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Purity: ≥98%
LP-211 is a potent and selective 5-HT7 receptor agonist with a Ki of 0.58 nM at rat cloned 5-HT7 receptors. It exhibits high selectivity against the D2 receptor (Ki=142 nM) and the 5-HT1A receptor (Ki of 188 nM) ((324- and 245-fold, respectively)). LP-211 exhibits agonist characteristics and can cross the blood-brain barrier (EC 50 = 0.60 microM, maximal effect = 82%). LP-211 entered the brain of mice shortly after intraperitoneal injection and quickly made its way into the systemic circulation. Its brain concentration-time profile resembled that of plasma, suggesting that LP-211 diffuses freely and quickly across the blood-brain barrier. N-dealkylation converts LP-211 into the corresponding 1-arylpiperazine metabolite.
| Targets |
5-HT7 Receptor ( Ki = 0.58 nM ); 5-HT1A Receptor ( Ki = 188 nM ); D2 Receptor ( Ki = 142 nM )
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| ln Vitro |
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| Enzyme Assay |
In the experiment, [3H]-LSD binds to a rat cloned 5-HT7 receptor. 30-gram membranes with 2.5 nM [3H]-LSD and LP-211 (6−9 concentrations) are suspended in 1 milliliter of the incubation buffer (50 milliliters of Tris, 10 milliliters of MgCl2, and 0.5 milliliters of EDTA, pH 7.4). At 37°C, the samples are incubated for 60 minutes. Using GF/A glass fiber filters that have been presoaked in 0.5% polyethylenimine for 30 minutes, the incubation is quickly stopped. An ice-cold buffer (50 mM Tris, pH 7.4) measuring 3 x 53 mL is used to wash the filters. In the presence of 10 μM 5-CT, nonspecific binding is identified. Under these conditions, about 90% of specific binding is determined[1].
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| References |
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| Molecular Formula |
C30H34N4O
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| Molecular Weight |
466.63
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| Exact Mass |
466.27
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| Elemental Analysis |
C, 77.22; H, 7.34; N, 12.01; O, 3.43
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| CAS # |
1052147-86-0
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| Appearance |
Solid powder
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| SMILES |
C1CN(CCN1CCCCCC(=O)NCC2=CC=C(C=C2)C#N)C3=CC=CC=C3C4=CC=CC=C4
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| InChi Key |
BQEDZLDNNBDKDS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C30H34N4O/c31-23-25-14-16-26(17-15-25)24-32-30(35)13-5-2-8-18-33-19-21-34(22-20-33)29-12-7-6-11-28(29)27-9-3-1-4-10-27/h1,3-4,6-7,9-12,14-17H,2,5,8,13,18-22,24H2,(H,32,35)
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| Chemical Name |
N-[(4-cyanophenyl)methyl]-6-[4-(2-phenylphenyl)piperazin-1-yl]hexanamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.36 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.36 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.36 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1430 mL | 10.7151 mL | 21.4303 mL | |
| 5 mM | 0.4286 mL | 2.1430 mL | 4.2861 mL | |
| 10 mM | 0.2143 mL | 1.0715 mL | 2.1430 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Dose-response curves for effects of saline (mg/kg, i.p.) on bladder capacity in SCI, intact and sham rats.Am J Transl Res.2016 Jun 15;8(6):2525-33. |
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Effect of antagonist SB-269970 (0.1 mg/kg, i.p.) on dose-response effects of LP-211 (mg/kg, i.p.) on bladder capacity in SCI, intact and sham rats.Am J Transl Res.2016 Jun 15;8(6):2525-33. |
Effect of antagonist SB-269970 (0.1 mg/kg, i.p.) on dose-response effects of LP-211 (mg/kg, i.p.) on micturition volume in SCI, intact and sham rats.Am J Transl Res.2016 Jun 15;8(6):2525-33. |
 Effect of antagonist SB-269970 (0.1 mg/kg, i.p.) on dose-response effects of LP-211 (mg/kg, i.p.) on micturition volume in SCI, intact and sham rats.Am J Transl Res.2016 Jun 15;8(6):2525-33. |
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 Dose-response curves for effects of saline (mg/kg, i.p.) on first urine drop micturition in SCI, intact and sham rats.Am J Transl Res.2016 Jun 15;8(6):2525-33. |
Dose-response curves for effects of LP-211 (mg/kg, i.p.) on first urine drop micturition in SCI, intact and sham rats.Am J Transl Res.2016 Jun 15;8(6):2525-33. |
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