About 31 results found for searched term "ET receptor antagonist 2" (0.076 seconds)
Cat.No. | Name | Target |
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M43591 | ET receptor antagonist 2 | Estrogen Receptor |
ET receptor antagonist 2 is an orally active ET receptor antagonist (IC50=0.22 nM), which can be used for research in pulmonary arterial hypertension (PAH). | ||
M1917 | Mozavaptan | Vasopressin Receptor |
OPC-31260 | ||
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. | ||
M2230 | Agomelatine | Melatonin Receptor |
Valdoxan; Melitor; S-20098 | ||
Agomelatine is a metabolically stable analog of melatonin that displays agonist activity for MT1 and MT2 binding with nanomolar affinity. Agomelatine is also a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively. | ||
M3072 | Timolol Maleate | Adrenergic Receptor |
(S)-Timolol Maleate; L-714465 Maleate; MK 950 | ||
Timolol Maleate is a non-selective, beta-adrenergic receptor antagonist for β1/β2 with Ki of 1.97 nM/2.0 nM. | ||
M3239 | Ketanserin | 5-HT Receptor |
R41468 | ||
Ketanserin is specific 5-HT2A serotonin receptor antagonist with a Ki of 2.5 nM for rat and human 5-HT2A. | ||
M3320 | Quetiapine Fumarate | 5-HT Receptor |
Quetiapine hemifumarate | ||
Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. | ||
M3331 | Trospium chloride | AChR/AChE |
Trospium chloride is an orally active, competitive muscarinic cholinergic receptors (mAChRs) antagonist. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors. | ||
M3480 | Tolvaptan | Vasopressin Receptor |
OPC-41061 | ||
Tolvaptan is a selective, competitive arginine vasopressin receptor 2 antagonist with an IC50 of 1.28μM for the inhibition of AVP-induced platelet aggregation. | ||
M3947 | ELN 441958 | Bradykinin Receptor |
ELN-441958 is a potent, neutral, competitive and selective oral bioavailable bradykinin B1 receptor antagonist with a Ki of 0.26 nM against native human bradykinin B1 receptor. | ||
M1565 | Quetiapine sulfoxide | 5-HT Receptor |
Quetiapine sulfoxide; Quetiapine S-oxide | ||
Quetiapine sulfoxide is a 5-HT receptor agonist with a pEC50 value of 4.77 for human 5-HT1A. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 value of 6.33 for human D2. | ||
M1564 | Quetiapine Sulfone | 5-HT Receptor |
Quetiapine Sulfone is a 5-HT receptor agonist with a pEC50 value of 4.77 for human 5-HT1A. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 value of 6.33 for human D2. | ||
M4833 | Eliprodil | GluR |
SL-820715 | ||
Eliprodil is a non-competitive NR2B-NMDA receptor antagonist(IC50=1 uM), less potent for NR2A- and NR2C-containing receptors(IC50> 100 uM). | ||
M5135 | Ro-46-2005 | Endothelin Receptor |
Ro 46-2005 is a novel synthetic non-peptide endothelin receptor antagonist, inhibits the specific binding of 125I-ET-1 to human vascular smooth muscle cells (ETA receptor) with IC50 of 220 nM. | ||
M5942 | Roxatidine Acetate HCl | Histamine Receptor |
HOE 760 | ||
Roxatidine Acetate HCl is a specific and competitive histamin H2-receptor antagonist, with IC50 of 3.2 μM, inhibits gastric acid secretion and ulcer formation. | ||
M6374 | A-804598 | P2 Receptor |
A804598 | ||
A-804598 is a CNS penetrant, competitive and selective P2X7 receptor antagonist with IC50s of 9 nM, 10 nM and 11 nM for mouse, rat and human P2X7 receptors, respectively. | ||
M6416 | AGN 193109 | RAR/RXR |
AGN193109 | ||
AGN 193109 is a high affinity pan-RAR (retinoic acid receptors) antagonist, with Kds of 2 nM, 2 nM, and 3 nM for RARα, RARβ, and RARγ, respectively. | ||
M6457 | AR-C 118925XX | P2 Receptor |
ARC118925XX | ||
AR-C 118925XX is a selective, competitive P2Y2 receptor antagonist. AR-C 118925XX is inactive against a panel of 37 other receptors at a concentration of 10 μM. AR-C 118925XX inhibits ATP-γS-induced mucin secretion in bronchial epithelial cells (IC50 = 1 μM). AR-C 118925XX inhibits P2Y2 receptor-induced β-arrestin translocation in vitro (pA2 = 37.2-51.3 nM). | ||
M6621 | Conantokin-R | Others |
Con-R | ||
Conantokin-R is a potent, non-competitive NMDA receptor peptide antagonist with an IC50 of 93 nM.Conantokin-R is also NR2 subunit selective. It inhibits the inward current induced by NMDA in CNS neurons (IC50 = 350 nM). In addition, Conantokin R bound to Zn2+ and Mg2+ with Kd of 0.15 μM and 6.5 μM, respectively. | ||
M7327 | Lintitript | Cholecystokinin Receptor |
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). | ||
M7581 | Dizocilpine maleate | NMDA |
Dizocilpine hydrogen maleate; (+)-MK 801 maleate; MK-801 maleate | ||
Dizocilpine maleate (MK-801 maleate) is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes. | ||
M7796 | Fluspirilene | Calcium Channel |
Fluspirilene is a non-competitive L-type calcium channel antagonist (IC50 = 0.03μM). It is also a dopamine receptor antagonist and can be used as a precursor structure for the development of 20S proteasome agonists. | ||
M8278 | MLS000389544 | Others |
MLS000389544 is a selective and potent methylsulfonylnitrobenzoa |
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M8349 | AE9C90CB | Others |
AE9C90CB is a muscarinic acetylcholine receptor antagonist with 20-fold selectivity for M3 receptor subtypes compared to M2. | ||
M8437 | BMS-195614 | Others |
BMS-195614 (BMS614) is a potent neutral retinoic acid receptor RARα selective antagonist with an IC50 of 2. | ||
M8700 | PCS1055 dihydrochloride | Others |
PCS1055 is a potent and selective muscarinic M4 acetylcholine receptor competitive antagonist that exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. | ||
M9839 | Lemborexant | OX Receptor |
E-2006 | ||
Lemborexant (E-2006) is an orally active, competitive and reversible dual OX1 and OX2 receptors antagonist, with IC50 values of 6.1 nM and 2.6 nM, respectively. | ||
M10654 | Ajmalicine (Raubasine) | Adrenergic Receptor |
Raubasine | ||
Ajmalicine (Raubasine) is an adrenolytic agent which preferentially blocks alpha 1-adrenoceptor than alpha 2-adrenoceptor. Ajmalicine (Raubasine) is an reversible non-competitive nicotine receptor antagonist with an IC50 of 72.3 μM. | ||
M10916 | RO 46-8443 | Endothelin Receptor |
RO 46-8443 is the first non-peptide endothelin ETB receptor selective antagonist. RO 46-8443 displays up to 2000-fold selectivity for ETB receptors both in terms of binding inhibitory potency and functional inhibition. | ||
M11344 | JMV 2959 | Ghrelin Receptor/GHSR |
JMV 2959 is a growth hormone secretin receptor type 1A (GHS-R1A) antagonist that acts on LC-PK1 cells and inhibits GHS-R1A with an IC50 value of 32±3 nM. | ||
M13375 | Cetrorelix Acetate | LHRH/GnRH |
Cetrorelix Acetate (SB-75 acetate) is a potent gonadotropin-releasing hormone (GnRH) receptor antagonist with an IC50 of 1.21 nM. Sequence:Ac-D2Nal-D4Cpa-D3Pal-Ser-Tyr-DCit-Leu-Arg-Pro-DAla-NH2 | ||
M13876 | SB-269970 hydrochloride | 5-HT Receptor |
SB-269970A | ||
SB-269970 hydrochloride is a potent, selective and brain-penetrant 5-HT7 receptor antagonist with a pKi of 8.3. SB-269970 hydrochloride exhibits >50-fold selectivity against other 5-HT receptors. |
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