About 31 results found for searched term "TR antagonist 1" (0.077 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M14798 | TR antagonist 1 | Others |
| TR antagonist 1 is a high-affinity thyroid hormone receptor (TR) antagonist with IC50s of 36 and 22 nM for TRα and TRβ, respectively. | ||
| 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. | ||
| 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. | ||
| M2757 | Homatropine Bromide | AChR/AChE |
| Homatropine hydrobromide | ||
| Homatropine Bromide is muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively. | ||
| M2758 | Homatropine Methylbromide | AChR/AChE |
| Homatropine methobromide | ||
| Homatropine Methylbromide is muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively. | ||
| M2934 | Phenazopyridine hydrochloride | TRP Channel |
| Phenazopyridine HCl is a competitive SARM1 inhibitor as well as a TRPM8 antagonist with an IC50 for SARM1 inhibition of 145 μM. It has local anesthetic/analgesic activity and can be used in studies related to traumatic brain injury, peripheral neuropathy, and neurodegenerative diseases. | ||
| M2954 | PPADS Tetrasodium Salt | P2 Receptor |
| PPADS tetrasodium salt is a non-selective P2 purinergic antagonist blocking recombinant P2X1, P2X2, P2X3, P2X5 with IC50 of 1-2.6 μM, native P2Y2-like with IC50 of ~ 0.9 mM, and recombinant P2Y4 receptors with IC50 of ~ 15 mM | ||
| M3006 | Sertraline hydrochloride | 5-HT Receptor |
| Sertraline hydrochloride is a 5-HT antagonist with Ki of 13 nM. | ||
| 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. | ||
| M3570 | Candesartan Cilexetil | ATM/ATR |
| TCV-116 | ||
| Candesartan Cilexetil is a specific nonpeptide Ang II receptor (ATR) antagonist and the procompound of candesartan which is an ATR antagonist with an IC50 of 15 μg/kg. | ||
| 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. | ||
| M5074 | ANA-12 | Trk |
| ANA-12 is a selective TrkB antagonist with Kd of 10 nM and 12 μM for the high and low affinity sites, respectively. | ||
| M5835 | Ondansetron Hydrochloride Dihydrate | 5-HT Receptor |
| GR 38032; SN 307; NSC 665799 | ||
| Ondansetron is a highly specific and selective serotonin 5-HT3 receptor antagonist (Ki=6.16 nM), with low affinity for dopamine receptors. | ||
| M5902 | Progesterone | Animal Modeling |
| Pregn-4-ene-3,20-dione | ||
| Progesterone is an endogenous steroid hormone involved in the menstrual cycle, pregnancy, and embryogenesis of humans and other species. A potent agonist of the nuclear progesterone receptor (nPR) with Kd of 1 nM; An agonist of the membrane progesterone receptors(mPRs); An antagonist of the σ1 receptor. It can be used to construct a model of melasma as well as a model of fibrocystic hyperplasia of the breast. | ||
| M6198 | Verucerfont | CRFR |
| GSK561679 | ||
| Verucerfont is a corticotropin-releasing factor receptor 1 (CRF1) antagonist with IC50s of ~6.1, >1000 and >1000 nM for CRF1, CRF2, and CRF-BP, respectively. | ||
| M6303 | JNJ-31020028 | Neuropeptide Receptor |
| JNJ-31020028 is a selective brain penetrant antagonist of neuropeptide Y2 receptor with high affinity(pIC50=8.07, human; pIC50=8.22 rat); >100-fold selective versus human Y1/Y4/Y5 receptors. | ||
| M6494 | BCTC | TRP Channel |
| BCTC is a tRPV1 antagonist. BCTC is also a potent and specific inhibitor of transient receptor potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells. | ||
| M6710 | Endoxifen Z-isomer hydrochloride | Estrogen Receptor |
| Endoxifen Z-isomer HCl | ||
| Endoxifen Z-isomer hydrochloride is a Tamoxifen metabolite and a potent estrogen receptor (ER) antagonist that concentration-dependently inhibits hERG with an IC50 value of 1.6 μM. | ||
| M7353 | Tamoxifen | Estrogen Receptor |
| ICI47699; Z-Tamoxifen; trans-Tamoxifen | ||
| Tamoxifen is an orally active, selective estrogen receptor partial agonist/antagonist. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 µM and 1.8 µM, respectively. | ||
| M7387 | TCS 5861528 | TRP Channel |
| Chembridge-5861528 | ||
| TCS 5861528 (Chembridge-5861528) is a potent TRPA1 channel antagonist that antagonizes similarly allyl isothiocyanate- and 4-HNE-evoked TRPA1 responses, with IC50 values of 14.3 μM and 18.7 μM, respectively. | ||
| M7534 | SSR240612 | Bradykinin Receptor |
| Treatment with the kinin B1 receptor antagonist, SSR240612, provided a protective effect against organ damage by interfering with multiple target functions, including the suppression of B1R-induced inflammation and platelet aggregation. | ||
| M7886 | LY255283 | Leukotriene Receptor |
| LY255283 is a competitive leukotriene B4 receptor antagonist, with an IC50 of about 100 nM. | ||
| M8504 | EPPTB | TAAR |
| EPPTB is a potent, selective trace amine-associated receptor 1 (TAAR1) antagonist with an IC50 value of 28 nM for mouse TAAR1. EPPTB is less selective in rats and humans, with IC50 values of 4539 nM and 7487 nM, respectively. | ||
| M8611 | Ex26 | S1P Receptor |
| Ex26 is a peripherally-restricted biphenylcarboxamide derivative that acts as a highly potent and subtype-selective S1P1 antagonist (IC50 = 0.93 nM against S1PR1 and >3.1 μM against S1PR2/3/4/5). | ||
| M8665 | Landiolol hydrochloride | Adrenergic Receptor |
| Landiolol is an ultra-short acting cardioselective β-adrenoceptor antagonist the exhibit β1-selectivity. | ||
| M8762 | Cangrelor tetrasodium salt | P2 Receptor |
| Canrelor is an adenosine triphosphate analog as well as a potent and selective platelet P2Y12 antagonist and a non-specific GPR17 antagonist. | ||
| M8766 | Atrasentan hydrochloride | Endothelin Receptor |
| ABT-627 hydrochloride; Abbott 147627 | ||
| Atrasentan hydrochloride (ABT-627 hydrochloride) is a potent, orally active, selective endothelin A (ETA) receptor antagonist that inhibits ETA activity and blocks endothelin-induced cellular proliferation with an IC50 value of 0.0551 nM. It can be used in studies related to prostate cancer as well as IgA nephropathy (IgAN). It can be used in prostate cancer and IgA nephropathy (IgAN) related studies. | ||
| M9197 | Relugolix | LHRH/GnRH |
| Orgovyx; TAK-385; RVT-601 | ||
| Relugolix, also known as TAK-385, is an orally active gonadotropin-releasing hormone (GnRH) antagonist with an IC50 of 0.12 nM. | ||
| M9569 | Etrumadenant | Adenosine Receptor |
| AB928; A2aR/A2bR antagonist-1 | ||
| Etrumadenant (AB928, A2aR/A2bR antagonist-1) is an orally bioavailable, dual antagonist of the A2aR and A2bR adenosine receptors, leads to greater immunomodulatory activity and reduced tumor growth. | ||
| M9652 | CB1-IN-1 | Cannabinoid |
| DBPR211; BPRCB1184 | ||
| CB1-IN-1 is a novel potent restricted CB1R antagonist with Ki of 0.3 nM and 21 nM for CB1R and CB2R, respectively. | ||
| M9740 | Aurintricarboxylic acid | P2 Receptor |
| ATA | ||
| Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50 values of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively. | ||
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