AMXT-1501 tetrahydrochloride

Name: AMXT-1501 tetrahydrochloride
Brand: MedChemExpress
SKU: HY-124617A
Rating: 5.0 (10 reviews)

Cat. No.: HY-124617A Purity: 98.0%: Data Sheet
COA

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Handling Instructions
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AMXT-1501 tetrahydrochloride is a Bacterial agent and polyamine transport system inhibitor. AMXT-1501 tetrahydrochloride targets membrane phospholipids and exhibits antibacterial activity against a variety of Gram-positive and Gram-negative multidrug-resistant bacteria. AMXT-1501 tetrahydrochloride inhibits capsular biosynthesis in Streptococcus pneumoniae. AMXT-1501 tetrahydrochloride targets ornithine decarboxylase and polyamines to inhibit the proliferation of neuroblastoma cells. AMXT-1501 tetrahydrochloride in combination with DFMO (HY-B0744) induces Apoptosis in neuroblastoma cells. AMXT-1501 tetrahydrochloride is applicable to research related to multidrug-resistant bacterial infections, pneumococcal infections, Streptococcus pneumoniae infections, and neuroblastoma.

For research use only. We do not sell to patients.

CAS No. : 2444815-84-1

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in Water	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	Get quote
200 mg	Get quote

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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of AMXT-1501 tetrahydrochloride:

AMXT-1501 In-stock

10 Publications Citing Use of MCE AMXT-1501 tetrahydrochloride

Cell Proliferation/Viability Assay

Cell Imaging/Staining

2D/3D Cell Culture and Differentiation

: AMXT-1501 tetrahydrochloride purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2024 Jul;31(7):910-923. [Abstract]; IC50s of AMXT-1501 (4, 8, 12, 16, 20, 24 μM) in CLB-BAR, CLB-GE, SK-N-BE(2) and SH-SY5Y cells after 5 d treatment.

: AMXT-1501 tetrahydrochloride purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2024 Jul;31(7):910-923. [Abstract]; Immunoblot analysis of neuronal differentiation markers (RET and DLG2) in SK-N-BE(2) and SH-SY5Y cells treated with AMXT-1501 (0 or 8 µM) and RA (0 or 5 µM) for 48 h or 24 h .

: AMXT-1501 tetrahydrochloride purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2024 Jul;31(7):910-923. [Abstract]; Cells after AMXT-1501 (0 or 8 µM) and RA (0 or 5 µM) treatment as indicated for 48 h or 24 h.

: AMXT-1501 tetrahydrochloride purchased from MedChemExpress. Usage Cited in: bioRxiv. 2024 Nov 17:2024.08.24.609500.; Representative fluorescence images of cells upon indicated treatments. AMXT-1501 (0.5 μM; polyamine import inhibitor), DFMO (1 mM), and spermidine (5 μM).

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Polyamine transport^[1]

In Vitro

AMXT-1501 (1.56-50 μM) tetrahydrochloride exhibits dose-dependent antibacterial activity against a variety of Gram-positive and Gram-negative multidrug-resistant (MDR) bacterial isolates, with MIC₅₀/MIC₉₀ values ranging from 3.13 to 12.5 μM^[1].
AMXT-1501 (8× MIC; 0-24 h) tetrahydrochloride exhibits rapid and potent bactericidal activity against planktonic MRSA, ESBL-producing E. coli, and CR E. coli^[1].
AMXT-1501 (1-4× MIC; 0.5-24 h) tetrahydrochloride reduces biofilm formation in a dose-dependent manner in most tested Staphylococcus aureus (MSSA and MRSA) and Enterococcus faecalis strains, causes severe damage to the cell membranes of MRSA and CR E. coli, increases membrane permeability and depolarizes them, thereby leading to bacterial cell death^[1].
AMXT-1501 (3.125-50 μg/mL; 90 s) tetrahydrochloride binds directly to the bacterial membrane phospholipids CL and PG^[1].
AMXT-1501 (7.4 μM; cultured until OD₆₀₀ reaches 0.2-0.5) tetrahydrochloride inhibits capsular polysaccharide biosynthesis by 61% in Streptococcus pneumoniae serotype 2 (strain D39), depletes intracellular polyamines and glucuronic acid, and simultaneously increases intracellular glucose levels^[2].
AMXT-1501 (7.4 μM) tetrahydrochloride regulates gene expression in Streptococcus pneumoniae D39, thereby enhancing the biosynthesis of polyamines and glucose, inhibiting ATP production and fatty acid synthesis, and upregulating stress response pathways^[3].
AMXT-1501 (0.39-50 μM; 48 h) tetrahydrochloride potently inhibits the viability of human neuroblastoma cell lines BE (2)-C, SMS-KCNR and SH-SY5Y in vitro, with IC₅₀ values of 17.69 μM, 17.72 μM and 14.13 μM, respectively^[4].
AMXT-1501 (2.5 μM; 96 h) tetrahydrochloride induced apoptosis in BE (2)-C, SMS-KCNR and SH-SY5Y human neuroblastoma cells when used in combination with DFMO^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay^[4]

Cell Line:	BE(2)-C, SMS-KCNR, SH-SY5Y
Concentration:	0.39 µM, 1 µM, 3.1 µM, 10 µM, 31 µM, 50 µM
Incubation Time:	48 h
Result:	AMXT-1501 tetrahydrochloride exhibited cytotoxicity against this panel of NB cell lines.

Apoptosis Analysis^[4]

Cell Line:	BE(2)‐C, SMS‐KCNR and SH‐SY5Y cells
Concentration:	2.5 μM+2.5 mM DFMO
Incubation Time:	96 h
Result:	Induced apoptosis. Reduced the amount of uncleaved PARP and increased the amounts of cleaved PARP and cleaved caspase-3.

In Vivo

AMXT-1501 (20 mg/kg; i.p.; every 12 h; 3 days) tetrahydrochloride significantly reduces the size of skin abscesses and decreases MRSA loads in BALB/c mice^[1].
AMXT-1501 (20 mg/kg; i.p.; every 12 h; 3 days) tetrahydrochloride significantly improves the survival rate of BALB/c mice with bacterial abdominal infection and reduces the bacterial load of CRE E. coli in their lung and liver tissues^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	BALB/c (female, 6-8-week-old, 18-22 g) (S. aureus YUSA145 (MRSA)(1×107 CFU))^[1]
Dosage:	20 mg/kg
Administration:	i.p.; every 12 h; 3 days
Result:	Reduced skin abscess areas significantly. Lowered bacterial loads in abscess tissue (log₁₀ CFU/g) significantly.

Animal Model:	BALB/c (female, 6-8-week-old, 18-22 g) (S. aureus YUSA145 (MRSA)(1×107 CFU))^[1]
Dosage:	20 mg/kg
Administration:	i.p.; every 12 h; 3 days
Result:	Achieved a 50% survival rate through day 7, which was higher than the survival rate in tigecycline-treated mice. Lowered bacterial loads in lung tissue (log₁₀ CFU/g) significantly. Lowered bacterial loads in liver tissue (log₁₀ CFU/g) significantly.

Molecular Weight

714.77

Formula

C₃₂H₇₂Cl₄N₆O₂

CAS No.

2444815-84-1

Appearance

Solid

Color

Off-white to light yellow

SMILES

CCCCCCCCCCCCCCCC(NCCCC[C@@H](N)C(NCCCNCCCCNCCCN)=O)=O.Cl.Cl.Cl.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility

In Vitro:

H₂O : 83.33 mg/mL (116.58 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.3991 mL	6.9953 mL	13.9905 mL
5 mM	0.2798 mL	1.3991 mL	2.7981 mL
10 mM	0.1399 mL	0.6995 mL	1.3991 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 50 mg/mL (69.95 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 98.0%

Select Batch:

Data Sheet (275 KB) SDS (252 KB)

COA (239 KB) HNMR (283 KB)

Handling Instructions (2659 KB)

References

[1]. Zheng J, et al. AMXT-1501 tetrahydrochloride targets membrane phospholipids against Gram-positive and -negative multidrug-resistant bacteria. Emerg Microbes Infect. 2024;13(1):2321981. [Content Brief]

[2]. Ayoola MB, et al. Difluoromethylornithine (DFMO) and AMXT 1501 inhibit capsule biosynthesis in pneumococci. Sci Rep. 2022;12(1):11804. Published 2022 Jul 12. [Content Brief]

[3]. Ayoola MB, Shack LA, Phanstiel O 4th, Nanduri B. Impact of Difluoromethylornithine and AMXT 1501 on Gene Expression and Capsule Regulation in Streptococcus pneumoniae. Biomolecules. 2024 Feb 2;14(2):178. [Content Brief]

[4]. Samal K, Zhao P, Kendzicky A, Yco LP, McClung H, Gerner E, Burns M, Bachmann AS, Sholler G. AMXT-1501 tetrahydrochloride, a novel polyamine transport inhibitor, synergizes with DFMO in inhibiting neuroblastoma cell proliferation by targeting both ornithine decarboxylase and polyamine transport. Int J Cancer. 2013 Sep 15;133(6):1323-33. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O	1 mM	1.3991 mL	6.9953 mL	13.9905 mL	34.9763 mL
	5 mM	0.2798 mL	1.3991 mL	2.7981 mL	6.9953 mL
	10 mM	0.1399 mL	0.6995 mL	1.3991 mL	3.4976 mL
	15 mM	0.0933 mL	0.4664 mL	0.9327 mL	2.3318 mL
	20 mM	0.0700 mL	0.3498 mL	0.6995 mL	1.7488 mL
	25 mM	0.0560 mL	0.2798 mL	0.5596 mL	1.3991 mL
	30 mM	0.0466 mL	0.2332 mL	0.4664 mL	1.1659 mL
	40 mM	0.0350 mL	0.1749 mL	0.3498 mL	0.8744 mL
	50 mM	0.0280 mL	0.1399 mL	0.2798 mL	0.6995 mL
	60 mM	0.0233 mL	0.1166 mL	0.2332 mL	0.5829 mL
	80 mM	0.0175 mL	0.0874 mL	0.1749 mL	0.4372 mL
	100 mM	0.0140 mL	0.0700 mL	0.1399 mL	0.3498 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.