan Hydrate Bosentan hydrate is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively. Bosentan Hydrate
  5. BCC1898 Rimonabant hydrochloride Rimonabant hHydrochloride (SR 141716A Hydrochloride) is a highly potent and selective central cannabinoid receptor (CB1) antagonist with an Ki of 1.8 nM. Rimonabant hHydrochloride (SR 141716A Hydrochloride) also inhibits Mycobacterial membrane protein Large 3 (MMPL3). Rimonabant hydrochloride
  6. BCC7001 GR 159897 GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK2) receptor antagonist. GR 159897 has little or no affinity for NK1 and NK3 receptors. GR 159897 inhibits binding of [3H]GR100679 to human NK2 (hNK2)-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects. GR 159897
  7. BCC7085 GR 231118 GR 231118
  8. BCC7392 APC 366 Tryptase inhibitor APC 366
  9. BCC7282 L-755,507 L755507 is a potent, selective agonist of β3-AR with an IC50 of 35 nM. L-755,507
  10. BCC7285 PNU 22394 hydrochloride PNU 22394 hydrochloride
  11. BCC6913 GR 55562 dihydrochloride GR 55562 dihydrochloride
  12. BCC1638 Ibutamoren Mesylate Ibutamoren (Mesylate) is a potent, non-peptide Growth hormone secretagogue receptor (GHSR) agonist. Ibutamoren Mesylate
  13. BCC8056 NIBR189 NIBR189 is a small molecule antagonist of the Epstein-Barr virus-induced gene 2 (EBI2; GPR183) receptor with IC50 of 16 nM(Binding) and 11 nM (Functional). NIBR189
  14. BCC7306 SCH 58261 SCH 58261 is a potent, selective and competitive antagonist of adenosine A2A receptor with an IC50 of 15 nM, and displays 323-, 53- and 100-fold more selective for A2A receptor than A1, A2B, and A3 receptors, respectively. SCH 58261
  15. BCC5822 BIM 23127 BIM 23127
  16. BCC7438 L-368,899 hydrochloride L-368,899 hydrochloride is a potent, selective, orally bioavailable, non-peptide oxytocin receptor antagonist, with IC50s of 8.9 nM and 26 nM for rat uterus and human uterus oxytocin receptor, respectively, used as a tocolytic agent. L-368,899 hydrochloride
  17. BCC6915 BW 723C86 hydrochloride 5-HT2B agonist BW 723C86 hydrochloride
  18. BCN2164 Silodosin Silodosin (KAD 3213; KMD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH. Silodosin
  19. BCC6001 GLP-1 (9-36) amide GLP-1 (9-36) amide
  20. BCC7353 L-371,257 L-371,257 is an orally bioavailable, non-blood-brain barrier penetrant, selective and competitive antagonist of oxytocin receptor (pA2=8.4) with high affinity at both the oxytocin receptor (Ki=19 nM) and vasopressin V1a receptor (Ki=3.7 nM). L-371,257
  21. BCC7385 Melperone hydrochloride Melperone hydrochloride
  22. BCC7523 CI 1020 CI 1020
  23. BCN2167 Fingolimod hydrochloride Fingolimod hydrochloride is a sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod hydrochloride also is a pak1 activator. Fingolimod hydrochloride
  24. BCC5538 K-Ras G12C-IN-1 K-Ras G12C-IN-1 is a novel and irreversible inhibitor of mutant K-ras G12C extracted from patent WO 2014152588 A1. K-Ras G12C-IN-1
  25. BCC5539 K-Ras G12C-IN-2 K-Ras G12C-IN-2 is an irreversible covalent K-Ras G12C inhibitor. K-Ras G12C-IN-2
  26. BCC5540 K-Ras G12C-IN-3 K-Ras G12C-IN-3 is a novel and irreversible inhibitor of mutant K-ras G12C. K-Ras G12C-IN-3
  27. BCC6938 2-Cl-IB-MECA 2-Cl-IB-MECA is a selective A3 adenosine receptor agonist (Ki = 0.33 nM). Displays 2500- and 1400-fold selectivity over A1 and A2A receptors respectively. 2-Cl-IB-MECA
  28. BCC6914 WIN 64338 hydrochloride Bradykinin B2 antagonist WIN 64338 hydrochloride
  29. BCC1353 AM630 6-Iodopravadoline (AM630) is a selective CB2 antagonist with Ki of 31.2 nM, and displays 165-fold selectivity over CB1 receptors. AM630
  30. BCC6339 SA 4503 dihydrochloride Cutamesine dihydrochloride (SA4503 dihydrochloride; AGY94806 dihydrochloride) is a potent Sigma 1 receptor agonist with an IC50 of 17.4 nM in guinea pig brain membranes. SA 4503 dihydrochloride
  31. BCC1525 Desmopressin Synthetic vasopressin analog; V1B and V2 agonist,Desmopressin(DDAVP) is the synthetic analogue of the antidiuretic hormone arginine vasopressin. Desmopressin
  32. BCC7164 R-96544 hydrochloride R-96544 hydrochloride
  33. BCC5694 RS 39604 hydrochloride RS 39604 hydrochloride
  34. BCC4414 Rimonabant Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial Rimonabant
  35. BCC6019 SHU 9119 SHU 9119 is a potent human melanocortin 3 and 4 receptors (MC3/4R) antagonist and a partial MC5R agonist; with IC50 values of 0.23, 0.06, and 0.09 nM for human MC3R, MC4R and MC5R, respectively. SHU 9119
  36. BCC3756 Conivaptan HCl Conivaptan (hydrochloride) is a non-peptide antagonist of vasopressin receptor, with Ki values of 0.48 and 3.04 nM for rat liver V1A receptor and rat kidney V2 receptor respectively. Conivaptan HCl
  37. BCC5693 RS 67333 hydrochloride RS 67333 hydrochloride
  38. BCC6878 RS 67506 hydrochloride 5-HT4 partial agonist RS 67506 hydrochloride
  39. BCC6874 RS 17053 hydrochloride RS 17053 hydrochloride is a potent and selective α1A adrenoceptor antagonist, with a pKi value of 9.1 in native cell membrane and a pA2 value of 9.8 in functional assays. RS 17053 hydrochloride
  40. BCC7192 IRL-2500 IRL 2500 is a potent Endothelin receptor antagonist. IRL 2500 shows IC50 values of 1.3 and 94 nM for ETB and ETA receptors, respectively. IRL 2500 inhibits ETB receptor-mediated blood pressure increase and renal vascular resistance in rats in vivo. IRL-2500
  41. BCC7196 Ro 60-0175 fumarate Ro 60-0175 fumarate
  42. BCC5686 Nociceptin Nociceptin, a heptadecapeptide, is the endogenous ligand of the nociceptin receptor, acting as a potent anti-analgesic. Nociceptin
  43. BCC5790 Astressin Astressin is a potent corticotropin releasing factor (CRF) antagonist. Astressin
  44. BCC7742 Donitriptan hydrochloride 5-HT1B/1D agonist Donitriptan hydrochloride
  45. BCC6697 N-Methylquipazine dimaleate N-Methylquipazine dimaleate
  46. BCC5789 Urocortin (rat) 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. Urocortin (rat)
  47. BCC7558 LY 272015 hydrochloride LY 272015 hydrochloride
  48. BCC7856 LY 266097 hydrochloride LY 266097 hydrochloride
  49. BCC7411 PB 28 dihydrochloride PB 28 dihydrochloride
  50. BCC5865 BWX 46 Highly selective NPY Y5 agonist BWX 46
  51. BCC7628 Rec 15/2615 dihydrochloride Rec 15/2615 dihydrochloride
  52. BCC7650 BGC 20-761 High affinity 5-HT6 antagonist BGC 20-761
  53. BCC7734 FR 171113 FR 171113
  54. BCC1379 Atrasentan Atrasentan
  55. BCC1795 Nepicastat Nepicastat (SYN117) is a selective, potent, and orally active inhibitor of dopamine-beta-hydroxylase. Nepicastat (SYN117) produces concentration-dependent inhibition of bovine (IC50=8.5 nM) and human (IC50=9 nM) dopamine-beta-hydroxylase. Nepicastat (SYN117) can cross the blood-brain barrier (BBB). Nepicastat
  56. BCC7037 SB 218795 SB 218795
  57. BCC1926 SB-222200 SB 222200 is a selective, reversible and competitive antagonist of human NK-3 receptor(Ki=4.4 nM) that effectively crosses the blood-brain barrier. SB-222200
  58. BCC1981 Talnetant Talnetant (SB 223412) is a potent and selective NK3 receptor antagonist (ki=1.4 nM, hNK-3-CHO); 100-fold selective for the hNK-3 versus hNK-2 receptor, with no affinity for the hNK-1 at concentrations up to 100 uM. Talnetant
  59. BCC5913 CH 275 CH 275
  60. BCC5788 Urocortin (human) Urocortin, human, a 40-aa neuropeptide, acts as a selective agonist of endogenous CRF2 receptor, with Kis of 0.4, 0.3, and 0.5 nM for hCRF1, rCRF2α and mCRF2β, respectively. Urocortin (human)
  61. BCC6709 Metergoline Metergoline is a psychoactive drug of the ergoline chemical class which acts as a ligand for various serotonin and dopamine receptors. Metergoline
  62. BCC7346 LY 320135 LY 320135
  63. BCC7781 R 568 hydrochloride Tecalcet Hydrochloride (R 568 Hydrochloride), an orally active calcimimetic compound, allosterically and positively modulates the calcium-sensing receptor (CaSR). Tecalcet Hydrochloride (R 568 Hydrochloride) increases the sensitivity to activation by extracellular Ca2+. R 568 hydrochloride
  64. BCC5749 Nociceptin (1-13)NH2 Nociceptin (1-13), amide is a potent ORL1 (OP4) receptor agonist with a pEC50 of 7.9 for mouse vas deferens and a Ki of 0.75 nM for binding to rat forebrain membranes. Nociceptin (1-13)NH2
  65. BCC6085 Orphanin FQ (1-11) Orphanin FQ (1-11)
  66. BCC5738 Nociceptin (1-7) Nociceptin (1-7)
  67. BCC5878 ZD 2079 ZD 2079
  68. BCC7069 N-Arachidonylglycine N-Arachidonylglycine
  69. BCC6883 AH 11110 hydrochloride AH 11110 hydrochloride
  70. BCC6976 SB 224289 hydrochloride SB-224289 hydrochloride is a selective 5-HT1B receptor antagonist, with anxiolytic effect. SB 224289 hydrochloride
  71. BCC7284 PD 160170 PD 160170
  72. BCC7036 SB 228357 SB228357 is a selective, potent oral active 5-HT2C/2B receptor antagonist with pKi values of 6.9, 8.0 and 9.0 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. SB228357 has antidepressant/anxiolytic effects. SB 228357
  73. BCC4412 AM251 AM251 is a selective cannabinoid 1 (CB1) receptor antagonist with an IC50 of 8 nM, also acts as a potent GPR55 agonist with an EC50 of 39 nM. AM251
  74. BCC5823 CYN 154806 CYN 154806, a cyclic octapeptide, is a potent and selective somatostatin sst2 receptor antagonist, with pIC50 values of 8.58, 5.41, 6.07, 5.76 and 6.48 for human recombinant sst2, sst1, sst3, sst4 and sst5 receptors respectively. CYN 154806
  75. BCC6972 MRS 1220 MRS 1220
  76. BCC1951 sitaxsentan Sitaxsentan (IPI 1040; TBC-11251) is a selective endothelin A (ETA) receptor antagonist. sitaxsentan
  77. BCC7323 SR 142948 SR 142948
  78. BCC6014 R 715 R 715
  79. BCC5679 GR 46611 GR 46611
  80. BCC5182 AMD 3465 hexahydrobromide AMD 3465 hexahydrobromide (GENZ-644494 hexahydrobromide) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses. AMD 3465 hexahydrobromide
  81. BCC5181 AMD 3465 AMD 3465 is a potent, selective CXCR4 antagonist, and inhibits SDF-1α-ligand binding with Ki of 41.7 nM. AMD 3465
  82. BCC6876 RS 79948 hydrochloride RS 79948 hydrochloride
  83. BCC2524 Zibotentan (ZD4054) Zibotentan (ZD4054) is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM). Zibotentan (ZD4054)
  84. BCC7695 ML 10302 hydrochloride ML 10302 hydrochloride
  85. BCC7408 PNU 109291 PNU 109291
  86. BCC7222 PNU 142633 PNU-142633 is a high affinity, selective and orally active 5-HT1D receptor agonist with Kis of 6 nM and > 18 000 nM for human 5-HT1D receptor and human 5-HT1B receptor, respectively. PNU-142633 has anti-migraine efficacy. PNU 142633
  87. BCC7500 Arachidonyl serotonin Arachidonyl serotonin
  88. BCC5704 NocII NocII
  89. BCC7059 MAFP MAFP (Methyl Arachidonyl Fluorophosphonate) is an selective, active-site directed and irreversible inhibitor of cPLA2 and iPLA2. MAFP is also a potent irreversible inhibitor of anandamide amidase. MAFP
  90. BCC1919 Salmefamol Salmefamol
  91. BCC7955 Tegaserod maleate Tegaserod maleate is a partial agonist of the 5-HT4 receptor; stimulates the peristaltic reflex and accelerates gastrointestinal transit. Tegaserod maleate
  92. BCC7187 Palmitoylisopropylamide Palmitoylisopropylamide
  93. BCC6836 GR 135531 GR 135531
  94. BCC6194 AT 1015 Long-acting 5-HT2A antagonist AT 1015
  95. BCC7325 L-168,049 L-168,049
  96. BCC7355 BIBO 3304 trifluoroacetate BIBO3304 TFA is a potent, orally active, and selective neuropeptide Y (NPY) Y1 receptor antagonist, with subnanomolar affinity for both the human and the rat Y1 receptor (IC50=0.38 and 0.72 nM, respectively). BIBO 3304 trifluoroacetate
  97. BCC7270 NTNCB hydrochloride NTNCB hydrochloride
  98. BCC5753 MRS 1334 MRS 1334
  99. BCC4081 Prazosin Prazosin is an alpha-adrenergic blocker and is a sympatholytic drug used to treat high blood pressure and anxiety, PTSD, and panic disorder. Prazosin
  100. BCC7283 CGP 71683 hydrochloride CGP71683 hydrochloride is a competitive neuropeptide Y5 receptor antagonist with a Ki of 1.3 nM, and shows no obvious activity at Y1 receptor (Ki, >4000 nM) and Y2 receptor (Ki, 200 nM) in cell membranes. CGP 71683 hydrochloride
  101. BCC2505 Prazosin HCl Prazosin hydrochloride is an alpha-adrenergic blocker and is a sympatholytic drug used to treat high blood pressure and anxiety, PTSD, and panic disorder. Prazosin HCl

Items 301 to 400 of 944 total