| Size | Price | |
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| 500mg | ||
| 1g | ||
| Other Sizes |
Description: Pentamidine dimesylate (MP-601205) is a novel and potent antimicrobial and annticancer agent that interferes with DNA biosynthesis. It exhibits antitumor and antibacterial activities by inhibiting protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL). It can be potentially used for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment.
| ln Vitro |
Cancer cell growth is inhibited in a concentration-dependent manner by pentamidine (0-10 µg/mL; 6 days; WM9, DU145, C4-2, Hey, WM480, and A549 cells) dimesylate administration [1]. It was established that pentamidine isethionate proved cytotoxic to Leishmania infantum promastigotes. After incubation for 72 hours, pentamidine isethionate exhibited 60 times greater leishmanicidal activity than cisplatin. Compared to cisplatin, pentamidine isethionate causes a greater amount of programmed cell death (PCD), which is linked to suppression of DNA synthesis and cell cycle arrest during the G2/M phase. When pentamidine isethionate binds to calf thymus DNA (CT-DNA), the DNA double helix undergoes structural changes that align with the B-to-A transition. Pentamidine isethionate-ubiquitin interaction causes a 6% rise in the protein's β-sheet content [2].
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| ln Vivo |
The growth of WM9 human melanoma in nude mice is greatly inhibited by pentamidine (0.25 mg/mouse; intramuscular injection; every 2 days; for 4 weeks; athymic nude mice) dimesylate therapy [1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: WM9, DU145, C4-2, Hey, WM480 and A549 Cell Tested Concentrations: 0-10 µg/mL Incubation Duration: 6 days Experimental Results: Growth of all six cell lines in culture Inhibited in a concentration-dependent manner, with complete growth inhibition of the cell line at 10 µg/mL. |
| Animal Protocol |
Animal/Disease Models: Athymic nude mice (6 weeks old) injected with WM9 cells [1]
Doses: 0.25mg/mouse Route of Administration: intramuscularinjection; once every 2 days; for 4 consecutive weeks Experimental Results: Dramatically inhibited WM9 human melanoma Growth in nude mice. |
| References | |
| Additional Infomation |
Pentamidine Mesylate is the mesylate salt form of pentamidine, a synthetic derivative of amidine, with antiprotozoal and antifungal activities. Although the precise mode of action of pentamidine is unclear, it appears to interfere with microbial nuclear metabolism by inhibiting DNA, RNA, phospholipid and protein synthesis.
Antiprotozoal agent effective in trypanosomiasis, leishmaniasis, and some fungal infections; used in treatment of PNEUMOCYSTIS pneumonia in HIV-infected patients. It may cause diabetes mellitus, central nervous system damage, and other toxic effects. |
| Molecular Formula |
C19H24N4O2.CH3O3S-
|
|---|---|
| Molecular Weight |
435.51718
|
| Exact Mass |
436.178
|
| CAS # |
6823-79-6
|
| Related CAS # |
Pentamidine isethionate;140-64-7;Pentamidine;100-33-4;Pentamidine dihydrochloride;50357-45-4
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| PubChem CID |
72196
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
5.067
|
| Hydrogen Bond Donor Count |
6
|
| Hydrogen Bond Acceptor Count |
10
|
| Rotatable Bond Count |
10
|
| Heavy Atom Count |
35
|
| Complexity |
468
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
WRXSODAXJSKMAW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H24N4O2.2CH4O3S/c20-18(21)14-4-8-16(9-5-14)24-12-2-1-3-13-25-17-10-6-15(7-11-17)19(22)23;2*1-5(2,3)4/h4-11H,1-3,12-13H2,(H3,20,21)(H3,22,23);2*1H3,(H,2,3,4)
|
| Chemical Name |
4-[5-(4-carbamimidoylphenoxy)pentoxy]benzenecarboximidamide;methanesulfonic acid
|
| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2961 mL | 11.4805 mL | 22.9611 mL | |
| 5 mM | 0.4592 mL | 2.2961 mL | 4.5922 mL | |
| 10 mM | 0.2296 mL | 1.1481 mL | 2.2961 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.
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.
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