Pentamidine (Synonyms: NSC 9921) |
Catalog No.GC11468
One-Click Copy Product Info
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Pentamidine is a broad-spectrum anti-infective agent that interferes with polyamine synthesis and RNA polymerase activity, demonstrating efficacy against a variety of parasites, protozoa, and fungi.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 100-33-4
Sample solution is provided at 25 µL, 10mM.
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Pentamidine is a broad-spectrum anti-infective agent that interferes with polyamine synthesis and RNA polymerase activity, demonstrating efficacy against a variety of parasites, protozoa, and fungi[1,2]. As a well-established diamidine drug with a long history of clinical use, Pentamidine is widely employed for the treatment of Pneumocystis pneumonia, leishmaniasis, and trypanosomiasis, and is also commonly used in research related to infectious diseases[3].
In vitro, treatment of various human malignant cell lines (WM9, DU145, C4-2, Hey, WM480, and A549) with Pentamidine (0-10μM) for 6 days resulted in concentration-dependent inhibition of cell growth across all six lines, with complete suppression observed at 10μM[4]. In LPS-induced (20ng/mL) RAW264.7 cells, 24h treatment with Pentamidine (1, 10, 100μM) concentration-dependently suppressed the overexpression of pro-inflammatory cytokines TNF-α and IL-1β at both mRNA and protein levels[5]. Exposure of HeLa cells to γ-irradiation (5Gy) in the presence of Pentamidine (0.05mM) disrupted mitotic progression and led to an increase in multinucleated cells[6].
In vivo, intramuscular administration of Pentamidine (6-10mg/kg (0.25mg/mouse); every 2 days) in 6-week-old nude mice inoculated with WM9 cells significantly inhibited tumor growth throughout the 16-week study period. No significant abnormalities were observed, and the mice exhibited steady weight gain[4]. In a LPS-induced (25mg/kg; i.p.) septic C57BL/6 mouse model, intraperitoneal injection of Pentamidine (10mg/kg; once a day) for 4 days prolonged survival, attenuated systemic inflammation, and ameliorated LPS-induced damage in the liver, kidney, and lungs[5]. Treatment with Pentamidine (0.8, 4mg/kg) in dextran sodium sulphate (DSS)-induced acute colitis CD-1 mice resulted in comprehensive improvement of colitis-related intestinal symptoms, preserved colon length, and prevented splenomegaly[7].
References:
[1] HAFIZ S, KYRIAKOPOULOS C. Pentamidine[M]//StatPearls. Treasure Island (FL): StatPearls Publishing, 2025.
[2] SANDS M, KRON M A, BROWN R B. Pentamidine: a review[J]. Reviews of infectious diseases, 1985, 7(5): 625-6344.
[3] BRAY P G, BARRETT M P, WARD S A, et al. Pentamidine uptake and resistance in pathogenic protozoa: past, present and future[J]. Trends in parasitology, 2003, 19(5): 232-239.
[4] PATHAK M K, DHAWAN D, LINDNER D J, et al. Pentamidine is an inhibitor of PRL phosphatases with anticancer activity[J]. Molecular cancer therapeutics, 2002, 1(14): 1255-1264.
[5] WU S, LIN C, ZHANG T, et al. Pentamidine alleviates inflammation and lipopolysaccharide-induced sepsis by inhibiting TLR4 activation via targeting MD2[J]. Frontiers in pharmacology, 2022, 13: 835081.
[6] KOBAYASHI J, KATO A, OTA Y, et al. Bisbenzamidine derivative, pentamidine represses DNA damage response through inhibition of histone H2A acetylation[J]. Molecular cancer, 2010, 9(1): 34.
[7] ESPOSITO G, CAPOCCIA E, SARNELLI G, et al. The antiprotozoal drug pentamidine ameliorates experimentally induced acute colitis in mice[J]. Journal of neuroinflammation, 2012, 9(1): 277.
| Cell experiment [1]: | |
Cell lines | Macrophage RAW264.7 cells |
Preparation Method | RAW264.7 cells were treated with 20ng/mL LPS and indicated concentrations of pentamidine (1, 10, 100μM) for 24h. Total RNA was extracted and qRT-PCR was performed to measure the expression of TNF-α and IL-1β mRNAs. The TNF-α and IL-1β proteins in the supernatant were measured by ELISA. |
Reaction Conditions | 1, 10, 100μM; 24h |
Applications | Pentamidine (1, 10, 100μM) inhibits LPS-induced pro-inflammatory factors TNF-α and IL-1β at mRNAs and protein level overproduction. |
| Animal experiment [2]: | |
Animal models | 6-week-old athymic nude mice with WM9 cells (4×106 cells/site; two sites/mice; s.c.) |
Preparation Method | Athymic nude mice 6 weeks of age were inoculated (s.c.) in the flanks with WM9 cells (4×106 cells/site, two sites/mice) on day 0. Starting on day 2, the mice were subjected to treatment with pentamidine (6-10mg/kg (0.25mg/mouse); every 2 days; i.m.) injected at the hip area. Tumor volume was calculated and mouse viability and body weights were recorded weekly. |
Dosage form | 6-10mg/kg (0.25mg/mouse); every 2 days; i.m. |
Applications | Following 16 weeks of treatment, Pentamidine (0.25mg/mouse; every two days) exhibited significant inhibition of WM9 tumor growth. The treatment was well-tolerated, as evidenced by the absence of overt abnormalities and steady body weight gain throughout the study period. |
References: | |
| Cas No. | 100-33-4 | SDF | |
| Synonyms | NSC 9921 | ||
| Chemical Name | 4-[5-(4-carbamimidoylphenoxy)pentoxy]benzenecarboximidamide | ||
| Canonical SMILES | C1=CC(=CC=C1C(=N)N)OCCCCCOC2=CC=C(C=C2)C(=N)N | ||
| Formula | C19H24N4O2 | M.Wt | 340.42 |
| Solubility | ≥ 13.5mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9375 mL | 14.6877 mL | 29.3755 mL |
| 5 mM | 587.5 μL | 2.9375 mL | 5.8751 mL |
| 10 mM | 293.8 μL | 1.4688 mL | 2.9375 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)