About 31 results found for searched term "p-fin4" (0.139 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M52779 | p-fin4 | GluR |
| p-fin4 is a peptide inhibitor of STEP Phosphatase-GluA2 AMPA receptor interaction with a Ki of 0.4 μM. | ||
| M2145 | Loperamide hydrochloride | Animal Modeling |
| R-18553 hydrochloride | ||
| Loperamide hydrochloride is a high affinity μ-opioid receptor agonist with peripheral selectivity with Ki values of 2, 48 and 1156 nM for μ-, δ- and κ-opioid receptors respectively. Loperamide hydrochloride is also a selective and competitive human intestinal carboxylesterases (hiCE) inhibitor. It can be used to construct animal models of functional constipation. | ||
| 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. | ||
| M2593 | Siramesine hydrochloride | Sigma Receptor |
| Lu 28-179 | ||
| Siramesine (Lu 28-179) hydrochloride is an effective sigma-2 receptor agonist. Siramesine has a nanomolar affinity for sigma-2 receptors (IC50=0.12 nM) and is 140 times more selective for sigma-2 receptors (IC50=17 nM). Siramesine has xC-system inhibitory activity associated with iron death. | ||
| M2592 | Siramesine | Sigma Receptor |
| Lu 28-179 | ||
| Siramesine (Lu 28-179) is a potent sigma-2 receptor agonist. Siramesine has a subnanomolar affinity for sigma-2 receptors (IC50=0.12 nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17 nM). Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. | ||
| M2945 | Pimozide | Dopamine Receptor |
| R6238 | ||
| Pimozide is an antagonist of 6-hydroxyapatide against 6-hydroxyapatide, with Ki values of 1.4 nM, 2.5 nM and 588 nM for 6-hydroxyapatide, D3 and D1 receptors, respectively. Pimozide also has a high affinity for α1-adrenoceptor. Ki value is 39 nM. Pimozide is also an inhibitor of STAT3 and STAT5, and piperimidate triggers ADCD in glioblastoma cell lines (LN-229, MZ-54, GOS-3 and U343) by inducing dephosphorylation and inactivation of mTORC1. | ||
| M2965 | Prucalopride Succinat | 5-HT Receptor |
| R-108512 | ||
| Prucalopride is a selective, high affinity 5-HT4 receptor agonist, inhibiting human 5-HT(4a) and 5-HT(4b) receptor with Ki value of 2.5 nM and 8 nM, respectively. | ||
| M3153 | TTP 22 | Casein Kinase |
| TTP 22 is a high affinity, ATP-competitive casein kinase 2 (CK2) inhibitor with IC50/Ki of 0.1 uM/40 nM. | ||
| M3242 | Sumanirole Maleate | Dopamine Receptor |
| U 95666E; PNU-95666 | ||
| Sumanirole maleate is a highly selective dopamine D2 receptor agonist with binding affinity of 9 nM and EC50 of about 46 nM, exhibits >200-fold selectivity over the other dopamine receptor subtypes. | ||
| M3412 | Propafenone hydrochloride | Sodium Channel |
| Propafenone HCl is a sodium-channel blocker that also has a high affinity for β-receptors (IC50 = 32 nM). It blocks transient outward potassium current (Ito) and sustained delayed rectifier K+ current (Isus) with IC50 values of 4.9 μM and 8.6 μM, respectively.In addition, Propafenone inhibits the proliferation of esophageal cancer by inducing mitochondrial dysfunction and apoptosis. | ||
| M25394 | BPTF-IN-1 | Epigenetic Reader Domain |
| compound AU1 | ||
| BPTF-IN-1 (compound AU1) is a selective bromodomain and PHD finger containing transcription factor (BPTF) bromodomain inhibitor with a Kd of 2.8 μM. BPTF-IN-1 shows to be selective for BPTF over BRD4 bromodomain. | ||
| M3592 | Chlorprothixene | Dopamine Receptor |
| Chlorprothixene has strong binding affinities to dopamine and histamine receptors, such as D1, D2, D3, D5, H1, 5-HT2, 5-HT6 and 5-HT7, with Ki of 18 nM, 2.96 nM, 4.56 nM, 9 nM, 3.75 nM, 9.4 nM, 3 nM and 5.6 nM, respectively. | ||
| M4458 | Tetrahydroberberine | Dopamine Receptor |
| Canadine; THB | ||
| Tetrahydroberberine is an isoquinoline alkaloid isolated from corydalis tuber; has micromolar affinity for dopamine D(2) (pK(i) = 6.08) and 5-HT(1A) (pK(i) = 5.38) receptors but moderate to no affinity for other relevant serotonin receptors (5-HT(1B), 5-HT(1D), 5-HT(3), and 5-HT(4); pK(i) < 5.00). | ||
| M5059 | Furafylline | Cytochrome P450 (e.g. CYP17) |
| Furafylline was a potent, non-competitive inhibitor of high affinity phenacetin O-deethylase activity of microsomal fractions of human liver, a reaction catalysed by P450IA2, with an IC50 value of 0.07 microM. | ||
| M5239 | Batefenterol | Adrenergic Receptor |
| GSK961081; TD-5959 | ||
| Batefenterol (GSK961081;TD-5959) is a novel muscarinic receptor antagonist and β2-adrenoceptor agonist; displays high affinity for hM2, hM3 muscarinic and hβ2-adrenoceptor with Ki values of 1.4, 1.3 and 3.7 nM, respectively. | ||
| M5272 | Bioymifi | TNF Receptor |
| DR5 Activator | ||
| Bioymifi, a small-molecule death receptor 5 (DR5) agonist, binds to the extracellular domain(ECD) of DR5 with a Kd of 1.2 μM but showed little binding affinity to the DR4 ECD. It induces DR5 clustering and aggregation, leading to apoptosis. | ||
| M6206 | ARV-825 | Epigenetic Reader Domain |
| ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 shows affinity to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, 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. | ||
| M6392 | AC 265347 | Calcium-sensing Receptor |
| AC 265347 is a calcium-sensitive receptor (CaSR) agonist and orthosteric modulator (auto-PAM) with a functional affinity (pKB) of 5.1.AC 265347 is used in the study of hyperparathyroidism and related disorders. | ||
| M7213 | Roxindole hydrochloride | Others |
| Roxindole hydrochloride is a dopamine D 2 autoreceptor agonist. Also has affinity for D 3, D 4, 5-HT 1A receptors and the 5-HT transporter. | ||
| M7396 | TCS-OX2-29 | OX Receptor |
| TCS-OX2-29 is a potent, high affinities and selective orexin-2 receptor (OX2R) antagonist with an IC50 value of 40 nM and a pKI value of 7.5. TCS-OX2-29 displays ~250-fold selectivity for OX2 over OX1. | ||
| M7479 | VUF 8430 dihydrobromide | Others |
| VUF 8430 dihydrobromide is a potent, high affinity H 4 agonist. | ||
| M7535 | Siremadlin | Mdm2 |
| NVP-HDM201; HDM201 | ||
| Siremadlin (HDM201) is a novel, highly potent and selective inhibitor of the p53-Mdm2 interaction with affinity constant for Mdm2 in the picomolar range and a selectivity ratio greater than 10000-fold vs Mdm4. | ||
| M8269 | 4-DAMP | AChR/AChE |
| 4-DAMP methiodide | ||
| 4-DAMP (4-DAMP methiodide) is a potent and selective antagonist of M3 receptors and also has a high affinity for the closely-related M5 receptors. 4-DAMP combined with 5-Fluorouracil (5-Fu) could significantly reduce the cell viability and enhance apoptosis in MKN45 and BGC823 gastric cancer cells. | ||
| M9290 | S 38093 | Histamine Receptor |
| S38093 | ||
| S 38093 is an inverse agonist at histamine H3 receptors, displays a moderate affinity for rat, mouse and human H3 receptors with Ki of 8.8, 1.44 and 1.2µM, respectively. | ||
| M10722 | PRE-084 hydrochloride | Sigma Receptor |
| PRE-084 hydrochloride is a highly affinity selective σ1 agonist with an IC50 value of 44 nM in the sigma receptor detection. | ||
| M10841 | Mavatrep | TRP Channel |
| JNJ-39439335 | ||
| Mavatrep is an orally active TRPV1 antagonist with high affinity for the hTRPV1 channel, inhibits the binding of the TRPV1 agonist to [3H]-Resiniferatoxin (Ki=6.5 nM), and has a low effect on the enzymatic activity of CYP subtypes 3A4, 1A2, and 2D6. | ||
| M10856 | MF498 | Prostaglandin Receptor |
| MF498 is a novel selective prostaglandin E4 receptor (EP4 receptor) antagonist with a strong affinity with the EP4 receptor, with a Ki of 0.7 nM. | ||
| M10858 | MK-2894 | Prostaglandin Receptor |
| MK-2894 is a potent, selective, orally active and high affinity (Ki=0.56 nM) full antagonist against E prostanoid receptor 4 (EP4 receptor) (IC50=2.5 nM). MK-2894 possesses potent anti-inflammatory activity in animal models of pain/inflammation and can be used for the research of arthritis. | ||
| M10890 | Spartalizumab | PD-1/PD-L1 |
| Spartalizumab (anti-PD-1) is a human-derived IgG4 antibody against PD-1 that inhibits the binding of PD-L1 and PD-L2 to PD-1. PDR001 binds to PD-1 with high affinity to inhibit its biological activity; MW: 145.8 KD. | ||
| M11328 | FINO2 | Ferroptosis |
| FINO2 is a potent ferroptosis inducer. FINO2 inhibits GPX4 activity. FINO2 is a stable oxidant that oxidizes ferrous iron and stable at varying pH levels. FINO2 causes widespread lipid peroxidation. | ||
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