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Postion:Product Catalog >LP-211
LP-211
  • LP-211

LP-211 NEW

Price $39 $64 $97
Package 2mg 5mg 10mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-19

Product Details

Product Name: LP-211 CAS No.: 1052147-86-0
Purity: 98.65% Supply Ability: 10g
Release date: 2024/11/19

Product Introduction

Bioactivity

NameLP-211
DescriptionLP-211 is a brain penetrant selective agonist for a 5-HT7 receptor (Ki: 0.58 nM), and >300-fold selectivity over the 5-HT1A receptor.
Kinase AssayHuman 5-HT1A serotonin receptors stably expressed in HEK293 cells were radiolabeled with 1.0 nM [3H]-8-OH-DPAT. Samples containing 40 μg of membrane protein and different concentrations of each compound ranging from 0.1 nM to 10 μM were incubated in a final volume of 500 μL of 50 mM Tris-HCl pH 7.4, 5 mM MgSO4 for 120 min at 37 °C. After this incubation time, samples were filtered through GF/C presoaked in polyethylenimine 0.5% for at least 30 min prior to use. The filters were washed twice with 1 mL of ice-cold buffer (50 mM Tris-HCl, pH 7.4). Nonspecific binding was determined in the presence of 10 μM 5-HT [1].
Animal ResearchMice were given the test compounds intraperitoneally (10 mg/kg) and were killed by decapitation at various times thereafter. Mixed arteriovenous trunk blood was collected in heparinized tubes, centrifuged at 3000g for 10 min, and the plasma was stored at -20 °C. Brain was removed immediately, blotted with paper to remove surface blood, and quickly frozen in dry ice. Compounds and their 1-arylpiperazine metabolites were extracted from plasma and brain homogenate and quantified by reversed-phase HPLC with UV detection (230 nm). Briefly: to 0.1 mL of plasma, 0.2 mL of 20 mM of ammonium bicarbonate and 0.02 mL of a methanolic solution of the internal standard (100 μg/mL) were added; samples were then extracted twice with 1.5 mL of hexane containing 1% of isoamyl alcohol, and the combined extracts were evaporated to dryness and reconstituted in 0.15 mL of the mobile phase, which was injected into the chromatographic column. Brain tissue was homogenized in distilled water (1 g/10 mL), and 1 mL of the homogenate was extracted twice with 1.5 mL of hexane/isoamyl alcohol as described for plasma. Then, the organic phase was shaken with 0.2 mL of the mobile phase (LP-211 only); after centrifugation, 0.1 mL of the aqueous phase was injected into the chromatographic column [1].
In vitroLP-211 showed high 5-HT 7 receptor affinity (Ki = 0.58 nM), high selectivity over 5-HT 1A and D 2 receptors (324- and 245-fold, respectively), and agonist properties (maximal effect = 82%, EC 50 = 0.60 microM) [1]. Pretreatment with LP-211 had no effect on Fos-like immunoreactivity but strongly increased the response produced by capsaicin [2].
In vivoAfter intraperitoneal injection in mice, LP-211 (10 mg/kg) rapidly reached the systemic circulation and entered the brain. Its brain concentration-time profile paralleled that in plasma [1]. SCI rats responded to LP-211 (0.003-0.3, mg/kg, i.v.) with dose-dependent increases in bladder capacity and residual volume [3]. LP-211 reduced synaptic integration in layer 5 pyramidal neurons, which was enhanced in neuropathic pain due to a dysfunction of dendritic hyperpolarization-activated-and-cyclic-nucleotide-regulated (HCN) channels [4].
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationDMSO : 90 mg/mL (192.87 mM)
KeywordsInhibitor | 5-HT Receptor | LP211 | Serotonin Receptor | 5-hydroxytryptamine Receptor | inhibit | LP 211 | LP-211
Inhibitors RelatedAlverine citrate | Dapoxetine hydrochloride | CLOZAPINE N-OXIDE | Octopamine hydrochloride | Citicoline | Amitriptyline hydrochloride | Cloperastine hydrochloride | Oxolinic acid | Trazodone hydrochloride | Mianserin hydrochloride | Fluoxetine hydrochloride | Cinchonidine
Related Compound LibrariesAnti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Neurotransmitter Receptor Compound Library | Angiogenesis related Compound Library | NO PAINS Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Hypertension Compound Library

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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