About 31 results found for searched term "OT-R antagonist 1" (0.063 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M29995 | OT-R antagonist 1 | Oxytocin Receptor |
| Oxytocin receptor antagonist 1 | ||
| OT-R antagonist 1 is a new potent and selective nonpeptide low molecular weight OT-R antagonist. OT-R antagonist 1 inhibits oxytocin-evoked intracellular Ca2+ mobilization (IC50 = 8 nM). | ||
| M1816 | Zibotentan | Endothelin Receptor |
| ZD4054 | ||
| Zibotentan (ZD4054) is a more selective and specific endothelin-A receptor (ETAR) antagonist with an IC50 value of 21 nM. | ||
| M1846 | SB-705498 | TRP Channel |
| SB705498 | ||
| SB-705498 is a potent, selective and orally bioavailable transient receptor potential vanilloid 1 (TRPV1) receptor antagonist with a pIC50 of 7.1. | ||
| 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. | ||
| M2105 | Azilsartan medoxomil | Angiotensin Receptor |
| TAK-491 | ||
| Azilsartan Medoxomil is an effective angiotensin II Type 1 (AT1) receptor antagonist that inhibits RAAS more than 10,000 times more selectively than AT2, and is used to study hypertension. | ||
| M2124 | MK-6096 | OX Receptor |
| Filorexant | ||
| MK-6096 is an orally bioavailable potent and selective reversible antagonist of OX(1)R and OX(2)R. | ||
| M2133 | MK-3207 hydrochloride | CGRP Receptor |
| MK-3207 hydrochloride is a potent CGRP receptor antagonist with IC50 of 0.12 nM. | ||
| M2266 | Pizotifen malate | 5-HT Receptor |
| Sandomigran, pizotyline | ||
| Pizotifen malate is a potent 5-HT2 receptor antagonist, with a high affinity for 5-HT1C binding site. | ||
| M2383 | AMG-517 | TRP Channel |
| AMG 517 is a potent and selective TRPV1 antagonist, antagonizes capsaicin, proton, and heat activation of TRPV1 with IC50 of 0.76 nM, 0.62 nM and 1.3 nM. | ||
| M2418 | AZD1981 | GPR/FFAR |
| AZD1981 is a potent, selective CRTh2 (DP2) receptor antagonist with IC50 of 4 nM, showing >1000-fold selectivity over more than 340 other enzymes and receptors, including DP1. | ||
| M2650 | Doxepin hydrochloride | Histamine Receptor |
| Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2. | ||
| M2674 | Eprosartan Mesylate | Angiotensin Receptor |
| Futuran; Navixen | ||
| Eprosartan is a nonpeptide angiotensin II receptor antagonist, [3H]-eprosartan binds to the AT1 receptor with KD of 0.83 nM in rat vascular smooth muscle cells. | ||
| M2784 | JNJ-7777120 | Histamine Receptor |
| JNJ-7777120 is the first potent and selective non-imidazole histamine H4 receptor antagonist with Ki of 4.5 nM, exhibits >1000-fold selectivity over the other histamin receptors. | ||
| M2869 | MRS 2578 | P2 Receptor |
| MRS2578 is a potent P2Y6 receptor antagonist with IC50 of 37 nM, exhibits insignificant activity at P2Y1, P2Y2, P2Y4,and P2Y11 receptors. | ||
| M3106 | UNC1215 | Epigenetic Reader Domain |
| UNC1215 is a potent and selective MBT (malignant brain tumor) antagonist, which binds L3MBTL3 with IC50 of 40 nM and Kd of 120 nM, 50-fold selective versus other members of the human MBT family. | ||
| M3123 | Vorapaxar | PAR |
| SCH 530348 | ||
| Vorapaxar (SCH 530348) is a potent and orally active thrombin receptor (PAR-1) antagonist with Ki of 8.1 nM. | ||
| M3275 | Irbesartan | Angiotensin Receptor |
| SR-47436; BMS-186295 | ||
| Irbesartan (SR-47436, BMS-186295) is a highly potent and specific angiotensin II type 1 (AT1) receptor antagonist with IC50 of 1.3 nM. | ||
| M3417 | Clozapine | 5-HT Receptor |
| HF 1854 | ||
| Clozapine is a potent 5-HT1C receptor antagonist with an IC50 of 110 nM for 5-HT-stimulated phosphoinositide hydrolysis. | ||
| M3481 | WAY-100635 Maleate | 5-HT Receptor |
| WAY-100635 maleate is a potent, selective 5-HT1A receptor antagonist with an IC50 value of 0.91 nM, a Ki value of 0.39 nM, and a pIC50 of 8.87, which is more than 100-fold more selective than for use at the other 5-HT receptor subtypes and major neurotransmitter receptors. In addition, WAY-100635 maleate is a potent dopamine D4 receptor agonist. | ||
| M3507 | Valsartan | Angiotensin Receptor |
| CGP 48933 | ||
| Valsartan is an angiotensin II receptor antagonist with IC50 of ranging from 39.5 to 116 μM. | ||
| M3618 | MK-0974 | CGRP Receptor |
| Telcagepant | ||
| MK-0974 (Telcagepant) is a highly potent, selective and orally bioavailable CGRP receptor antagonist with Ki values of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors respectively. | ||
| M3760 | TCS-1102 | OX Receptor |
| TCS 1102 is a potent, dual orexin receptor antagonist (Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively). | ||
| M3818 | Rotigotine Hydrochloride | Dopamine Receptor |
| Rotigotine HCl;N-0923 Hydrochloride | ||
| Rotigotine Hydrochloride (N-0923 Hydrochloride) is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Ki of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor. | ||
| 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. | ||
| M9117 | W-54011 | Immunology/Inflammation |
| W-54011 HCl | ||
| W-54011 is a potent, specific, and orally active CD88 (C5a receptor) antagonist, which inhibits the binding of 125I-labeled C5a to human neutrophils with a Ki value of 2.2 nM. | ||
| 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. | ||
| M5290 | (±)-SLV-319 | Cannabinoid |
| (±)-Ibipinibant; BMS-646256 | ||
| (±)-SLV319 (Ibipinabant) is a potent and selective CB1 receptor antagonist (Ki = 7.8 nM). Exhibits 1000-fold selectivity for CB1 over CB2 receptors. Inhibits CP 55,940-induced hypotension and WIN 55,212-2-induced hypothermia in vivo. | ||
| M5291 | Sufugolix | LHRH/GnRH |
| TAK-013 | ||
| Sufugolix (TAK-013) is a highly potent and orally available luteinizing hormone-releasing hormone LHRH receptor antagonist with an IC50 of 0.1 nM. | ||
| M5403 | Alvimopan dihydrate | Opioid Receptor |
| LY 246736 dihydrate; ADL 8-2698 dihydrate | ||
| Alvimopan dihydrate (ADL 8-2698 dihydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan dihydrate has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). | ||
| M5467 | Brexpiprazole | Dopamine Receptor |
| OPC-34712, OPC 34712, OPC34712 | ||
| Brexpiprazole is a novel D2 dopamine and serotonin 1A partial agonist, called serotonin-dopamine activity modulator (SDAM), and a potent antagonist of serotonin 2A receptors, noradrenergic alpha 1B and 2C receptors. | ||
| M5544 | Cyproterone Acetate | Androgen Receptor |
| Cyproterone acetate is an androgen receptor (AR) antagonist with IC50 of 7.1 nM. | ||
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