RL648_81 | CAS#1919050-87-5

RL648_81
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 525434

CAS#: 1919050-87-5

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

Chemical Structure

RL648_81

CAS# 1919050-87-5

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 525434
Name: RL648_81
CAS#: 1919050-87-5
Chemical Formula: C17H17F4N3O2
Exact Mass: 371.13
Molecular Weight: 371.340
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
25mg	USD 850
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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

More Info:

Product Data:

Product Data

Instruction:

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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

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	Ethanol	100.0	269.30

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:	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 vivo protocol:	To be determined

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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.

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