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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. BCC6962 PACAP 1-38 PACAP (1-38), human, ovine, rat is a neuropeptide with 38 amino acid residues. PACAP (1-38) binds to PACAP type I receptor, PACAP type II receptor VIP1, and PACAP type II receptor VIP2 with IC50s of 4 nM, 2 nM, and 1 nM, respectively. PACAP 1-38
  3. BCC7490 Alprenolol hydrochloride Alprenolol (hydrochloride) is a non-selective beta blocker as well as 5-HT1A receptor antagonist. Alprenolol hydrochloride
  4. BCC6286 BETP BETP is an agonist of glucagon-like peptide-1 (GLP-1) receptor, with EC50s of 0.66 and 0.755 μM for human and rat GLP-1 receptor, respectively. BETP
  5. BCC7101 LY 215840 LY 215840
  6. BCC6235 TUG 891 TUG-891is a potent and selective agonist for the long chain free fatty acid (LCFA) receptor 4 (FFA4/GPR120). TUG 891
  7. BCC5994 [Lys5,MeLeu9,Nle10]-NKA(4-10) [Lys5,MeLeu9,Nle10]-NKA(4-10)
  8. BCC5800 GR 64349 GR 64349
  9. BCC5933 BIM 187 BIM 187
  10. BCC5017 Valsartan Valsartan (CGP-48933) is an angiotensin II receptor antagonist for the treatment of high blood pressure and heart failure. Valsartan
  11. BCC5095 Mozavaptan Mozavaptan (OPC-31260) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment. Mozavaptan
  12. BCC6238 CYM 9484 CYM 9484 is a selective and highly potent neuropeptide Y (NPY) Y2 receptor antagonist with an IC50 value of 19 nM. CYM 9484
  13. BCC6674 BD 1008 dihydrobromide BD 1008 dihydrobromide
  14. BCC6863 BD 1047 dihydrobromide BD-1047 (dihydrobromide) is a selective functional antagonist of sigma-1 receptor, shows antipsychotic activity in animal models predictive of efficacy in schizophrenia. BD 1047 dihydrobromide
  15. BCC2560 Irbesartan Irbesartan is a highly potent and specific angiotensin II type 1 (AT1) receptor antagonist with IC50 of 1.3 nM. Irbesartan
  16. BCC6266 LP 20 hydrochloride LP 20 hydrochloride
  17. BCC5863 JMV 449 JMV 449
  18. BCC6726 2-PMDQ 2-PMDQ
  19. BCC6902 ZM 241385 ZM241385 is a potent, high affinity and selective adenosine A2a receptor (A2AR) antagonist with a Ki value of 1.4 nM. ZM 241385
  20. BCC7877 MDL 100907 Volinanserin is a potent and selective antagonist of 5-HT2 receptor, with a Ki of 0.36 nM, and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 and DA D2 receptors. Volinanserin has antipsychotic activity. MDL 100907
  21. BCC1840 PB-22 PB-22
  22. BCC2018 TUG-770 TUG-770 is a highly potent free fatty acid receptor 1 (FFA1/GPR40) agonist with EC50 of 6 nM for hFFA1. TUG-770
  23. BCC5688 ICI 215,001 hydrochloride ICI 215,001 hydrochloride
  24. BCC1854 PF-543 PF-543 (Sphingosine Kinase 1 Inhibitor II) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 is >100-fold selectivity for SPHK1 over SPHK2. PF-543 is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 induces apoptosis, necrosis, and autophagy. PF-543
  25. BCC5799 GR 94800 GR 94800
  26. BCC5763 Galanin (2-29) (rat) Galanin (2-29) (rat)
  27. BCC6994 SDZ SER 082 fumarate SDZ SER 082 fumarate
  28. BCC1568 Exendin-4 Exendin-4 (Exenatide), a 39 amino acid peptide, is a long-acting glucagon-like peptide-1 receptor agonist with an IC50 of 3.22 nM. Exendin-4
  29. BCC5934 BIM 189 BIM 189
  30. BCC6337 CYM 50769 CYM 50769
  31. BCC5733 FR 139317 FR 139317
  32. BCC5728 BQ-3020 Selective ETB agonist BQ-3020
  33. BCC1929 SB-408124 Hydrochloride SB-408124 Hydrochloride is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively; exhibits 50-fold selectivity over OX2 receptor. SB-408124 Hydrochloride
  34. BCC7813 WAY 267464 dihydrochloride WAY 267464 dihydrochloride
  35. BCC6877 RS 56812 hydrochloride RS 56812 hydrochloride
  36. BCC7611 PACAP 6-38 PACAP (6-38), human, ovine, rat is a potent PACAP receptor antagonist with IC50s of 30, 600, and 40 nM for PACAP type I receptor, PACAP type II receptor VIP1, and PACAP type II receptor VIP2, respectively. PACAP 6-38
  37. BCC5751 SB 200646 hydrochloride SB 200646 hydrochloride
  38. BCC7686 M40 M40 is a potent, non-selective galanin receptor antagonist. M40
  39. BCC4658 Eprosartan Mesylate Eprosartan mesylate (SKF-108566J) is a nonpeptide angiotensin II receptor antagonist with IC50 of 9.2 and 3.9 nM in rat and human adrenal cortical membranes, respectively. Eprosartan Mesylate
  40. BCC5730 IRL-1038 IRL-1038
  41. BCC7019 GR 113808 GR 113808 is a potent and highly selective 5-HT4 receptor antagonist (pKb= 8.8). GR 113808 shows 300-fold selectivity over 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C and 5-HT3 receptors. GR 113808
  42. BCC1819 Olmesartan Olmesartan (RNH-6270) is an angiotensin II receptor (AT1R) antagonist used to treat high blood pressure. Olmesartan
  43. BCC6678 4F 4PP oxalate 4F 4PP oxalate
  44. BCC7437 L-703,664 succinate L-703,664 succinate
  45. BCC7386 MRS 2693 trisodium salt MRS 2693 trisodium salt
  46. BCC7052 YM 022 YM022 is a highly potent, selective and orally active gastrin/cholecystokinin (CCK)-B receptor (CCK-BR) antagonist. YM022 shows the Ki values of 68 pM and 63 nM for CCK-B and CCK-A receptor, respectively. YM022 can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo. YM 022
  47. BCC4347 Dexmedetomidine HCl Dexmedetomidine Hydrochloride is an agonist of adrenergic alpha-2 receptor, which is used in veterinary medicine for its analgesic and sedative properties. Dexmedetomidine HCl
  48. BCC7305 L-692,585 L-692,585
  49. BCC5685 MRS 2179 tetrasodium salt MRS 2179 tetrasodium salt
  50. BCC6004 AR-C 66096 tetrasodium salt Potent and selective P2Y12 antagonist AR-C 66096 tetrasodium salt
  51. BCC7575 2-Chloroadenosine 2-Chloroadenosine, a stable adenosine analogue, protects against long term development of ischaemic cell loss in the rat hippocampus. 2-Chloroadenosine is an apparent competitive inhibitor of uridine influx (apparent Ki=33 μM) and high-affinity nitrobenzylthioinosine binding (apparent Ki=0.18 mM). 2-Chloroadenosine is a transported permeant for the nucleoside transporter in human erythrocytes. 2-Chloroadenosine
  52. BCC5941 SC 51322 SC 51322
  53. BCC7773 SC 51089 SC 51089
  54. BCC7763 SR 48692 Meclinertant (SR 48692) is a potent, selective, nonpeptide and orally active neurotensin receptor 1 (NTS1) antagonist. In human colon carcinoma (HT-29) cells, Meclinertant competitively antagonizes neurotensin-induced intracellular Ca2+ mobilization with a pA2 values of 8.13. Meclinertant has anxiolytic, anti-addictive and memory-impairing effects. SR 48692
  55. BCC7536 1-Methylpsilocin 1-Methylpsilocin
  56. BCC7180 SR 2640 hydrochloride SR 2640 hydrochloride
  57. BCC5734 ZD 7155 hydrochloride ZD 7155 hydrochloride is an angiotensin II receptor type 1 (AT1 receptor) antagonist. ZD 7155 hydrochloride
  58. BCC5562 K-Ras(G12C) inhibitor 12 K-Ras(G12C) inhibitor 12 is a K-Ras(G12C) inhibitor, the half-maximum effective concentration (EC50) for K-Ras(G12C) inhibitor 12 in H1792 cells is 0.32 μM. K-Ras(G12C) inhibitor 12
  59. BCC6248 TT 232 TT 232
  60. BCC5014 Azilsartan Azilsartan(TAK-536) is a specific and potent angiotensin II type 1 receptor antagonist with IC50 of 2.6 nM. Azilsartan
  61. BCC5772 LY 288513 LY 288513
  62. BCC4640 Bosentan Bosentan 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
  63. BCC7640 8-(3-Chlorostyryl)caffeine 8-(3-Chlorostyryl)caffeine
  64. BCC7393 L-161,982 L-161982 is a selective EP4 receptor antagonist. L-161982 completely blocks PGE2-induced ERK phosphorylation and cell proliferation of HCA-7 cells. L-161982 alleviates collagen-induced arthritis in mice. L-161,982
  65. BCC4304 Siramesine Siramesine(Lu 28-179) is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo. Siramesine
  66. BCC6048 GRK2i GRK2i
  67. BCC7081 GR 127935 hydrochloride GR 127935 hydrochloride
  68. BCC5752 SB 204070 SB 204070
  69. BCC4350 Ivabradine HCl Ivabradine hydrochloride is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker. Ivabradine HCl
  70. BCC7573 NE 100 hydrochloride NE 100 hydrochloride
  71. BCC4088 AHU-377(Sacubitril) Sacubitril (AHU-377) is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril (AHU-377) is a component of the heart failure medicine LCZ696. AHU-377(Sacubitril)
  72. BCC6767 RS 23597-190 hydrochloride RS 23597-190 hydrochloride
  73. BCC6741 2-MPMDQ 2-MPMDQ
  74. BCC5824 BIM 23056 sst receptor ligand BIM 23056
  75. BCC6727 Quipazine dimaleate Quipazine dimaleate
  76. BCC7324 SR 49059 SR 49059
  77. BCC7514 MRS 2690 MRS 2690
  78. BCC5096 Tolvaptan Tolvaptan is a selective, competitive arginine vasopressin receptor 2 antagonist with an IC50 of 1.28μM for the inhibition of AVP-induced platelet aggregation. Tolvaptan
  79. BCC7091 CL 316243 disodium salt CL 316243 disodium salt
  80. BCC7774 CP 135807 CP 135807
  81. BCC4680 Montelukast Sodium Montelukast (sodium) (MK0476) is a potent, selective CysLT1 receptor antagonist. Montelukast Sodium
  82. BCC6018 AC 187 Potent and selective amylin receptor antagonist AC 187
  83. BCC6748 2-Phenylmelatonin 2-Phenylmelatonin
  84. BCC7336 A 80426 mesylate A 80426 mesylate
  85. BCC7035 SB 204741 SB 204741
  86. BCC4332 Nebivolol Nebivolol hydrochloride selectively inhibits β1- adrenergic receptor with IC50 of 0.8 nM. Nebivolol
  87. BCC7237 PSB 1115 PSB 1115
  88. BCC7068 BMY 45778 Non-prostanoid prostacyclin IP receptor partial agonist BMY 45778
  89. BCC7690 [D-Trp34]-Neuropeptide Y [D-Trp34]-Neuropeptide Y
  90. BCC8025 NBOH-2C-CN hydrochloride NBOH-2C-CN hydrochloride
  91. BCC6359 ANQ 11125 Selective motilin receptor antagonist ANQ 11125
  92. BCC7429 PD 144418 oxalate PD 144418 is a highly affinity, potent and selective sigma 1 (σ1) receptor ligand (Ki values of 0.08 nM and 1377 nM for σ1 and σ2 respectively), devoid of any significant affinity for other receptors, ion channels and enzymes. PD 144418 shows potential antipsychotic activity. PD 144418 oxalate
  93. BCC7576 BAY-u 9773 Dual CysLT1 and CysLT2 antagonist BAY-u 9773
  94. BCC6784 N-[2-(Piperidinylamino)ethyl]-4-iodobenzamide N-[2-(Piperidinylamino)ethyl]-4-iodobenzamide
  95. BCC6780 SM-21 maleate SM-21 maleate
  96. BCC6771 2-[1-(4-Piperonyl)piperazinyl]benzothiazole 2-[1-(4-Piperonyl)piperazinyl]benzothiazole
  97. BCC4447 Plerixafor 8HCl (AMD3100 8HCl) Plerixafor octahydrochloride (AMD3100 octahydrochloride) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor 8HCl (AMD3100 8HCl)
  98. BCC4948 Bimatoprost Bimatoprost is a prostaglandin analog used topically (as eye drops) to control the progression of glaucoma and in the management of ocular hypertension. Bimatoprost
  99. BCC3798 Istradefylline (KW-6002) Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease. Istradefylline (KW-6002)
  100. BCC6779 PG-9 maleate PG-9 maleate
  101. BCC6777 4-IBP 4-IBP is a selective σ1 agonist with a high level of affinity for the σ1 receptor (Ki = 1.7 nM) and a moderate affinity for the σ2 receptor (Ki = 25.2 nM) . 4-IBP

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