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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. BCC5870 GIP (human) Gastric Inhibitory Peptide (GIP), human is thought to act as an inhibitor of gastric functions. GIP (human)
  3. BCC3702 TAK-875 Fasiglifam (TAK-875) is a potent, selective and orally bioavailable GPR40 agonist with EC50 of 72 nM. TAK-875
  4. BCC7218 AS 19 AS19 is a potent, selective 5-HT7 receptor agonist with an IC50 value of 0.83 nM and a Ki of 0.6 nM. AS19 is selective for 5-HT7 over 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT5A receptors (Kis = 89.7 nM, 490 nM, 6.6 nM and 98.5 nM, respectively). AS19 enhances memory consolidation and reverses Scopolamine- or Dizocilpine-induced amnesia. AS 19
  5. BCC8010 GSK 1562590 hydrochloride GSK 1562590 hydrochloride
  6. BCC5958 Gastrin I (human) Gastrin-1, human is the endogenous peptide produced in the stomach, and increases gastric acid secretion via cholecystokinin 2 (CCK2) receptor. Gastrin I (human)
  7. BCC7804 NF 546 NF546 is a selective non-nucleotide P2Y11 agonist with a pEC50 of 6.27. NF546 stimulates release of interleukin-8 from human monocyte-derived dendritic cells. NF 546
  8. BCC1757 MK-2894 MK-2894 is a highly potent and selective second generation EP4 antagonist. MK-2894
  9. BCC1758 MK-2894 sodium salt MK-2894 sodium salt is a highly potent and selective second generation EP4 antagonist. MK-2894 sodium salt
  10. BCC7178 Zacopride hydrochloride Zacopride hydrochloride
  11. BCC7604 CP 376395 hydrochloride CP 376395 hydrochloride
  12. BCC6618 N-Acetyltryptamine N-Acetyltryptamine
  13. BCC5438 LPA2 antagonist 1 LPA2 antagonist 1 is a LPA2 antagonist with an IC50 of 17 nM. LPA2 antagonist 1
  14. BCC6649 DPCPX DPCPX
  15. BCC7599 PSB 0788 PSB 0788
  16. BCC5968 [D-p-Cl-Phe6,Leu17]-VIP [D-p-Cl-Phe6,Leu17]-VIP
  17. BCC1760 MK-4305 MK-4305
  18. BCC6366 CTCE 9908 CTCE 9908
  19. BCC5845 Kinetensin (human) Kinetensin is a neurotensin-like peptide isolated from pepsin-treated human plasma. Kinetensin (human)
  20. BCC7156 L-655,240 L-655,240
  21. BCC3786 GSK1292263 GSK1292263 is a novel GPR119 receptor agonist used for the treatment of type 2 diabetes. GSK1292263
  22. BCC7319 Devazepide Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC50s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders. Devazepide
  23. BCC4329 Maprotiline HCl Maprotiline hydrochloride is a selective noradrenalin re-uptake inhibitor and a tetracyclic antidepressant. Maprotiline HCl
  24. BCC7716 (±)-5'-Chloro-5'-deoxy-ENBA Highly selective A1 agonist (±)-5'-Chloro-5'-deoxy-ENBA
  25. BCC1732 MBX-2982 MBX-2982 is a selective, orally-available G protein-coupled receptor 119 (GPR119) agonist. MBX-2982
  26. BCC7521 Atipamezole hydrochloride Atipamezole hydrochloride is a synthetic α2-adrenoceptor antagonist with a Ki of 1.6 nM. Atipamezole hydrochloride
  27. BCC4344 Bisoprolol fumarate (±)-Bisoprolol (hemifumarate) is a selective type β1 adrenergic receptor blocker. Bisoprolol fumarate
  28. BCC7157 CGS 15943 CGS 15943 is an orally bioavailable non-xanthine Adenosine Receptor antagonist. Its Ki for human A1, A2A, A2B, and A3 Adenosine Receptors are 3.5, 4.2, 16, and 50 nM in transfected CHO cells, respectively. . CGS 15943
  29. BCC7973 Strontium chloride Strontium chloride
  30. BCC7800 MRS 2768 tetrasodium salt MRS 2768 tetrasodium salt
  31. BCC6282 COR 170 COR 170
  32. BCC4091 Tranilast Sodium Tranilast is an antiallergic agent. Tranilast Sodium
  33. BCC1599 GPR120 modulator 1 GPR120 modulator 1 is useful for modulating G protein-coupled receptor 120 (GPR120). GPR120 modulator 1
  34. BCC1600 GPR120 modulator 2 GPR120 modulator 2 is useful for modulating G protein-coupled receptor 120 (GPR120). GPR120 modulator 2
  35. BCC6281 Q94 hydrochloride Q94 hydrochloride
  36. BCC6095 PSB 0739 PSB 0739
  37. BCC7335 WEB 2086 Apafant (WEB 2086), a potent platelet-activating factor (PAF) antagonist, inhibits PAF binding to human PAF receptors with a Ki of 9.9 nM. WEB 2086
  38. BCC6728 Spiroxatrine Spiroxatrine
  39. BCC5759 BMY 14802 hydrochloride BMY 14802 hydrochloride
  40. BCC6921 Senktide Senktide is a tachykinin NK3 receptor agonist. Senktide
  41. BCC6165 TC-G 1004 TC-G 1004
  42. BCC5909 DAPTA DAPTA is a synthetic peptide, functions as a viral entry inhibitor by targeting selectively CCR5, and shows potent anti-HIV activities. DAPTA
  43. BCC6041 Parstatin (human) Parstatin (human)
  44. BCC6042 Parstatin (mouse) Parstatin (mouse)
  45. BCC7456 BIBP 3226 trifluoroacetate BIBP3226 TFA is a potent and selective neuropeptide Y Y1 (NPY Y1) and neuropeptide FF (NPFF) receptor antagonist, with Kis of 1.1, 79, and 108 nM for rNPY Y1, hNPFF2, and rNPFF, respectively. BIBP3226 TFA displays anxiogenic-like effect. BIBP 3226 trifluoroacetate
  46. BCC7258 Glucagon-like peptide 1 (7-36) amide (human, rat) Glucagon-Like Peptide (GLP) I (7-36), amide, human (Human GLP-1-(7-36)-amide) is a physiological incretin hormone that stimulates insulin secretion. Glucagon-like peptide 1 (7-36) amide (human, rat)
  47. BCC6822 MDL 11,939 MDL 11,939
  48. BCC4881 Zafirlukast Zafirlukast is a potent orally active leukotriene D4 (LTD4) receptor antagonist. Zafirlukast
  49. BCC6912 A 61603 hydrobromide A 61603 hydrobromide
  50. BCC6299 PF 04418948 PF-04418948 is an orally active, potent and selective prostaglandin EP2 receptor antagonist with an IC50 of 16 nM. PF 04418948
  51. BCC5844 [D-Phe12]-Bombesin [D-Phe12]-Bombesin
  52. BCC6020 [D-Phe12,Leu14]-Bombesin [D-Phe12,Leu14]-Bombesin
  53. BCC7598 PSB 603 PSB 603
  54. BCC6234 IT1t dihydrochloride IT1t dihydrochloride is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM. IT1t dihydrochloride
  55. BCC7722 CYM 5442 hydrochloride CYM5442 is a potent, highly-selective and orally active sphingosine 1-phosphate (S1P1) receptor agonist with an EC50 of 1.35 nM. CYM5442 is inactive against S1P2, S1P3, S1P4, and S1P5. CYM5442 activates S1P1-dependent p42/p44-MAPK phosphorylation. CYM5442 exerts retinal neuroprotection. CYM5442 can easily penetrate the central nervous system (CNS). CYM 5442 hydrochloride
  56. BCC7021 RX 821002 hydrochloride RX 821002 hydrochloride
  57. BCC1158 Plerixafor (AMD3100) Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM. Plerixafor (AMD3100)
  58. BCC5885 des-His1-[Glu9]-Glucagon (1-29) amide des-His1-[Glu9]-Glucagon (1-29) amide
  59. BCC4161 MCOPPB trihydrochloride MCOPPB 3Hcl is a nociceptin receptor agonist with pKi of 10.07; weaker activity at other opioid receptors. MCOPPB trihydrochloride
  60. BCC7084 Oleylethanolamide Oleoylethanolamide is a high affinity endogenous PPAR-α agonist, which plays an important role in the treatment of obesity and arteriosclerosis. Oleylethanolamide
  61. BCC5998 BIM 23042 Selective neuromedin B receptor antagonist (NMB-R, BB1) BIM 23042
  62. BCC5762 Galanin (1-15) (porcine, rat) Galanin (1-15) (porcine, rat)
  63. BCC6947 (S)-(+)-Niguldipine hydrochloride (S)-(+)-Niguldipine hydrochloride
  64. BCC7094 SR 59230A hydrochloride SR59230A hydrochloride is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist with IC50s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively. SR 59230A hydrochloride
  65. BCC7183 Altanserin hydrochloride Altanserin hydrochloride
  66. BCC6959 Neuropeptide Y 13-36 (porcine) Neuropeptide Y 13-36 (porcine)
  67. BCC4326 Dexmedetomidine Dexmedetomidine is a sedative medication used by intensive care units and anesthetists. Dexmedetomidine
  68. BCC5928 Galanin (1-29) (rat, mouse) Galanin (1-29) (rat, mouse)
  69. BCC4090 Losartan Losartan is an angiotensin II receptor antagonist, competing with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM. Losartan
  70. BCC8076 MK-571 sodium salt hydrate MK-571 sodium salt is a selective, orally active leukotriene D4 receptor antagonist, with Kis of 0.22 and 2.1 nM in guinea pig and human lung membranes. MK-571 sodium salt hydrate
  71. BCC7334 MK 571 MRP1 inhibitor; also CysLT1 (LTD4) inverse agonist MK 571
  72. BCC5720 Sarafotoxin S6b Sarafotoxin S6b
  73. BCC7876 ML 145 ML 145 is a selective GPR35/CXCR8 antagonist with an IC50/EC50 of 20.1 nM, but not for the related GPR55 orphan receptor. GPR35 is expressed by various cells of the immune system and it may has potential as a therapeutic target in inflammatory disease. ML 145
  74. BCC6053 M 1145 M 1145
  75. BCC7260 RS 102895 hydrochloride RS102895 hydrochloride is a potent CCR2 antagonist, with an IC50 of 360 nM, and shows no effect on CCR1. RS 102895 hydrochloride
  76. BCC5713 Endothelin 3 (human, rat) Endothelin-3, human, mouse, rabbit, rat is a 21-amino acid vasoactive peptide that binds to G-protein-linked transmembrane receptors, ET-RA and ET-RB. Endothelin 3 (human, rat)
  77. BCC5876 Xenin 8 Xenin 8
  78. BCC7290 LY 255283 LY 255283
  79. BCC4775 Dexamethasone acetate Dexamethasone acetate (Dexamethasone 21-acetate) is a glucocorticoid receptor agonist. Dexamethasone acetate has the potential for ophthalmic infections treatment. Dexamethasone acetate
  80. BCC7338 CGH 2466 dihydrochloride Anti-inflammatory agent. Inhibitor of PDE4 and p38 MAPK, also adenosine receptor antagonist CGH 2466 dihydrochloride
  81. BCC6826 Luzindole Luzindole (N-0774) is a selective melatonin receptor antagonist. Luzindole preferentially targets MT2 (Mel1b) over MT1 (Mel1a) with Ki values of 10.2 and 158 nM for human MT2 and MT1, respectively. Luzindole suppresses experimental autoimmune encephalomyelitis (EAE), and exerts antidepressant-like activity. Luzindole
  82. BCC5869 PHM 27 (human) PHM 27 (human)
  83. BCC7477 L-365,260 L-365,260
  84. BCC5995 [Phe8Ψ(CH-NH)-Arg9]-Bradykinin [Phe8Ψ(CH-NH)-Arg9]-Bradykinin
  85. BCC7517 LP 12 hydrochloride LP 12 hydrochloride
  86. BCC7401 Tocrifluor T1117 Tocrifluor T1117
  87. BCC1780 MTEP hydrochloride MTEP hydrochloride is a potent, selective and non-competitive mGlu5 antagonist with an IC50 of 5 nM and a Ki of 16 nM. MTEP hydrochloride produces antiparkinsonian-like effects. MTEP hydrochloride
  88. BCC5905 ABT 702 dihydrochloride ABT-702 dihydrochloride is a potent adenosine kinase (AK) inhibitor (IC50=1.7 nM). ABT 702 dihydrochloride
  89. BCC6961 Galanin (1-30) (human) Galanin (1-30), human is a 30-amino acid neuropeptide, and acts as an agonist of GalR1 and GalR2 receptors, with Kis of both 1 nM. Galanin (1-30) (human)
  90. BCC7959 N,N-Dimethylsphingosine N,N-Dimethylsphingosine
  91. BCC4987 PF-05212384 (PKI-587) Gedatolisib (PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC50s of 0.4 nM, 5.4 nM and 1.6 nM, respectively. PKI-587 is equally effective in both complexes of mTOR, mTORC1 and mTORC2. PF-05212384 (PKI-587)
  92. BCC7246 SDZ 205-557 hydrochloride SDZ 205-557 hydrochloride
  93. BCC7143 SB 206553 hydrochloride SB 206553 hydrochloride
  94. BCC5724 CGRP 8-37 (human) HCGRP-(8-37) is a human calcitonin gene-related peptide (hCGRP) fragment and also an antagonist of CGRP receptor. CGRP 8-37 (human)
  95. BCC5390 INT-777 INT-777 is a potent TGR5 agonist with an EC50 of 0.82 μM. INT-777
  96. BCC5791 CRF (6-33) CRF (6-33)
  97. BCC1475 CGS 21680 CGS 21680 is a selective adenosine A2A receptor agonist, with a Ki of 27 nM. CGS 21680
  98. BCC2035 Verlukast Verlukast
  99. BCC1965 SRT3109 SRT3109 is an antagonist of CXCR2, with a pIC50 of 8.2, and used in the research of chemokine mediated diseases. SRT3109
  100. BCC1966 SRT3190 SRT3190 is an antagonist of CXCR2, used in the research of chemokine mediated diseases. SRT3190
  101. BCC7807 WAY 208466 dihydrochloride WAY 208466 dihydrochloride

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