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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. BCC6153 5-OMe-UDP trisodium salt Potent P2Y6 agonist 5-OMe-UDP trisodium salt
  3. BCC7919 ST 1936 oxalate ST 1936 oxalate
  4. BCC5848 Secretin (rat) Secretin (33-59), rat is a 27-aa peptide, acts on secretin receptor, enhances the secretion of bicarbonate, enzymes, and K+ from the pancreas. Secretin (rat)
  5. BCC7414 Melanotan II Melanotan (MT)-II, a synthetic melanocortin receptor agonist, is an injectable peptide hormone used to promote tanning. Melanotan II
  6. BCC5857 L-670,596 L-670,596
  7. BCC5731 [Ala1,3,11,15]-Endothelin [Ala1,3,11,15]-Endothelin
  8. BCC7833 SR 58611A hydrochloride Amibegron hydrochloride is a selective β3-adrenoceptor agonist, with an EC50 of 3.5 nM for β-adrenoceptor in rat colon; Amibegron hydrochloride has anxiolytic and antidepressant activity. SR 58611A hydrochloride
  9. BCC5949 SB 242084 SB 242084
  10. BCC5741 RS 100329 hydrochloride RS 100329 hydrochloride
  11. BCC7124 NBI 27914 hydrochloride NBI 27914 hydrochloride
  12. BCC7216 SB 258585 hydrochloride SB 258585 hydrochloride
  13. BCC5940 BX 513 hydrochloride BX 513 hydrochloride
  14. BCC7390 Trap 101 Trap 101
  15. BCC7125 SCH 79797 dihydrochloride SCH79797 dihydrochloride is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 dihydrochloride inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes. SCH 79797 dihydrochloride
  16. BCC6893 CGP 20712 dihydrochloride CGP 20712 dihydrochloride
  17. BCC5721 Sarafotoxin S6c Sarafotoxin S6c
  18. BCC7056 NAS-181 NAS-181
  19. BCC5937 SB 258719 hydrochloride SB 258719 hydrochloride
  20. BCC6890 RS 16566 dihydrochloride RS 16566 dihydrochloride
  21. BCC7137 [bAla8]-Neurokinin A(4-10) [bAla8]-Neurokinin A(4-10) is a neurokinin 2 (NK2) receptor agonist. [bAla8]-Neurokinin A(4-10)
  22. BCC6017 Amylin Amylin, amide, human, a 37-amino acid polypeptide, is a pancreatic hormone cosecreted with insulin that exerts unique roles in metabolism and glucose homeostasis. Amylin, amide, human inhibits glucagon secretion, delays gastric emptying, and acts as a satiety agent. Amylin
  23. BCC6028 ACTH (1-39) Adrenocorticotropic Hormone (ACTH) (1-39), human is a melanocortin receptor agonist. ACTH (1-39)
  24. BCC6133 MRS 2957 triethylammonium salt MRS 2957 triethylammonium salt
  25. BCC1355 AM966 AM966 is a high affinity, selective, oral LPA1-antagonist, inhibits LPA-stimulated intracellular calcium release (IC50=17 nM). AM966
  26. BCC1352 AM-095 free base AM095 (free acid) is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively. AM-095 free base
  27. BCC6115 GSK 9027 GSK 9027
  28. BCC5114 BAF312 (Siponimod) Siponimod (BAF-312) is a potent and selective sphingosine-1-phosphate (S1P) receptor modulator. It is selective for S1P1 and S1P5 receptors over S1P2, S1P3, and S1P4 (EC50s of 0.39, 0.98, >10,000, >1,000, and 750 nM, respectively). Used to treat adult multiple sclerosis. BAF312 (Siponimod)
  29. BCC6699 PCA 4248 PCA 4248
  30. BCC4316 CGS 21680 HCl CGS 21680 Hydrochloride is a selective adenosine A2A receptor agonist with a Ki of 27 nM. CGS 21680 HCl
  31. BCC1596 Glucocorticoid receptor agonist Glucocorticoid receptor agonist is a potent Glucocorticoid receptor agonist. Glucocorticoid receptor agonist
  32. BCC7215 GR 79236 GR79236 is a highly potent and selective adenosine A1 receptor agonist (Ki = 3.1 nM) that has analgesic and anti-inflammatory actions in humans and animals. GR 79236
  33. BCC4893 Meprednisone Meprednisone is a glucocorticoid and a methylated derivative of prednisone. Meprednisone
  34. BCC5716 [Leu31,Pro34]-Neuropeptide Y (porcine) [Leu31,Pro34]-Neuropeptide Y (porcine)
  35. BCC7926 TC-SP 14 Potent S1P1 receptor agonist TC-SP 14
  36. BCC7835 NPEC-caged-noradrenalin NPEC-caged-noradrenalin
  37. BCC7836 NPEC-caged-serotonin NPEC-caged-serotonin
  38. BCC7449 JP 1302 dihydrochloride JP1302 dihydrochloride is a selective, high affinity antagonist of the alpha2C-adrenoceptor (α2C-adrenoceptor), with a Kb value (antagonist activity) of 16 nM and a Ki (binding affinity) value of 28 nM. JP 1302 dihydrochloride
  39. BCC1648 INCB3344 INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity. INCB3344
  40. BCC5234 Ciclesonide Ciclesonide(RPR251526) is a glucocorticoid used to treat obstructive airway diseases. Ciclesonide
  41. BCC4190 S1RA hydrochloride S1RA hydrochloride (E-52862 hydrochloride) is a potent and selective sigma-1 receptor(σ1R, Ki=17 nM) antagonist, showed good selectivity against σ2R (Ki > 1000 nM). S1RA hydrochloride
  42. BCC7624 UTPγS trisodium salt UTPγS trisodium salt
  43. BCC5834 Sarafotoxin S6a Sarafotoxin S6a
  44. BCC6242 MK 1903 MK 1903
  45. BCC5996 Sar-[D-Phe8]-des-Arg9-Bradykinin Sar-[D-Phe8]-des-Arg9-Bradykinin
  46. BCC5921 CGP 42112 CGP-42112(CGP-42112A) is a potent Angiotensin-II subtype 2 receptor(AT2 R) agonist. CGP 42112
  47. BCC6860 BRL 37344, sodium salt BRL 37344 sodium (BRL 37344A) is a specific β3-adrenergic receptor agonist. BRL 37344 sodium treatment significantly lowers the body weight of obese mice. BRL 37344, sodium salt
  48. BCC5726 PACAP 1-27 PACAP (1-27), human, ovine, rat (PACAP 1-27) is the N-terminal fragment of PACAP-38, and is a potent PACAP receptor antagonist with IC50s of 3 nM, 2 nM and 5 nM for rat PAC1, rat VPAC1 and human VPAC2, respectively. PACAP 1-27
  49. BCC7440 Fananserin Fananserin (RP 62203) is an orally bioavailable, potent and selective 5-hydroxytryptamine2 (5-HT2) receptor antagonist, with a Ki of 0.37 nM for the rat 5-HT2A receptor. Fananserin also is a selective dopamine D4 receptor antagonist, with a Ki of 2.93 nM for the human dopamine D4 receptor. Fananserin
  50. BCC7026 Arvanil Arvanil
  51. BCC7244 Cinalukast Cinalukast
  52. BCC6068 MCH (human, mouse, rat) MCH (human, mouse, rat)
  53. BCC5698 Methysergide maleate Methysergide maleate
  54. BCC5717 CGRP 8-37 (rat) Rat CGRP-(8-37) (VTHRLAGLLSRSGGVVKDNFVPTNVGSEAF) is a highly selective CGRP receptor antagonist. CGRP 8-37 (rat)
  55. BCC6852 ZD 7114 hydrochloride ZD 7114 hydrochloride
  56. BCC5902 (+)-Igmesine hydrochloride (+)-Igmesine hydrochloride
  57. BCC7431 PD 135158 PD 135158
  58. BCC5964 HOE 140 Icatibant (HOE-140) is a selective and specific antagonist of bradykinin B2 receptor with IC50 and Ki of 1.07 nM and 0.798 nM respectively. HOE 140
  59. BCC7430 CI 988 CI 988
  60. BCC7354 A-71623 Potent and selective CCK1 agonist; suppresses feeding A-71623
  61. BCC5010 PD123319 PD 123319 (ditrifluoroacetate) is a potent, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM. PD123319
  62. BCC6533 Ozanimod (RPC1063) Ozanimod (RPC-1063) is a potent and selective S1P1 and S1P5 receptor agonist with EC50s of 410 pM and 11 nM in [35S]-GTPγS binding, respectively. Ozanimod (RPC1063)
  63. BCC7905 RP 001 hydrochloride RP-001 is a picomolar short-acting S1P1 (EDG1) selective agonist, with an EC50 of 9 pM. RP-00 induces internalization and polyubiquitination of S1P1. RP-001 has little activity on S1P2-S1P4 and only moderate affinity for S1P5. RP 001 hydrochloride
  64. BCC7374 SDZ WAG 994 SDZ WAG 994
  65. BCC5680 m-CPP hydrochloride m-CPP hydrochloride
  66. BCC4125 GPR40 Activator 1 GPR40 Activator 1 is a potent GPR40 activator for treatment of type 2 diabetes. GPR40 Activator 1
  67. BCC1745 mGlu2 agonist LY2979165 is a mGlu2 agonist, which is a novel potent agent that is used as anti-depressants. mGlu2 agonist
  68. BCC6057 Teijin compound 1 CCR2 antagonist 4 hydrochloride (Teijin compound 1 hydrochloride) is a potent and specific CCR2 antagonist, with IC50s of 180 nM for CCR2b. CCR2 antagonist 4 hydrochloride potently inhibits MCP-1-induced chemotaxis with an IC50 of 24 nM. Teijin compound 1
  69. BCC6065 Hemopressin (human, mouse) Hemopressin (human, mouse)
  70. BCC7812 OPC 21268 Fuscoside (OPC-21268) is an orally effective, nonpeptide, vasopressin V1 receptor antagonist with an IC50 of 0.4 μM. OPC 21268
  71. BCC6277 TC-G 1006 S1P1 Agonist III is a potent and orally active S1P1 agonist with EC50 of 18 nM; no activity on S1P3. TC-G 1006
  72. BCC5722 [Leu31,Pro34]-Neuropeptide Y (human, rat) [Leu31,Pro34]-Neuropeptide Y (human, rat)
  73. BCC7032 PD 81723 PD 81723
  74. BCC5272 Ramosetron Hydrochloride Ramosetron Hydrochloride(YM060 Hydrochloride) is a serotonin 5-HT3 receptor antagonist for the treatment of nausea and vomiting. Ramosetron Hydrochloride
  75. BCC6928 (+)-SK&F 10047 hydrochloride (+)-SK&F 10047 hydrochloride
  76. BCC6891 LY 225910 LY 225910
  77. BCC5945 BIM 23052 sst5 agonist BIM 23052
  78. BCC6202 DV 7028 hydrochloride DV 7028 hydrochloride
  79. BCC6705 3-MPPI 3-MPPI
  80. BCC7257 Exendin-3 (9-39) amide Avexitide (Exendin (9-39)) is a specific and competitive GLP-1 receptor antagonist. Exendin-3 (9-39) amide
  81. BCC5596 ML224 ML224(NCGC00242364; ANTAG3) is a selective TSHR inverse agonist; inhibits TSH-stimulated cAMP production with an IC50 = 2.3 μM. ML224
  82. BCC1649 INCB8761(PF-4136309) PF-4136309 is a potent, selective, and orally bioavailable CCR2 antagonist, with IC50s of 5.2 nM, 17 nM and 13 nM for human, mouse and rat CCR2. INCB8761(PF-4136309)
  83. BCC7928 BIMU 8 Potent 5-HT4 receptor full agonist BIMU 8
  84. BCC7603 alpha,beta-Methyleneadenosine 5'-triphosphate trisodium salt α,β-Methylene ATP trisodium, a phosphonic analog of ATP, is a P2X3 and P2X7 receptor ligand. alpha,beta-Methyleneadenosine 5'-triphosphate trisodium salt
  85. BCC7625 2-ThioUTP tetrasodium salt 2-ThioUTP tetrasodium salt
  86. BCC1351 AM095 AM095 is a selective LPA1 receptor antagonist. The IC50 for AM095 antagonism of LPA-induced calcium flux of human or mouse LPA1-transfected CHO cells is 0.025 and 0.023 μM, respectively. AM095
  87. BCC6260 CYM 50308 CYM50308 is a potent, selective and high affinity sphingosine-1-phosphate receptor 4 (S1P4-R) agonist with an EC50 of 56 nM. CYM50308 displays 37-fold more selective for S1P4-R than S1P5-R. CYM50308 has no activity at S1P1-R, S1P2-R and S1P3-R subtypes at concentrations up to 25 μM. CYM 50308
  88. BCC8022 ML 154 ML 154
  89. BCC6901 8-M-PDOT 8-M-PDOT (AH-002) is a selective melatonin MT2 receptor agonist. 8-M-PDOT is 5.2-fold selective for MT2 over MT1 receptors. 8-M-PDOT binds human recombinant MT2 and MT2 receptors with pKi values of 8.23 and 8.95 respectively. 8-M-PDOT has anxiolytic-like activity. 8-M-PDOT
  90. BCC6900 4-P-PDOT 4-P-PDOT is a potent, selective and affinity Melatonin receptor (MT2) antagonist. 4-P-PDOT is >300-fold more selective for MT2 than MT1. 4-P-PDOT significantly counteracts Melatonin-mediated antioxidant effects (GSH/GSSG ratio, phospho-ERK, Nrf2 nuclear translocation, Nrf2 DNA-binding activity). 4-P-PDOT
  91. BCC5247 Sarpogrelate hydrochloride Sarpogrelate hydrochloride (MCI-9042), a selective 5-HT2 antagonist, has been widely used as an anti-platelet agent for the treatment of PAD. Sarpogrelate hydrochloride
  92. BCC6881 Pindolol Pindolol (LB-46) is a nonselective β-blocker with partial beta-adrenergic receptor agonist activity, also functions as a 5-HT1A receptor weak partial antagonist (Ki=33nM). Pindolol
  93. BCC7133 MEN 10376 Men 10376 is a selective tachykinin NK-2 receptor antagonist, with a Ki of 4.4 μM for rat small intestine NK-2 receptor. MEN 10376
  94. BCC6346 ACT 335827 ACT 335827
  95. BCC6259 CYM 50260 CYM50260 is a potent and exquisitely selective sphingosine-1-phosphate 4 receptor (S1P4-R) agonist with an EC50 of 45 nM. CYM50260 displays no activity against S1P1-R, S1P2-R, S1P3-R and S1P5-R. CYM 50260
  96. BCC5729 MDL 29,913 MDL 29,913
  97. BCC5850 [D-Lys3]-GHRP-6 [D-Lys3]-GHRP-6
  98. BCC6124 KW 3902 Rolofylline (KW-3902) is a potent, selective adenosine A1 receptor antagonist that is under development for the treatment of patients with acute congestive heart failure and renal impairment. Rolofylline is metabolized primarily to the pharmacologically active M1-trans and M1-cis metabolites by cytochrome P450 (CYP450). Rolofylline is alleviating the presynaptic dysfunction and restores neuronal activity as well as dendritic spine levels in vitro, is an interesting candidate to combat the hypometabolism and neuronal dysfunction associated with Tau-induced neurodegenerative diseases. KW 3902
  99. BCC7277 SR 27897 Lintitript (SR 27897) is a highly potent, selective, orally active, competitive and non-peptide cholecystokinin (CCK1) receptor antagonist with an EC50 of 6 nM and a Ki of 0.2 nM. Lintitript displays > 33-fold selectivity more selective for CCK1 than CCK2 receptors (EC50 value of 200 nM). Lintitript increases plasma concentration of leptin and food intake as well as plasma concentration of insulin. SR 27897
  100. BCC6963 BQ-123 BQ-123 is a selective endothelin A receptors (ETAR) antagonist with an IC50 value of 7.3 nM and a Ki vaule of 25 nM. BQ-123
  101. BCC1841 PD 123319 ditrifluoroacetate PD 123319 (ditrifluoroacetate) is a potent, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM. PD 123319 ditrifluoroacetate

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