簡介:substance p(1-7) tfa, a fragment of the neuropeptide substance p (sp), induces depressor and bradycardic effects upon application to the nucleus tractus solitarius [1].
簡介:urotensin ii, mouse acetate, serves as an endogenous ligand for the orphan g-protein-coupled receptor gpr14 or senr and acts as a potent vasoconstrictor. its physiological function extends to the central nervous system [1].
簡介:urotensin ii, mouse tfa, an endogenous ligand for the orphan g-protein-coupled receptor gpr14 or senr, serves as a potent vasoconstrictor. it plays a significant physiological role within the central nervous system [1].
簡介:firocoxib (ml 1785713) is a selective non-steroidal inhibitor of cycooxygenase-2 (cox-2) (ic50 of 0.13 μm), with anti-inflammatory for use in dogs and horses.
簡介:calmodulin-dependent protein kinase ii (290-309) acetate is a potent antagonist of camk, exhibiting an ic50 of 52 nm for the inhibition of ca2+/calmodulin-dependent protein kinase ii [1].
簡介:β-amyloid 22-35 (amyloid β-protein 22-35) tfa, a fragment comprising residues 22-35 of the β-amyloid protein, exhibits cytotoxicity towards cultured rat hippocampal neurons in serum-free media. it aggregates and forms typical amyloid fibrils in neutral buffer solution, mirroring those observed with the full-length β-amyloid protein [1].
簡介:sphistin synthetic peptide (12-38, fitc in n-terminal-fluorescently labeled peptide) represents truncated fragments of the parent sphistin synthetic peptide, characterized by the presence of a fluorescent label (fitc) at the n-terminal.
簡介:mambalgin 1 tfa, a selective inhibitor of asic1a (with ic50 values of 192 nm for human asic1a and 72 nm for the asic1a/1b dimer), preferentially binds to the channel in its closed/inactive state. it demonstrates selectivity for asic1a over a range of other channels, including asic2a, asic3, trpv1, p2x2, 5-ht3, nav1.8, cav3.2, and kv1.2. in vivo, mambalgin 1 tfa effectively prolongs the latency of the withdrawal response in mouse tail-flick and paw-flick tests.
簡介:bekm-1 tfa is a potent, selective blocker of the kv11.1 (herg) channel, demonstrating specificity for kv11.1 over 14 other potassium channels. this compound dose-dependently prolongs the qtc interval in isolated rabbit hearts, affirming its role as a selective inhibitor.
簡介:rs 09 tfa, a tlr4 agonist, promotes nf-κb nuclear translocation and induces the secretion of inflammatory cytokines in raw264.7 macrophages in vitro. additionally, as an adjuvant in vivo, rs 09 tfa enhances serum concentrations of x-15 specific antibodies when co-administered with x-15-klh in mice.
簡介:neuropeptide s(rat) tfa, a robust endogenous agonist for the neuropeptide s receptor (nspr) with an ec50 of 3.2 nm, enhances locomotor activity and promotes wakefulness while concurrently diminishing anxiety-like behavior in mice.
簡介:neuropeptide s(mouse) tfa, an endogenous agonist for the neuropeptide s receptor (npsr) with an ec50 value of 3 nm, plays a significant role in physiological processes by inducing the mobilization of intracellular ca2+. this compound elevates locomotor activity and wakefulness, and simultaneously decreases anxiety-like behavior in mice.
簡介:noxa1ds tfa is a potent and selective inhibitor of nadph oxidase 1 (nox1), with an inhibition concentration (ic50) of 20 nm, demonstrating selectivity over nox2, nox4, nox5, and xanthine oxidase. it effectively inhibits nox1-derived o2- production in ht-29 human colon cancer cells and attenuates vegf-induced migration of human pulmonary artery endothelial cells under hypoxic conditions in vitro.
簡介:k-(d-1-nal)-fwll-nh2 tfa is a potent and high-affinity inverse agonist of the ghrelin receptor, exhibiting ki values of 4.9 nm in cos7 cells and 31 nm in hek293t cells. this compound effectively inhibits ghrelin receptor-mediated gq- and g13-dependent signaling pathways.
簡介:rfrp-1(human) tfa, an endogenous npff receptor agonist, exhibits potent activity with ec50 values of 0.0011 nm for npff2 and 29 nm for npff1. it significantly diminishes the contractile function of isolated rat and rabbit cardiac myocytes. moreover, it decreases heart rate, stroke volume, ejection fraction, and cardiac output, while elevating plasma prolactin levels in rats.
簡介:lei-dab7 tfa, a selective and high-affinity blocker of the k ca 2.2 (sk2) channel with a dissociation constant (k d) of 3.8 nm, demonstrates over 200-fold selectivity for k ca 2.2 compared to k ca 2.1, k ca 2.3, k ca 3.1, k v, and kir2.1. furthermore, lei-dab7 tfa enhances theta-burst responses and long-term potentiation (ltp) in rat hippocampal slices in vitro.
簡介:ba 1 tfa acts as a potent agonist for the bombesin (bb) family of receptors, exhibiting high affinity binding to bombesin receptor subtype-3 (brs3), gastrin-releasing peptide receptor (grpr), and neuromedin b receptor (nmbr), with ic50 values of 6, 0.4, and 2.5 nm, respectively [1].
簡介:spadin tfa, a natural peptide originating from a propeptide in blood, acts as a powerful trek-1 channel inhibitor with an ic 50 of 10 nm. it boosts dorsal raphe nucleus 5-ht neurotransmission in mice, activates hippocampal creb, and promotes neurogenesis. this compound is useful for antidepressant research [1] [2].
簡介:tat-cyclo-cllfvy tfa is a cyclic peptide inhibitor specifically targeting hif-1 heterodimerization to mitigate hypoxia signaling within cancer cells. it effectively disrupts the protein-protein interaction between hif-1α and hif-1β, demonstrating an inhibitory concentration (ic 50) of 1.3 μm [1].
簡介:dpc-aj1951 tfa, a 14-amino acid peptide, functions as a potent agonist for the parathyroid hormone (pth)/pth-related peptide receptor (ppr). it has been characterized for its activity through ex vivo and in vivo bone resorption assays [1].
簡介:foxy-5 tfa, a wnt5a agonist and mimicking peptide of wnt5a (a non-canonical wnt family member), induces cytosolic free calcium signaling without altering β-catenin activation. this compound inhibits the migration and invasion of epithelial cancer cells and significantly diminishes the metastatic progression of wnt5a-low prostate cancer cells in an orthotopic mouse model [1] [2] [3] [4].
簡介:norleual tfa, an analog of angiotensin (ang) iv, functions as a hepatocyte growth factor (hgf)/c-met inhibitor, displaying a potent inhibition capability with an ic50 of 3 pm. additionally, it acts as an at4 receptor antagonist and demonstrates significant antiangiogenic activities [1].
簡介:levomefolate calcium is a primary biologically active form of folate used at the cellular level for dna reproduction, the cysteine cycle and the regulation of homocysteine
簡介:z-vrpr-fmk (tfa), a selective and irreversible inhibitor of mucosa-associated lymphoid tissue lymphoma translocation protein 1 (malt1), is a tetrapeptide shown to provide protection against influenza a virus (iav) infection [1].
簡介:myristoylated tfa pep2m (myr-pep2m tfa) is a cell-permeable peptide that effectively disrupts the interactions between the protein kinase ζ (pkmζ) downstream targets—n-ethylmaleimide-sensitive factor/glutamate receptor subunit 2 (nsf/glur2). pkmζ, an autonomously active isozyme of protein kinase c (pkc), plays a crucial role in these interactions [1] [2].
簡介:rvd-hpα tfa is the n-terminally extended form of human hemopressin that acts as a selective cb1 receptor agonist. rvd-hpα tfa increases intracellular ca 2+ levels in cells expressing cb1 receptors in vitro. rvd-hpα tfa also high affinity cb2 positive allosteric modulator (k i =50 nm).
簡介:grk2i tfa, a grk2 inhibitory polypeptide, specifically targets and inhibits the activation of grk2 by gβγ. it mimics the gβγ-binding domain, functioning as a cellular antagonist of gβγ [1].
簡介:ac 187 tfa, a potent and orally active amylin receptor antagonist, exhibits an ic50 of 0.48 nm and a ki of 0.275 nm. it demonstrates greater selectivity for the amylin receptor over calcitonin and cgrp receptors and has been shown to possess neuroprotective effects [1] [2].