RL648_81 | CAS#1919050-87-5 | KCNQ2/3 channel activator

MedKoo Cat#: 525434 | Name: RL648_81

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Description:

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

RL648_81 is a novel potent and selective activator of KCNQ2/3 channels.

Chemical Structure

RL648_81

CAS#1919050-87-5

Theoretical Analysis

MedKoo Cat#: 525434

Name: RL648_81

CAS#: 1919050-87-5

Chemical Formula: C17H17F4N3O2

Exact Mass: 371.1257

Molecular Weight: 371.34

Elemental Analysis: C, 54.99; H, 4.61; F, 20.46; N, 11.32; O, 8.62

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 295.00
25mg	USD 850.00

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Related CAS #

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Synonym

RL648_81

IUPAC/Chemical Name

Ethyl (2-amino-3-fluoro-4-((4-(trifluoromethyl)benzyl)amino)phenyl)carbamate

InChi Key

MVSMZQRRMPUGHI-UHFFFAOYSA-N

InChi Code

InChI=1S/C17H17F4N3O2/c1-2-26-16(25)24-13-8-7-12(14(18)15(13)22)23-9-10-3-5-11(6-4-10)17(19,20)21/h3-8,23H,2,9,22H2,1H3,(H,24,25)

SMILES Code

O=C(OCC)NC1=CC=C(NCC2=CC=C(C(F)(F)F)C=C2)C(F)=C1N

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 ethanol

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in ethanol

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

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Product Data

Product Data

Instruction

View handling instruction

Biological target:

RL648_81 is a specific KQT-like subfamily 2/3 (KCNQ2/3) activator with an EC50 of 190 nM. RL648_81 shifts the V1/2 of KCNQ2/3 channels towards hyperpolarized potentials. RL648_81 does not shift the V1/2 of either KCNQ4 or KCNQ5.RL648_81 has the potential for neurologic disorders associated with neuronal hyperexcitability research.

In vitro activity:

RL648_81 is >15 times more potent and also more selective than retigabine. This study suggests that RL648_81 is a promising clinical candidate for treating or preventing neurologic disorders associated with neuronal hyperexcitability. Reference: Mol Pharmacol. 2016 Jun;89(6):667-77. https://pubmed.ncbi.nlm.nih.gov/27005699/

In vivo activity:

To be determined

	Solvent	mg/mL	mM
Solubility
	Ethanol	100.0	269.30

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 371.34 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. Shi S, Li J, Sun F, Chen Y, Pang C, Geng Y, Qi J, Guo S, Wang X, Zhang H, Zhan Y, An H. Molecular Mechanisms and Structural Basis of Retigabine Analogues in Regulating KCNQ2 Channel. J Membr Biol. 2020 Apr;253(2):167-181. doi: 10.1007/s00232-020-00113-6. Epub 2020 Mar 13. PMID: 32170353. 2. Kumar M, Reed N, Liu R, Aizenman E, Wipf P, Tzounopoulos T. Synthesis and Evaluation of Potent KCNQ2/3-Specific Channel Activators. Mol Pharmacol. 2016 Jun;89(6):667-77. doi: 10.1124/mol.115.103200. Epub 2016 Mar 22. PMID: 27005699.

In vitro protocol:

In vivo protocol:

To be determined

1: Kumar M, Reed N, Liu R, Aizenman E, Wipf P, Tzounopoulos T. Synthesis and Evaluation of Potent KCNQ2/3-Specific Channel Activators. Mol Pharmacol. 2016 Jun;89(6):667-77. doi: 10.1124/mol.115.103200. Epub 2016 Mar 22. PubMed PMID: 27005699. Shi S, Li J, Sun F, Chen Y, Pang C, Geng Y, Qi J, Guo S, Wang X, Zhang H, Zhan Y, An H. Molecular Mechanisms and Structural Basis of Retigabine Analogues in Regulating KCNQ2 Channel. J Membr Biol. 2020 Apr;253(2):167-181. doi: 10.1007/s00232-020-00113-6. Epub 2020 Mar 13. PMID: 32170353.