Endovion | CAS#265646-85-3 | ANO1 inhibitor

MedKoo Cat#: 532369 | Name: Endovion

Description:

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

Endovion, also known as NS3728 and SCO‐101, is an ANO1 inhibitor.

Chemical Structure

Endovion

CAS#265646-85-3

Theoretical Analysis

MedKoo Cat#: 532369

Name: Endovion

CAS#: 265646-85-3

Chemical Formula: C16H9BrF6N6O

Exact Mass: 493.9925

Molecular Weight: 495.18

Elemental Analysis: C, 38.81; H, 1.83; Br, 16.14; F, 23.02; N, 16.97; O, 3.23

Price and Availability

Size	Price	Availability
50mg	USD 450.00	2 Weeks
100mg	USD 750.00	2 Weeks
200mg	USD 1,250.00	2 Weeks
500mg	USD 2,650.00	2 Weeks
1g	USD 3,850.00	2 Weeks
2g	USD 6,450.00	2 Weeks

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Related CAS #

No Data

Synonym

NS3728; NS 3728; NS-3728; Endovion; SCO‐101; SCO101; SCO 101; Emidurdar

IUPAC/Chemical Name

1-[3,5-bis(trifluoromethyl)phenyl]-3-[4-bromo-2-(1H-1,2,3,4-tetrazol-5-yl)phenyl]urea

InChi Key

AEFYFGMSRKDXHZ-UHFFFAOYSA-N

InChi Code

InChI=1S/C16H9BrF6N6O/c17-9-1-2-12(11(6-9)13-26-28-29-27-13)25-14(30)24-10-4-7(15(18,19)20)3-8(5-10)16(21,22)23/h1-6H,(H2,24,25,30)(H,26,27,28,29)

SMILES Code

O=C(NC1=CC=C(Br)C=C1C2=NN=NN2)NC3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3

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:

Endovion (NS3728) is a pharmacological anion channel inhibitor (like chloride channel) and the specific VRAC/VSOAC blocker.

In vitro activity:

NS3728 was the most potent VRAC blocker in this series ( IC(50) = 0.40 micro M) and even more potent than tamoxifen (2.2 micro M). NS3728 accelerated channel inactivation at positive potentials. These results show that acidic di-aryl ureas constitute a promising starting point for the synthesis of potent inhibitors of VRAC. Reference: J Membr Biol. 2003 Nov 15;196(2):83-94. https://pubmed.ncbi.nlm.nih.gov/14724745/

In vivo activity:

TBD

	Solvent	mg/mL	mM
Solubility
	DMSO	91.5	184.79
	Ethanol	24.8	50.00

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 495.18 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. Poulsen KA, Andersen EC, Hansen CF, Klausen TK, Hougaard C, Lambert IH, Hoffmann EK. Deregulation of apoptotic volume decrease and ionic movements in multidrug-resistant tumor cells: role of chloride channels. Am J Physiol Cell Physiol. 2010 Jan;298(1):C14-25. doi: 10.1152/ajpcell.00654.2008. Epub 2009 Oct 21. PMID: 19846756. 2. Hélix N, Strøbaek D, Dahl BH, Christophersen P. Inhibition of the endogenous volume-regulated anion channel (VRAC) in HEK293 cells by acidic di-aryl-ureas. J Membr Biol. 2003 Nov 15;196(2):83-94. doi: 10.1007/s00232-003-0627-x. PMID: 14724745.

In vitro protocol:

In vivo protocol:

TBD

1: Godwin TD, Kelly ST, Brew TP, Bougen-Zhukov NM, Single AB, Chen A, Stylianou CE, Harris LD, Currie SK, Telford BJ, Beetham HG, Evans GB, Black MA, Guilford PJ. E-cadherin-deficient cells have synthetic lethal vulnerabilities in plasma membrane organisation, dynamics and function. Gastric Cancer. 2019 Mar;22(2):273-286. doi: 10.1007/s10120-018-0859-1. Epub 2018 Jul 31. PMID: 30066183; PMCID: PMC6394693. 2: Sørensen BH, Nielsen D, Thorsteinsdottir UA, Hoffmann EK, Lambert IH. Downregulation of LRRC8A protects human ovarian and alveolar carcinoma cells against Cisplatin-induced expression of p53, MDM2, p21Waf1/Cip1, and Caspase-9/-3 activation. Am J Physiol Cell Physiol. 2016 Jun 1;310(11):C857-73. doi: 10.1152/ajpcell.00256.2015. Epub 2016 Mar 16. PMID: 26984736; PMCID: PMC4935196. 3: Sauter DRP, Novak I, Pedersen SF, Larsen EH, Hoffmann EK. ANO1 (TMEM16A) in pancreatic ductal adenocarcinoma (PDAC). Pflugers Arch. 2015 Jul;467(7):1495-1508. doi: 10.1007/s00424-014-1598-8. Epub 2014 Aug 28. PMID: 25163766; PMCID: PMC4464647. 4: Poulsen KA, Andersen EC, Hansen CF, Klausen TK, Hougaard C, Lambert IH, Hoffmann EK. Deregulation of apoptotic volume decrease and ionic movements in multidrug-resistant tumor cells: role of chloride channels. Am J Physiol Cell Physiol. 2010 Jan;298(1):C14-25. doi: 10.1152/ajpcell.00654.2008. Epub 2009 Oct 21. PMID: 19846756. 5: Kjaer K, Strøbaek D, Christophersen P, Rønn LC. Chloride channel blockers inhibit iNOS expression and NO production in IFNgamma-stimulated microglial BV2 cells. Brain Res. 2009 Jul 24;1281:15-24. doi: 10.1016/j.brainres.2009.05.015. Epub 2009 May 13. Erratum in: Brain Res. 2009 Sep 29;1291:153. PMID: 19446535. 6: Schneider L, Klausen TK, Stock C, Mally S, Christensen ST, Pedersen SF, Hoffmann EK, Schwab A. H-ras transformation sensitizes volume-activated anion channels and increases migratory activity of NIH3T3 fibroblasts. Pflugers Arch. 2008 Mar;455(6):1055-62. doi: 10.1007/s00424-007-0367-3. Epub 2007 Oct 20. PMID: 17952454. 7: Klausen TK, Bergdahl A, Hougaard C, Christophersen P, Pedersen SF, Hoffmann EK. Cell cycle-dependent activity of the volume- and Ca2+-activated anion currents in Ehrlich lettre ascites cells. J Cell Physiol. 2007 Mar;210(3):831-42. doi: 10.1002/jcp.20918. PMID: 17111356. 8: Hélix N, Strøbaek D, Dahl BH, Christophersen P. Inhibition of the endogenous volume-regulated anion channel (VRAC) in HEK293 cells by acidic di-aryl-ureas. J Membr Biol. 2003 Nov 15;196(2):83-94. doi: 10.1007/s00232-003-0627-x. PMID: 14724745.