GW542573X | CAS# 660846-41-3| KCa2.1 channel activator

MedKoo Cat#: 531945 | Name: GW542573X

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Description:

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

GW542573X is an activator of small-conductance Ca2+-activated K+ channels (KCa2).

Chemical Structure

GW542573X

CAS#660846-41-3

Theoretical Analysis

MedKoo Cat#: 531945

Name: GW542573X

CAS#: 660846-41-3

Chemical Formula: C19H28N2O5

Exact Mass: 364.1998

Molecular Weight: 364.44

Elemental Analysis: C, 62.62; H, 7.74; N, 7.69; O, 21.95

Price and Availability

Size	Price	Availability
5mg	USD 350.00	2 Weeks
10mg	USD 600.00	2 Weeks
25mg	USD 1,050.00	2 Weeks

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Related CAS #

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Synonym

GW542573X; GW 542573X; GW-542573X

IUPAC/Chemical Name

tert-butyl 4-({[(2-methoxyphenyl)carbamoyl]oxy}methyl)piperidine-1-carboxylate

InChi Key

SAXGSDIZIYFNKD-UHFFFAOYSA-N

InChi Code

InChI=1S/C19H28N2O5/c1-19(2,3)26-18(23)21-11-9-14(10-12-21)13-25-17(22)20-15-7-5-6-8-16(15)24-4/h5-8,14H,9-13H2,1-4H3,(H,20,22)

SMILES Code

O=C(N1CCC(COC(NC2=CC=CC=C2OC)=O)CC1)OC(C)(C)C

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

Instruction

View handling instruction

Biological target:

GW 542573X is an activator of small-conductance Ca2+-activated K+ channels (KCa2); selective for KCa2.1 (EC50 = 8.2 μM in HEK293 cells expressing hKCa2.1) with the profile hKCa2.1 > hKCa2.2 = hKCa2.3 > hKCa3.1 (IK).

In vitro activity:

The Ca(2+)-response curve of hSK1 was left-shifted from an EC(50)(Ca(2+)) value of 410 +/- 20 nM (n = 9) to 240 +/- 10 nM (n = 5) in the presence of 10 microM GW542573X. In addition to this positive modulation, GW542573X activated SK1 in the absence of Ca(2+) and furthermore induced a 15% increase in the maximal current at saturating Ca(2+). Thus, GW542573X also acts as a genuine opener of the hSK1 channels, a mechanism of action (MOA) not previously obtained with SK channels. Reference: Mol Pharmacol. 2009 Sep;76(3):569-78. https://pubmed.ncbi.nlm.nih.gov/19515965/

In vivo activity:

TBD

	Solvent	mg/mL	mM
Solubility
	DMSO	36.4	100.00
	Ethanol	36.4	100.00

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 364.44 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. Hougaard C, Jensen ML, Dale TJ, Miller DD, Davies DJ, Eriksen BL, Strøbaek D, Trezise DJ, Christophersen P. Selective activation of the SK1 subtype of human small-conductance Ca2+-activated K+ channels by 4-(2-methoxyphenylcarbamoyloxymethyl)-piperidine-1-carboxylic acid tert-butyl ester (GW542573X) is dependent on serine 293 in the S5 segment. Mol Pharmacol. 2009 Sep;76(3):569-78. doi: 10.1124/mol.109.056663. Epub 2009 Jun 10. PMID: 19515965.

In vitro protocol:

In vivo protocol:

TBD

1: Hougaard C, Jensen ML, Dale TJ, Miller DD, Davies DJ, Eriksen BL, Strøbaek D, Trezise DJ, Christophersen P. Selective activation of the SK1 subtype of human small-conductance Ca2+-activated K+ channels by 4-(2-methoxyphenylcarbamoyloxymethyl)-piperidine-1-carboxylic acid tert-butyl ester (GW542573X) is dependent on serine 293 in the S5 segment. Mol Pharmacol. 2009 Sep;76(3):569-78. doi: 10.1124/mol.109.056663. PubMed PMID: 19515965.