GSK4716 | CAS#101574-65-6 |ERRβ & ERRγ Agonist

MedKoo Cat#: 531876 | Name: GSK4716

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Description:

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

GSK4716 is a selective agonist at estrogen-related receptors ERRβ and ERRγ. GSK4716 displays selectivity over ERRα and the classical estrogen receptors.

Chemical Structure

GSK4716

CAS#101574-65-6

Theoretical Analysis

MedKoo Cat#: 531876

Name: GSK4716

CAS#: 101574-65-6

Chemical Formula: C17H18N2O2

Exact Mass: 282.1368

Molecular Weight: 282.34

Elemental Analysis: C, 72.32; H, 6.43; N, 9.92; O, 11.33

Price and Availability

Size	Price	Availability
10mg	USD 250.00	2 Weeks
25mg	USD 450.00	2 Weeks
50mg	USD 750.00	2 Weeks

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Related CAS #

No Data

Synonym

GSK4716; GSK 4716; GSK-4716

IUPAC/Chemical Name

4-hydroxy-N-[(4-propan-2-ylphenyl)methylideneamino]benzamide

InChi Key

IKPPIUNQWSRCOZ-WOJGMQOQSA-N

InChi Code

InChI=1S/C17H18N2O2/c1-12(2)14-5-3-13(4-6-14)11-18-19-17(21)15-7-9-16(20)10-8-15/h3-12,20H,1-2H3,(H,19,21)/b18-11+

SMILES Code

O=C(N/N=C/C1=CC=C(C(C)C)C=C1)C2=CC=C(O)C=C2

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:

GSK-4716 is a selective ERRβ/γ agonist.

In vitro activity:

As shown in Figure 7B, a 6h-period incubation of these cells with GSK4716 increased the expression of NKCC2 by a factor of 2. On the contrary, neither the expression of the Na,K-ATPase α1 subunit (Figure 7C) nor that of the barttin (Figure 7D) is affected by incubation with GSK4716. Reference: PLoS One. 2012;7(3):e34223. https://pubmed.ncbi.nlm.nih.gov/22457827/

In vivo activity:

When administrated in vivo in mice, GSK4716 induced miR-433 expression to a similar extent in both the WT and SHP–/– mice (Figure 6B, left). Reference: Nucleic Acids Res. 2008 Oct;36(18):5727-35. https://pubmed.ncbi.nlm.nih.gov/18776219/

	Solvent	mg/mL	mM
Solubility
	DMF	20.0	70.84
	DMSO	50.1	177.29
	Ethanol	34.7	123.05
	Ethanol:PBS (pH 7.2) (1:6)	0.1	0.50

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 282.34 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. Kim HJ, Yoon HJ, Lee DK, Jin X, Che X, Choi JY. The estrogen-related receptor γ modulator, GSK5182, inhibits osteoclast differentiation and accelerates osteoclast apoptosis. BMB Rep. 2021 May;54(5):266-271. doi: 10.5483/BMBRep.2021.54.5.243. PMID: 33612148; PMCID: PMC8167243. 2. Krid H, Dorison A, Salhi A, Cheval L, Crambert G. Expression profile of nuclear receptors along male mouse nephron segments reveals a link between ERRβ and thick ascending limb function. PLoS One. 2012;7(3):e34223. doi: 10.1371/journal.pone.0034223. Epub 2012 Mar 23. PMID: 22457827; PMCID: PMC3311618. 3. Song G, Wang L. Transcriptional mechanism for the paired miR-433 and miR-127 genes by nuclear receptors SHP and ERRgamma. Nucleic Acids Res. 2008 Oct;36(18):5727-35. doi: 10.1093/nar/gkn567. Epub 2008 Sep 6. PMID: 18776219; PMCID: PMC2566885.

In vitro protocol:

In vivo protocol:

1. Song G, Wang L. Transcriptional mechanism for the paired miR-433 and miR-127 genes by nuclear receptors SHP and ERRgamma. Nucleic Acids Res. 2008 Oct;36(18):5727-35. doi: 10.1093/nar/gkn567. Epub 2008 Sep 6. PMID: 18776219; PMCID: PMC2566885.

1: Wang SC, Myers S, Dooms C, Capon R, Muscat GE. An ERRbeta/gamma agonist modulates GRalpha expression, and glucocorticoid responsive gene expression in skeletal muscle cells. Mol Cell Endocrinol. 2010 Feb 5;315(1-2):146-52. doi: 10.1016/j.mce.2009.07.012. PubMed PMID: 19631715. 2: Kim Y, Koh M, Kim DK, Choi HS, Park SB. Efficient discovery of selective small molecule agonists of estrogen-related receptor gamma using combinatorial approach. J Comb Chem. 2009 Sep-Oct;11(5):928-37. doi: 10.1021/cc900081j. PubMed PMID: 19746993. 3: Di Micco S, Renga B, Carino A, D'Auria MV, Zampella A, Riccio R, Fiorucci S, Bifulco G. Structural insights into Estrogen Related Receptor-β modulation: 4-methylenesterols from Theonella swinhoei sponge as the first example of marine natural antagonists. Steroids. 2014 Feb;80:51-63. doi: 10.1016/j.steroids.2013.11.017. PubMed PMID: 24315836.