LP-211 | CAS#1052147-86-0 | 5-HT7 receptor Agonist

MedKoo Cat#: 532114 | Name: LP-211

Description:

WARNING: This product is for research use only, not for human or veterinary use.

LP-211 is a a selective agonist of the serotonin 5-HT7 receptor with a Ki value of 0.58 nM at rat cloned 5-HT7 receptors, and >300-fold selectivity over the 5-HT1A receptor.

Chemical Structure

LP-211

CAS#1052147-86-0

Theoretical Analysis

MedKoo Cat#: 532114

Name: LP-211

CAS#: 1052147-86-0

Chemical Formula: C30H34N4O

Exact Mass: 466.2733

Molecular Weight: 466.63

Elemental Analysis: C, 77.22; H, 7.34; N, 12.01; O, 3.43

Price and Availability

Size	Price	Availability
50mg	USD 250.00	Ready to ship
100mg	USD 450.00	Ready to ship
200mg	USD 850.00	Ready to ship
500mg	USD 1,750.00	Ready to ship
1g	USD 2,950.00	Ready to ship
2g	USD 4,950.00	Ready to ship
5g	USD 7,250.00	2 weeks

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Related CAS #

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Synonym

LP-211; LP 211; LP211.

IUPAC/Chemical Name

N-[(4-cyanophenyl)methyl]-6-[4-(2-phenylphenyl)piperazin-1-yl]hexanamide

InChi Key

BQEDZLDNNBDKDS-UHFFFAOYSA-N

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)

SMILES Code

O=C(NCC1=CC=C(C#N)C=C1)CCCCCN2CCN(C3=CC=CC=C3C4=CC=CC=C4)CC2

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#T9D11P15

QC Data

View QC data: current batch, Lot#T9D11P15

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

LP-211 is a 5-HT7 receptor agonist with a Ki of 0.58 nM.

In vitro activity:

LP-211 induced a significant depolarization of the dendritic membrane potential (baseline − 66.16 ± 1.33 mV; LP-211 − 64.96 ± 1.21 mV, n = 5; p < 0.05). In parallel, the voltage sag in response to a hyperpolarizing current step increased (baseline 1.37 ± 0.07, LP-211 1.5 ± 0.08, n = 5; p < 0.05), indicating an enhancement of HCN (hyperpolarization-activated-and-cyclic-nucleotide-regulated) channel function (Fig. 2A–C). LP-211 had no influence on synaptic function, i.e. no influence on the amplitude or coefficient of variation of evoked EPSPs (excitatory postsynaptic potentials) (Fig. 2D, E, amplitude: baseline 5.42 ± 0.57 mV, LP-211 5.26 ± 0.56 mV; CV2: baseline 29.59 ± 1.14, LP-211 22.67 ± 4.06, n = 10; p > 0.05), suggesting no modulation of pre- and post-synaptic function by 5-HT7Rs. Instead, there was a reduction in the single EPSP integral (baseline 143 ± 16 ms·mV, LP-211128 ± 16 ms·mV, n = 10; p < 0.05) as well as a reduction in EPSP summation, evaluated from the paired-pulse ratio of two EPSPs evoked at 50 Hz (Fig. 2F, second/first amplitude: baseline 2.10 ± 1.0, LP-211 1.73 ± 0.12, n = 10; p < 0.05). These results suggested that activation of 5-HT7Rs by LP-211 lead to an increase in HCN channel function resulting in accelerated EPSP repolarization and a reduction in dendritic integration. Reference: Neurobiol Dis. 2017 Oct;106:214-221. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5560654/

In vivo activity:

The effect of a 5-HT7 receptor agonist, LP-211 (N-(4-cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide) on micturition reflex in acute spinal cord-injured (SCI) rats during infusion of vehicle into the bladder was investigated. Intact and sham-operated rats showed few significant changes in micturition reflex. SCI rats responded to LP-211 (0.003-0.3, mg/kg, i.v.) with dose-dependent increases in bladder capacity, and residual volume. LP-211 induced significant dose-dependent increases in micturition volume, resulting in significant increases in voiding efficiency (P<0.001) compared to intact and sham-operated rats, SB-269970 (0.1 mg/kg, i.v.) completely reversed the LP-211-induced changes on micturition volume and voiding efficiency was decreased significantly. Reference: Am J Transl Res. 2016 Jun 15;8(6):2525-33. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4931148/

	Solvent	mg/mL	mM
Solubility
	DMSO	100.0	214.30
	Ethanol	50.0	107.15

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 466.63 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Santello M, Bisco A, Nevian NE, Lacivita E, Leopoldo M, Nevian T. The brain-penetrant 5-HT7 receptor agonist LP-211 reduces the sensory and affective components of neuropathic pain. Neurobiol Dis. 2017 Oct;106:214-221. doi: 10.1016/j.nbd.2017.07.005. Epub 2017 Jul 6. PMID: 28690143; PMCID: PMC5560654. 2. Beaudet G, Paizanis E, Zoratto F, Lacivita E, Leopoldo M, Freret T, Laviola G, Boulouard M, Adriani W. LP-211, a selective 5-HT7 receptor agonist, increases novelty-preference and promotes risk-prone behavior in rats. Synapse. 2017 Dec;71(12). doi: 10.1002/syn.21995. Epub 2017 Aug 17. PMID: 28752923. 3. Norouzi-Javidan A, Javanbakht J, Barati F, Fakhraei N, Mohammadi F, Dehpour AR. Effect of 5-HT7 receptor agonist, LP-211, on micturition following spinal cord injury in male rats. Am J Transl Res. 2016 Jun 15;8(6):2525-33. PMID: 27398137; PMCID: PMC4931148.

In vitro protocol:

In vivo protocol:

1. Beaudet G, Paizanis E, Zoratto F, Lacivita E, Leopoldo M, Freret T, Laviola G, Boulouard M, Adriani W. LP-211, a selective 5-HT7 receptor agonist, increases novelty-preference and promotes risk-prone behavior in rats. Synapse. 2017 Dec;71(12). doi: 10.1002/syn.21995. Epub 2017 Aug 17. PMID: 28752923. 2. Norouzi-Javidan A, Javanbakht J, Barati F, Fakhraei N, Mohammadi F, Dehpour AR. Effect of 5-HT7 receptor agonist, LP-211, on micturition following spinal cord injury in male rats. Am J Transl Res. 2016 Jun 15;8(6):2525-33. PMID: 27398137; PMCID: PMC4931148.

1: Norouzi-Javidan A, Javanbakht J, Barati F, Fakhraei N, Mohammadi F, Dehpour AR. Effect of 5-HT7 receptor agonist, LP-211, on micturition following spinal cord injury in male rats. Am J Transl Res. 2016 Jun 15;8(6):2525-33. PubMed PMID: 27398137; PubMed Central PMCID: PMC4931148. 2: Demirkaya K, Akgün ÖM, Şenel B, Öncel Torun Z, Seyrek M, Lacivita E, Leopoldo M, Doğrul A. Selective 5-HT7 receptor agonists LP 44 and LP 211 elicit an analgesic effect on formalin-induced orofacial pain in mice. J Appl Oral Sci. 2016 May-Jun;24(3):218-22. doi: 10.1590/1678-775720150563. PubMed PMID: 27383702; PubMed Central PMCID: PMC5022221.