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
- 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.
- BCC7490 Alprenolol hydrochloride Alprenolol (hydrochloride) is a non-selective beta blocker as well as 5-HT1A receptor antagonist.
- 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.
- BCC7101 LY 215840
- BCC6235 TUG 891 TUG-891is a potent and selective agonist for the long chain free fatty acid (LCFA) receptor 4 (FFA4/GPR120).
- BCC5994 [Lys5,MeLeu9,Nle10]-NKA(4-10)
- BCC5800 GR 64349
- BCC5933 BIM 187
- BCC5017 Valsartan Valsartan (CGP-48933) is an angiotensin II receptor antagonist for the treatment of high blood pressure and heart failure.
- 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.
- BCC6238 CYM 9484 CYM 9484 is a selective and highly potent neuropeptide Y (NPY) Y2 receptor antagonist with an IC50 value of 19 nM.
- BCC6674 BD 1008 dihydrobromide
- 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.
- BCC2560 Irbesartan Irbesartan is a highly potent and specific angiotensin II type 1 (AT1) receptor antagonist with IC50 of 1.3 nM.
- BCC6266 LP 20 hydrochloride
- BCC5863 JMV 449
- BCC6726 2-PMDQ
- BCC6902 ZM 241385 ZM241385 is a potent, high affinity and selective adenosine A2a receptor (A2AR) antagonist with a Ki value of 1.4 nM.
- 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.
- BCC1840 PB-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.
- BCC5688 ICI 215,001 hydrochloride
- 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.
- BCC5799 GR 94800
- BCC5763 Galanin (2-29) (rat)
- BCC6994 SDZ SER 082 fumarate
- 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.
- BCC5934 BIM 189
- BCC6337 CYM 50769
- BCC5733 FR 139317
- BCC5728 BQ-3020 Selective ETB agonist
- 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.
- BCC7813 WAY 267464 dihydrochloride
- BCC6877 RS 56812 hydrochloride
- 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.
- BCC5751 SB 200646 hydrochloride
- BCC7686 M40 M40 is a potent, non-selective galanin receptor antagonist.
- 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.
- BCC5730 IRL-1038
- 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.
- BCC1819 Olmesartan Olmesartan (RNH-6270) is an angiotensin II receptor (AT1R) antagonist used to treat high blood pressure.
- BCC6678 4F 4PP oxalate
- BCC7437 L-703,664 succinate
- BCC7386 MRS 2693 trisodium salt
- 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.
- 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.
- BCC7305 L-692,585
- BCC5685 MRS 2179 tetrasodium salt
- BCC6004 AR-C 66096 tetrasodium salt Potent and selective P2Y12 antagonist
- 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.
- BCC5941 SC 51322
- BCC7773 SC 51089
- 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.
- BCC7536 1-Methylpsilocin
- BCC7180 SR 2640 hydrochloride
- BCC5734 ZD 7155 hydrochloride ZD 7155 hydrochloride is an angiotensin II receptor type 1 (AT1 receptor) antagonist.
- 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.
- BCC6248 TT 232
- BCC5014 Azilsartan Azilsartan(TAK-536) is a specific and potent angiotensin II type 1 receptor antagonist with IC50 of 2.6 nM.
- BCC5772 LY 288513
- 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.
- BCC7640 8-(3-Chlorostyryl)caffeine
- 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.
- 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.
- BCC6048 GRK2i
- BCC7081 GR 127935 hydrochloride
- BCC5752 SB 204070
- BCC4350 Ivabradine HCl Ivabradine hydrochloride is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker.
- BCC7573 NE 100 hydrochloride
- 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.
- BCC6767 RS 23597-190 hydrochloride
- BCC6741 2-MPMDQ
- BCC5824 BIM 23056 sst receptor ligand
- BCC6727 Quipazine dimaleate
- BCC7324 SR 49059
- BCC7514 MRS 2690
- 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.
- BCC7091 CL 316243 disodium salt
- BCC7774 CP 135807
- BCC4680 Montelukast Sodium Montelukast (sodium) (MK0476) is a potent, selective CysLT1 receptor antagonist.
- BCC6018 AC 187 Potent and selective amylin receptor antagonist
- BCC6748 2-Phenylmelatonin
- BCC7336 A 80426 mesylate
- BCC7035 SB 204741
- BCC4332 Nebivolol Nebivolol hydrochloride selectively inhibits β1- adrenergic receptor with IC50 of 0.8 nM.
- BCC7237 PSB 1115
- BCC7068 BMY 45778 Non-prostanoid prostacyclin IP receptor partial agonist
- BCC7690 [D-Trp34]-Neuropeptide Y
- BCC8025 NBOH-2C-CN hydrochloride
- BCC6359 ANQ 11125 Selective motilin receptor antagonist
- 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.
- BCC7576 BAY-u 9773 Dual CysLT1 and CysLT2 antagonist
- BCC6784 N-[2-(Piperidinylamino)ethyl]-4-iodobenzamide
- BCC6780 SM-21 maleate
- BCC6771 2-[1-(4-Piperonyl)piperazinyl]benzothiazole
- BCC4447 Plerixafor 8HCl (AMD3100 8HCl) Plerixafor octahydrochloride (AMD3100 octahydrochloride) is a selective CXCR4 antagonist with an IC50 of 44 nM.
- 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.
- 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.
- BCC6779 PG-9 maleate
- 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) .