Alexidine Dihydrochloride

Alias: Alexidine Dihydrochloride; Alexidine 2HCl;
Cat No.:V10758 Purity: ≥98%
Alexidine dihydrochloride is an anticancer agent that targets a mitochondrial tyrosine phosphatase.
Alexidine Dihydrochloride Chemical Structure CAS No.: 1715-30-6
Product category: Fungal
This product is for research use only, not for human use. We do not sell to patients.
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Other Forms of Alexidine Dihydrochloride:

  • Alexidine
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
Alexidine dihydrochloride is an anticancer agent that targets a mitochondrial tyrosine phosphatase, PTPMT1, in mammalian cells and causes mitochondrial apoptosis.A wide variety of fungal pathogens are susceptible to the antifungal and antibiofilm properties of alexidine dihydrochloride.
Biological Activity I Assay Protocols (From Reference)
Targets
PTPMT1
ln Vitro
With the exception of Candida parapsilosis and Candida krusei, all isolates tested under planktonic conditions showed MIC values of ≤1.5 μg/mL. Alexidine dihydrochloride exhibits activity against most Candida spp. Fascinatingly, clinically significant fluconazole-resistant Candida isolates such as C. albicans (CA2, CA6, and CA10), C. glabrata (CG2 and CG5), C. parapsilosis (CP5), and C. auris (CAU-09 and CAU-03) are all significantly active against alexidine dihydrochloride[1].
When Alexidine dihydrochloride is used to inhibit planktonic growth, it completely stops the fungi being imaged from filamentating or proliferating. Alexidine dihydrochloride is able to decimate at low concentrations (1.5 to 6 μg/mL) mature biofilms of Candida, Cryptococcus, and Aspergillus spp. that are known to be resistant to almost all classes of antifungal drugs. In reality, alexidine dihydrochloride could prevent lateral yeast formation and biofilm dispersal in Candida albicans at concentrations of planktonic MICs that are 10-fold lower—150 ng/mL—than those of Candida albicans[1].
HUVECs and lung epithelial cells are 50% killed by alexidine dihydrochloride at concentrations five to ten times higher than the minimum inhibitory concentration needed to kill planktonically growing fungal pathogens[1].
ln Vivo
decided to concentrate on C. albicans biofilm formation because this fungus has a well-established murine biofilm model that is used to evaluate the efficacy of both new and old antifungal medications. When the drugs are seen under a microscope, the impact they have on the 24-hour-old biofilms that are developing in the mice's jugular vein catheters is evident. The biofilm density in the catheters treated with Alexidine dihydrochloride is considerably lower. In fact, compared to the untreated control biofilms, alexidine dihydrochloride inhibits 67% of the growth and viability of fungal biofilms, according to fungal CFU determination[1].
References

[1]. Alexidine Dihydrochloride Has Broad-Spectrum Activities against Diverse Fungal Pathogens. mSphere. 2018 Oct 31;3(5). pii: e00539-18.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C26H58CL2N10
Molecular Weight
581.71172
Exact Mass
580.42
Elemental Analysis
C, 53.68; H, 10.05; Cl, 12.19; N, 24.08
CAS #
1715-30-6
Related CAS #
Alexidine;22573-93-9
Appearance
Solid powder
SMILES
CCCCC(CC)CNC(=N)NC(=N)NCCCCCCNC(=N)NC(=N)NCC(CC)CCCC.Cl.Cl
InChi Key
BRJJFBHTDVWTCJ-UHFFFAOYSA-N
InChi Code
InChI=1S/C26H56N10.2ClH/c1-5-9-15-21(7-3)19-33-25(29)35-23(27)31-17-13-11-12-14-18-32-24(28)36-26(30)34-20-22(8-4)16-10-6-2;;/h21-22H,5-20H2,1-4H3,(H5,27,29,31,33,35)(H5,28,30,32,34,36);2*1H
Chemical Name
1-[N'-[6-[[amino-[[N'-(2-ethylhexyl)carbamimidoyl]amino]methylidene]amino]hexyl]carbamimidoyl]-2-(2-ethylhexyl)guanidine;dihydrochloride
Synonyms
Alexidine Dihydrochloride; Alexidine 2HCl;
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO :~125 mg/mL (~214.88 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.58 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.08 mg/mL (3.58 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.08 mg/mL (3.58 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.08 mg/mL (3.58 mM)

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.7191 mL 8.5953 mL 17.1907 mL
5 mM 0.3438 mL 1.7191 mL 3.4381 mL
10 mM 0.1719 mL 0.8595 mL 1.7191 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • Inhibition of biofilm growth, C. albicans biofilm dispersal, and abrogation of planktonic growth in diverse fungi by alexidine dihydrochloride (AXD).[1]. Alexidine Dihydrochloride Has Broad-Spectrum Activities against Diverse Fungal Pathogens. mSphere. 2018 Oct 31;3(5). pii: e00539-18.
  • Toxicity of AXD on host cells and on biofilm killing in combination with fluconazole. [1]. Alexidine Dihydrochloride Has Broad-Spectrum Activities against Diverse Fungal Pathogens. mSphere. 2018 Oct 31;3(5). pii: e00539-18.
  • Impact of AXD, fluconazole (FLC), and caspofungin (CAS) as lock therapy against C. albicans biofilm cells in an in vivo catheter model. [1]. Alexidine Dihydrochloride Has Broad-Spectrum Activities against Diverse Fungal Pathogens. mSphere. 2018 Oct 31;3(5). pii: e00539-18.
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