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
- GIP Receptor(2)
- FFAR1 (GPR40)(7)
- 5-HT Receptor(238)
- Urotensin-II Receptor(10)
- CCK2 Receptors(7)
- P2Y Receptor(25)
- EP4 Receptor(3)
- CRF1 Receptors(6)
- Melatonin Receptors(9)
- LPL Receptor(1)
- Adenosine Receptor(54)
- VIP Receptors(7)
- OX Receptor(15)
- Chemokine Receptors(16)
- Neurotensin Receptors(7)
- Prostanoid Receptors(21)
- CCK1 Receptors(5)
- Adrenergic Receptor(136)
- GPR119(5)
- Calcium-Sensing Receptor(3)
- Cannabinoid Receptor(36)
- Angiotensin Receptor(21)
- GPR120(2)
- Protease-Activated Receptors(9)
- PAF Receptors(3)
- Sigma Receptor(24)
- NK3 Receptor(6)
- NPY Receptors(23)
- Glucagon Receptor(16)
- Leukotriene Receptor(9)
- Bombesin Receptors(14)
- Sphingosine(14)
- CXCR(16)
- NOP Receptor(21)
- GPR55(5)
- Galanin Receptors(11)
- Endothelin Receptor(11)
- GPR35(7)
- Glucocorticoid Receptor(17)
- Calcitonin and Related Receptors(10)
- Bradykinin Receptors(12)
- mGluR(11)
- Adenosine Kinase(2)
- GPR109A(2)
- GPCR19(1)
- Non-selective CRF(7)
- LTD4 Receptor(1)
- Secretin Receptors(1)
- Melanocortin (MC) Receptors(16)
- ETB Receptors(5)
- NK2 Receptors(7)
- LPA Receptor(5)
- S1P receptor inhibitor(5)
- CCR2(5)
- Hydroxycarboxylic Acid Receptors(5)
- PACAP Receptors(3)
- Melanin-concentrating Hormone Receptors(7)
- Vasopressin Receptor(10)
- Somatostatin Receptor(15)
- TSH Receptor(1)
- Peptide Receptors(8)
- Ghrelin Receptors(9)
- ETA Receptors(3)
- Orphan 7-TM Receptors(6)
- Oxytocin Receptors(4)
- Ras(6)
- Heterotrimeric(1)
- CysLT1 receptor(1)
- Motilin Receptor(4)
- Acetylcholine(3)
- Prostaglandin Receptor(4)
- GHSR(4)
- EBI2/GPR183(1)
- Gonadotropin-Releasing Hormone Receptors(3)
- Orexin(3)
- Apelin Receptor(5)
- CRF2 Receptors(3)
- Calcimimetic Agent(2)
- Adrenergic Transporters(5)
- CaSR(3)
- EP1 Receptor(1)
- Sensory Neuron-Specific Receptors(1)
- 17,20-lyase(3)
- Adenosine Deaminase(3)
- NK Receptor(1)
- PGD2 Receptor(1)
- GLUT1(1)
- RGS(2)
- GPR44(1)
- Adiponectin Receptor(1)
- ERRγ(1)
- Cat.No. Product Name Information
- BCC6049 Lys-γ3-MSH
- BCC7350 SNAP 5089
- 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.
- 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).
- 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.
- BCC7085 GR 231118
- BCC7392 APC 366 Tryptase inhibitor
- BCC7282 L-755,507 L755507 is a potent, selective agonist of β3-AR with an IC50 of 35 nM.
- BCC7285 PNU 22394 hydrochloride
- BCC6913 GR 55562 dihydrochloride
- BCC1638 Ibutamoren Mesylate Ibutamoren (Mesylate) is a potent, non-peptide Growth hormone secretagogue receptor (GHSR) agonist.
- 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).
- 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.
- BCC5822 BIM 23127
- 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.
- BCC6915 BW 723C86 hydrochloride 5-HT2B agonist
- 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.
- BCC6001 GLP-1 (9-36) amide
- 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).
- BCC7385 Melperone hydrochloride
- BCC7523 CI 1020
- 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.
- 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.
- BCC5539 K-Ras G12C-IN-2 K-Ras G12C-IN-2 is an irreversible covalent K-Ras G12C inhibitor.
- BCC5540 K-Ras G12C-IN-3 K-Ras G12C-IN-3 is a novel and irreversible inhibitor of mutant K-ras G12C.
- 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.
- BCC6914 WIN 64338 hydrochloride Bradykinin B2 antagonist
- BCC1353 AM630 6-Iodopravadoline (AM630) is a selective CB2 antagonist with Ki of 31.2 nM, and displays 165-fold selectivity over CB1 receptors.
- 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.
- BCC1525 Desmopressin Synthetic vasopressin analog; V1B and V2 agonist,Desmopressin(DDAVP) is the synthetic analogue of the antidiuretic hormone arginine vasopressin.
- BCC7164 R-96544 hydrochloride
- BCC5694 RS 39604 hydrochloride
- 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
- 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.
- 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.
- BCC5693 RS 67333 hydrochloride
- BCC6878 RS 67506 hydrochloride 5-HT4 partial agonist
- 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.
- 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.
- BCC7196 Ro 60-0175 fumarate
- BCC5686 Nociceptin Nociceptin, a heptadecapeptide, is the endogenous ligand of the nociceptin receptor, acting as a potent anti-analgesic.
- BCC5790 Astressin Astressin is a potent corticotropin releasing factor (CRF) antagonist.
- BCC7742 Donitriptan hydrochloride 5-HT1B/1D agonist
- BCC6697 N-Methylquipazine dimaleate
- 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.
- BCC7558 LY 272015 hydrochloride
- BCC7856 LY 266097 hydrochloride
- BCC7411 PB 28 dihydrochloride
- BCC5865 BWX 46 Highly selective NPY Y5 agonist
- BCC7628 Rec 15/2615 dihydrochloride
- BCC7650 BGC 20-761 High affinity 5-HT6 antagonist
- BCC7734 FR 171113
- BCC1379 Atrasentan
- 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).
- BCC7037 SB 218795
- 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.
- 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.
- BCC5913 CH 275
- 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.
- BCC6709 Metergoline Metergoline is a psychoactive drug of the ergoline chemical class which acts as a ligand for various serotonin and dopamine receptors.
- BCC7346 LY 320135
- 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+.
- 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.
- BCC6085 Orphanin FQ (1-11)
- BCC5738 Nociceptin (1-7)
- BCC5878 ZD 2079
- BCC7069 N-Arachidonylglycine
- BCC6883 AH 11110 hydrochloride
- BCC6976 SB 224289 hydrochloride SB-224289 hydrochloride is a selective 5-HT1B receptor antagonist, with anxiolytic effect.
- BCC7284 PD 160170
- 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.
- 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.
- 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.
- BCC6972 MRS 1220
- BCC1951 sitaxsentan Sitaxsentan (IPI 1040; TBC-11251) is a selective endothelin A (ETA) receptor antagonist.
- BCC7323 SR 142948
- BCC6014 R 715
- BCC5679 GR 46611
- 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.
- BCC5181 AMD 3465 AMD 3465 is a potent, selective CXCR4 antagonist, and inhibits SDF-1α-ligand binding with Ki of 41.7 nM.
- BCC6876 RS 79948 hydrochloride
- BCC2524 Zibotentan (ZD4054) Zibotentan (ZD4054) is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM).
- BCC7695 ML 10302 hydrochloride
- BCC7408 PNU 109291
- 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.
- BCC7500 Arachidonyl serotonin
- BCC5704 NocII
- 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.
- BCC1919 Salmefamol
- BCC7955 Tegaserod maleate Tegaserod maleate is a partial agonist of the 5-HT4 receptor; stimulates the peristaltic reflex and accelerates gastrointestinal transit.
- BCC7187 Palmitoylisopropylamide
- BCC6836 GR 135531
- BCC6194 AT 1015 Long-acting 5-HT2A antagonist
- BCC7325 L-168,049
- 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).
- BCC7270 NTNCB hydrochloride
- BCC5753 MRS 1334
- 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.
- 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.
- 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.