Niclosamide-olamine | CAS#1420-04-8

MedKoo Cat#: 533885 | Name: Niclosamide-olamine

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Description:

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

Niclosamide-olamine is a Insect Attractant, Repellent and Chemosterilant.

Chemical Structure

Niclosamide-olamine

CAS#1420-04-8 (olamine)

Theoretical Analysis

MedKoo Cat#: 533885

Name: Niclosamide-olamine

CAS#: 1420-04-8 (olamine)

Chemical Formula: C15H15Cl2N3O5

Exact Mass: 387.0389

Molecular Weight: 388.20

Elemental Analysis: C, 46.41; H, 3.89; Cl, 18.26; N, 10.82; O, 20.61

Price and Availability

Size	Price	Availability
500mg	USD 250.00	2 Weeks
1g	USD 450.00	2 Weeks
2g	USD 750.00	2 Weeks
5g	USD 1,250.00	2 Weeks

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Related CAS #

50-65-7 (free base) 73360-56-2 (hydrate) 36466-48-5 (piperazine) 40321-86-6 (sodium) 1420-04-8 (olamine)

Synonym

Niclosamide-olamine, Niclosamide (ethanolamine salt)

IUPAC/Chemical Name

5-Chloro-N-(2-chloro-4-nitrophenyl)-2-hydroxybenzamide compd. with 2-aminoethanol (1:1)

InChi Key

XYCDHXSQODHSLG-UHFFFAOYSA-N

InChi Code

InChI=1S/C13H8Cl2N2O4.C2H7NO/c14-7-1-4-12(18)9(5-7)13(19)16-11-3-2-8(17(20)21)6-10(11)15;3-1-2-4/h1-6,18H,(H,16,19);4H,1-3H2

SMILES Code

O=C(NC1=CC=C([N+]([O-])=O)C=C1Cl)C2=CC(Cl)=CC=C2O.NCCO

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

>3 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:

Niclosamide (BAY2353) olamine is an orally active antihelminthic agent used in parasitic infection research. Niclosamide olamin is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells.

In vitro activity:

To further explore the potential mechanism of enhancement of PD-L1 antibody by niclosamide, it was evaluated whether niclosamide could have an impact on PD-L1 expression. The maximum niclosamide concentration tested (2 μM) was added to these NSCLC cell lines, which was lower than the IC30. Applying flow cytometry analysis, downregulation of PD-L1 expression after niclosamide treatment for 24 h (Fig. 3a) was observed. The inhibitory effect of niclosamide on PD-L1 expression was futher evaluated. After treatment with differing concentrations of niclosamide, it was observed that niclosamide decreased PD-L1 expression as well as STAT3 phosphorylation in a concentration-dependent manner in NSCLC cell lines (Fig.3b-d,3b-d, h-i). Moreover, cells treated with 2 μM niclosamide at different time points showed a time-dependent suppression of PD-L1 and p-STAT3 levels (Fig.3e-g,3e-g, k-m). Reference: J Immunother Cancer. 2019; 7: 245. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6739982/

In vivo activity:

As early embryonic development in zebrafish is dependent, in part, on uptake of maternally deposited nutrients in the yolk as well as metabolism of cellular lipid droplets, the metabolomic profiles of zebrafish embryos following niclosamide exposure were investigated. The abundance and distribution of non-polar metabolites and lipids were not significantly affected within embryos exposed to 0.313 μM niclosamide from 2–5 hpf (Figures 2A and 2B; Supplementary Data S1). However, niclosamide exposure resulted in significant alterations on polar metabolites, where the majority of significantly affected metabolites were amino acids involved in the aminoacyl-tRNA biosynthesis pathway (Figures 3A and 3B; Figure 4; Supplementary Data S1). These results suggest that, within embryos exposed from 2–5 hpf, niclosamide affected the abundance and distribution of amino acids in the absence of effects of non-polar metabolites and lipids. Reference: Toxicol Appl Pharmacol. 2019 Oct 1; 380: 114699. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6717554/

	Solvent	mg/mL	mM
Solubility
	DMF	30.0	77.28
	DMSO	30.0	77.28
	DMSO:PBS (pH 7.2) (1:1)	0.5	1.29
	Ethanol	0.3	0.64

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 388.20 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. Luo F, Luo M, Rong QX, Zhang H, Chen Z, Wang F, Zhao HY, Fu LW. Niclosamide, an antihelmintic drug, enhances efficacy of PD-1/PD-L1 immune checkpoint blockade in non-small cell lung cancer. J Immunother Cancer. 2019 Sep 11;7(1):245. doi: 10.1186/s40425-019-0733-7. PMID: 31511071; PMCID: PMC6739982. 2. Park SY, Kim JY, Choi JH, Kim JH, Lee CJ, Singh P, Sarkar S, Baek JH, Nam JS. Inhibition of LEF1-Mediated DCLK1 by Niclosamide Attenuates Colorectal Cancer Stemness. Clin Cancer Res. 2019 Feb 15;25(4):1415-1429. doi: 10.1158/1078-0432.CCR-18-1232. Epub 2018 Nov 16. PMID: 30446587. 3. Luo F, Luo M, Rong QX, Zhang H, Chen Z, Wang F, Zhao HY, Fu LW. Niclosamide, an antihelmintic drug, enhances efficacy of PD-1/PD-L1 immune checkpoint blockade in non-small cell lung cancer. J Immunother Cancer. 2019 Sep 11;7(1):245. doi: 10.1186/s40425-019-0733-7. PMID: 31511071; PMCID: PMC6739982. 4. Vliet SMF, Dasgupta S, Sparks NRL, Kirkwood JS, Vollaro A, Hur M, Zur Nieden NI, Volz DC. Maternal-to-zygotic transition as a potential target for niclosamide during early embryogenesis. Toxicol Appl Pharmacol. 2019 Oct 1;380:114699. doi: 10.1016/j.taap.2019.114699. Epub 2019 Aug 6. PMID: 31398420; PMCID: PMC6717554.

In vitro protocol:

In vivo protocol: