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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. BCC6861 Xamoterol hemifumarate Xamoterol hemifumarate
  3. BCC6256 SB 706375 SB 706375
  4. BCC4218 Doxazosin Doxazosin (UK 33274) is a quinazoline-derivative that selectively antagonizes postsynaptic α1-adrenergic receptors. Doxazosin
  5. BCC5715 Somatostatin 1-28 Somatostatin 1-28
  6. BCC7522 PAF (C16) Endogenous platelet-activating factor (PAF) PAF (C16)
  7. BCC5792 Sauvagine Sauvagine
  8. BCC4963 Alprostadil Alprostadil is used as a drug in the treatment of erectile dysfunction and has vasodilatory properties. It is a Prostaglandin Analog and Prostaglandin E1 Agonist. Alprostadil
  9. BCC5809 GRP (porcine) GRP (porcine)
  10. BCC6652 5-Carboxamidotryptamine maleate 5-Carboxamidotryptamine maleate
  11. BCC6708 PRE-084 hydrochloride PRE-084 hydrochloride is a high affinity, selective σ1 agonist, has an IC50 of 44 nM in the sigma receptor assay. PRE-084 hydrochloride
  12. BCC4203 TAK-700 R-form TAK-700 R-form
  13. BCC4358 Indacaterol Maleate Indacaterol is an ultra-long-acting β-adrenoceptor agonist with pKi of 7.36 for β1-adrenoceptor and pKi of 5.48 for β2-adrenoceptor. Indacaterol Maleate
  14. BCC7090 Rimcazole dihydrochloride Rimcazole dihydrochloride
  15. BCC5963 [Nle4,D-Phe7]-α-MSH Melanotan I is a synthetic analogue of α-melanocyte stimulating hormone (α-MSH), for gaining a tan. [Nle4,D-Phe7]-α-MSH
  16. BCC5711 Pancreatic Polypeptide (human) Pancreatic Polypeptide, human is a C-terminally amidated 36 amino acid peptide, which acts as a neuropeptide Y (NPY) Y4/Y5 receptor agonist. Pancreatic Polypeptide (human)
  17. BCC4079 Detomidine Detomidine produce dose-dependent sedative and analgesic effects, is a nonnarcotic, synthetic α2-adrenergic agonist Target: α2-adrenergic agonist Detomidine is an imidazole derivative and α2-adrenergic agonist, used as a large animal sedative, primarily used in horses. Detomidine
  18. BCC6967 SR 57227 hydrochloride SR 57227 hydrochloride
  19. BCC1257 Doxazosin Mesylate Doxazosin mesylate (UK 33274) is a quinazoline-derivative that selectively antagonizes postsynaptic α1-adrenergic receptors. Doxazosin Mesylate
  20. BCC5985 [Orn5]-URP [Orn5]-URP
  21. BCC7247 Iloprost Iloprost (ZK 36374) is a synthetic analogue of prostacyclin PGI2. Iloprost
  22. BCC5200 SB-334867 free base SB-334867 free base (SB334867A free base) is an excellent, selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo. SB-334867 free base
  23. BCC6798 Idazoxan hydrochloride Idazoxan hydrochloride (RX 781094 hydrochloride) is an α2-adrenoceptor antagonist and is also a imidazoline receptors (IRs) antagonist competitively antagonized the centrally induced hypotensive effect of imidazoline-like drugs (IMs). Idazoxan hydrochloride also improves motor symptoms in Parkinson’s disease, L-DOPA-induced dyskinesias, and experimental Parkinsonism. Idazoxan hydrochloride
  24. BCC5499 RG7090 Basimglurant (RG7090) is a potent, selective and orally available mGlu5 negative allosteric modulator with a Kd of 1.1 nM. RG7090
  25. BCC4907 Fluticasone propionate Fluticasone propionate is a high affinity, selective GR (glucocorticoid receptor) agonist which is derived from fluticasone used to treat asthma and allergic rhinitis. Fluticasone propionate
  26. BCN4344 Grifolic acid Grifolic acid
  27. BCC6875 Imiloxan hydrochloride Imiloxan hydrochloride
  28. BCC7191 Seglitide Seglitide
  29. BCC2494 Alfuzosin HCl Alfuzosin hydrochloride is an α1 adrenergic receptor antagonist used to treat benign prostatic hyperplasia (BPH). Alfuzosin HCl
  30. BCC4080 Alfuzosin Alfuzosin is an α1 adrenergic receptor antagonist used to treat benign prostatic hyperplasia (BPH). Alfuzosin
  31. BCC5832 Neuromedin C (porcine) Neuromedin C (porcine)
  32. BCC5431 Bambuterol Bambuterol ((±)-Bambuterol; KWD-2183) is a long acting beta-adrenoceptor agonist (LABA) used in the treatment of asthma; it also is a prodrug of terbutaline. Bambuterol
  33. BCC7399 LP 44 LP 44
  34. BCC7479 Nefazodone hydrochloride Nefazodone hydrochloride is an antidepressant drug. Nefazodone hydrochloride
  35. BCC4223 Perindopril Perindopril is a long-acting ACE inhibitor of which is used to treat high blood pressure, heart failure or stable coronary artery disease. Perindopril
  36. BCC2256 Methylprednisolone Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone
  37. BCC5643 Octreotide acetate Octreotide is a somatostatin analog that binds to the somatostatin receptor, mainly subtypes 2, 3, and 5, increases Gi activity, and reduces intracellular cAMP production. Octreotide acetate
  38. BCC5389 APD668 APD668 is a potent GPR119 agonist with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119 respectively. APD668
  39. BCC6341 4-[4-(3-Hydroxyphenyl)-3-(4-methylphenyl)-6-oxo-1,4-dihydropyrrolo[3,4-d]pyrazol-5-yl]benzoic acid CID 16020046 is a potent and selective GPR55(LPI receptor) antagonist; inhibitsGPR55 constitutive activity with IC50 of 0.15 uM. 4-[4-(3-Hydroxyphenyl)-3-(4-methylphenyl)-6-oxo-1,4-dihydropyrrolo[3,4-d]pyrazol-5-yl]benzoic acid
  40. BCC5712 CGRP (rat) CGRP (rat)
  41. BCC7693 Cyclosomatostatin Non-selective sst receptor antagonist Cyclosomatostatin
  42. BCC4486 Mifepristone Mifepristone is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay. Mifepristone
  43. BCC7018 CP 94253 hydrochloride CP 94253 hydrochloride
  44. BCC5663 2-Methyl-5-hydroxytryptamine hydrochloride 2-Methyl-5-HT hydrochloride (2-Methyl-5-hydroxytryptamine hydrochloride) is a potent and selective 5-HT3 receptor agonist. 2-Methyl-5-HT hydrochloride is shown to display anti-depressive-like effects. 2-Methyl-5-hydroxytryptamine hydrochloride
  45. BCC6210 SHA 68 SHA 68 is a potent and selective non-peptide neuropeptide S receptor (NPSR) antagonist with IC50s of 22.0 and 23.8 nM for NPSR Asn107 and NPSR Ile107, respectively. SHA 68 has limited the blood-brain barrier (BBB) penetration and the activity in neuralgia. SHA 68
  46. BCC6208 S 32212 hydrochloride S 32212 hydrochloride
  47. BCC5775 UFP-101 UFP-101
  48. BCC7854 PF9 tetrasodium salt PF9 tetrasodium salt
  49. BCC4507 OC000459 OC000459 is a potent and selective D prostanoid receptor 2 (DP2) antagonist with IC50 of 13 nM. Phase 2. Cas: 851723-84-7 OC000459
  50. BCC7746 PF 514273 PF 514273
  51. BCC4111 NBI-74330 NBI-74330 is a potent antagonist for CXCR3, and exhibits potent inhibition of (125I)CXCL10 and (125I)CXCL11 specific binding with Ki of 1.5 and 3.2 nM, respectively. NBI-74330
  52. BCC1946 Setiptiline maleate Setiptiline is a serotonin receptor antagonist. Setiptiline maleate
  53. BCC5408 PSN632408 PSN632408 is an optimized agonist of GPR119 receptors that shows similar potency to OEA at both recombinant mouse and human GPR119 receptors, exhibiting EC50 values of 5.6 and 7.9 uM, respectively. PSN632408
  54. BCC6664 1,3-Dipropyl-8-phenylxanthine 1,3-Dipropyl-8-phenylxanthine
  55. BCC7142 GR 125487 sulfamate GR 125487 sulfamate
  56. BCC5929 M617 M617
  57. BCC7795 SKF 86466 hydrochloride SKF 86466 hydrochloride
  58. BCC1364 Anamorelin hydrochloride Anamorelin hydrochloride is a novel ghrelin receptor agonist with EC50 value of 0.74 nM in the FLIPR assay. Anamorelin hydrochloride
  59. BCC5021 Azilsartan Medoxomil Azilsartan medoxomil(TAK 491) is an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM, which used in the treatment of adults with essential hypertension. Azilsartan Medoxomil
  60. BCC4089 Azilsartan medoxomil monopotassium Azilsartan medoxomil monopotassium is an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM, which used in the treatment of adults with essential hypertension. Azilsartan medoxomil monopotassium
  61. BCC1736 Medetomidine Medetomidine(Domtor) is a potent, highly selective α2-adrenoceptor agonist (Ki values are 1.08 and 1750 nM for α2- and α1-adrenoceptors respectively). Medetomidine
  62. BCC4351 Medetomidine HCl Medetomidine hydrochloride is an agonist of adrenergic alpha-2 receptor, which is used in veterinary medicine for its analgesic and sedative properties. Medetomidine HCl
  63. BCC6047 C 021 dihydrochloride Potent CCR4 antagonist C 021 dihydrochloride
  64. BCC7594 SB 699551 SB 699551
  65. BCC6149 TC-MCH 7c TC-MCH 7c, a phenylpyridone derivative, is an orally available, selective and brain-penetrable MCH1R antagonist with an IC50 of 5.6 nM for hMCH1R. TC-MCH 7c has Kis of 3.4 nM and 3.0 nM of human and mouse MCH1R, respectively. TC-MCH 7c
  66. BCC6387 AMG837 AMG 837 is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents. AMG837
  67. BCC5973 [Ala2,8,9,11,19,22,24,25,27,28]-VIP [Ala2,8,9,11,19,22,24,25,27,28]-VIP
  68. BCC5710 CRF (human, rat) Corticotropin-releasing factor human (Human CRF; Human corticotropin-releasing factor) stimulates the synthesis and secretion of adrenocorticotropin in the anterior pituitary. CRF (human, rat)
  69. BCC4411 Org 27569 Org 27569 is a potent CB1 receptor allosteric modulator, which increases agonist binding, yet blocks agonist-induced CB1 signaling. Org 27569
  70. BCC5912 Obestatin (rat) Obestatin (rat)
  71. BCC2011 Tozadenant Tozadenant is an adenosine A2A receptor antagonist, with Ki of 11.5 nM on human A2A and 6 nM on rhesus A2A. Tozadenant
  72. BCC7214 Ritanserin Ritanserin (R 55667) is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT2 receptor, with an IC50 of 0.9 nM, less active on Histamine H1, Dopamine D2, Adrenergic α1, Adrenergic α2 receptors. Ritanserin
  73. BCC1752 MK 0893 MK 0893 is a potent and selective glucagon receptor antagonist with an IC50 of 6.6 nM. MK 0893
  74. BCC5841 Neuromedin B (porcine) Neuromedin B (NMB) is a member of Bombesin (BN)-like peptide family in mammals. Neuromedin B (porcine)
  75. BCC8036 TCS 3035 GPR35 agonist TCS 3035
  76. BCC5122 Almorexant Almorexant (ACT 078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM, respectively. Almorexant
  77. BCC4599 CTEP (RO4956371) CTEP (RO 4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, and shows > 1000-fold selectivity over other mGlu receptors. CTEP (RO4956371)
  78. BCC7802 WAY 207024 dihydrochloride GnRH receptor antagonist WAY 207024 dihydrochloride
  79. BCC1531 Dipraglurant Dipraglurant (ADX 48621) is a mGluR5 antagonists with IC50 of 0.021 μM. Dipraglurant
  80. BCC7413 ZK 756326 ZK 756326
  81. BCC7826 YIL 781 YIL 781
  82. BCC6278 ML 221 ML221 is a potent apelin (APJ) functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC50s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays. ML 221
  83. BCC5827 Glucagon-like peptide 1 (1-37) (human, rat) Glucagon-like peptide 1 (1-37), human is a highly potent agonist of the GLP-1 receptor. Glucagon-like peptide 1 (1-37) (human, rat)
  84. BCC4189 S1RA S1RA(E-52862) is a potent and selective sigma-1 receptor(σ1R, Ki=17 nM) antagonist, showed good selectivity against σ2R (Ki > 1000 nM). S1RA
  85. BCC6899 CP 93129 dihydrochloride CP 93129 dihydrochloride
  86. BCC5917 UFP 803 UFP 803
  87. BCC1358 AMD-070 hydrochloride AMD-070 (hydrochloride) is a potent and selective antagonist of CXCR4 with an IC50 value of 13 nM in a CXCR4 125I-SDF inhibition binding assay, and inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs. AMD-070 hydrochloride
  88. BCC6163 26RFa 26RFa
  89. BCC4083 L-(-)-α-Methyldopa hydrochloride L-(-)-α-Methyldopa hydrochloride is an alpha-adrenergic agonist (selective for α2-adrenergic receptors) psychoactive drug used as a sympatholytic or antihypertensive. L-(-)-α-Methyldopa hydrochloride
  90. BCC1102 GW9508 GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC50s of 7.32 and 5.46, respectively. GW9508 shows ~100-fold selectivity for GPR40 over GPR120. GW9508 is inactive against other GPCRs, kinases, proteases, integrins and PPARs. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (KATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities. GW9508
  91. BCC1646 INCB 3284 dimesylate INCB 3284 dimesylate is a potent, selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2, with an IC50 of 3.7 nM. INCB 3284 dimesylate can be used in the research of acute liver failure. INCB 3284 dimesylate
  92. BCC5960 Galanin (porcine) Galanin (porcine)
  93. BCC1710 LUF6000 LUF6000 is an allosteric modulator of the human A3 adenosine receptor (AR). LUF6000
  94. BCC6797 Efaroxan hydrochloride Efaroxan hydrochloride
  95. BCC4346 Detomidine HCl Detomidine hydrochloride produce dose-dependent sedative and analgesic effects, is a nonnarcotic, synthetic α2-adrenergic agonist Target: α2-adrenergic agonist Detomidine is an imidazole derivative and α2-adrenergic agonist, used as a large animal sedative, primarily used in horses. Detomidine HCl
  96. BCC4110 SCH 546738 SCH 546738 is a potent, orally active and non-competitive CXCR3 antagonist, the affinity constant (Ki) of SCH 546738 binding to human CXCR3 receptor is determined to be 0.4 nM in multiple experiments. SCH 546738
  97. BCC5314 Atosiban Atosiban(RW22164; Tractocile) is a nonapeptide, desamino-oxytocin analogue, and a competitive vasopressin/oxytocin receptor antagonist (VOTra). Atosiban
  98. BCC5727 α-helical CRF 9-41 CRF receptor antagonist α-helical CRF 9-41
  99. BCC5930 M871 M871
  100. BCC5962 α-CGRP (human) α-CGRP (human)
  101. BCC7723 W146 W146 is a selective antagonist of sphingosine-1-phosphate receptor 1 (S1PR1) with an EC50 value of 398 nM. W146

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