Pentamidine
(Synonyms: 喷他脒; MP-601205) 目录号 : GC11468
Pentamidine是一种可干扰多胺合成和RNA聚合酶活性的广谱抗感染剂，对多种寄生虫、原生动物和真菌都具有活性。
Cas No.:100-33-4
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
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.
Pentamidine是一种可干扰多胺合成和RNA聚合酶活性的广谱抗感染剂，对多种寄生虫、原生动物和真菌都具有活性[1,2]。Pentamidine作为一种使用历史悠久的二脒类药物，已被广泛应用于肺孢子虫肺炎、利什曼病和锥虫病等的治疗，也常被用于相关感染性疾病的研究[3]。
在体外，Pentamidine（0-10μM）处理不同的人类恶性肿瘤WM9、DU145、C4-2、Hey、WM480和A549细胞6天，所有六种细胞系的生长均被Pentamidine以浓度依赖性的方式抑制，并在10μM时细胞的生长完全受到抑制[4]。Pentamidine（1, 10, 100μM）处理脂多糖LPS诱导（20ng/mL）的RAW264.7细胞24h，浓度依赖性地抑制了LPS诱导的促炎细胞因子TNF-α和1L-1β在mRNA和蛋白水平的过度产生[5]。用含有Pentamidine（0.05mM）的γ-射线（5Gy）照射HeLa细胞，会影响有丝分裂的进行并导致多核细胞数量的增加[6]。
在体内，Pentamidine（6~10mg/kg (0.25mg/mouse); every 2 days）通过臀部肌肉注射治疗接种了WM9细胞的6周龄裸鼠，在16周的研究期间，可显著抑制WM9细胞的生长，且小鼠未出现明显异常，体重还稳步增长[4]。Pentamidine（10mg/kg; once a day）通过腹腔注射治疗由LPS诱导（25mg/kg; i.p.）的脓毒症C57BL/6小鼠4天，延长了小鼠的存活时间，并减轻了LPS引起的小鼠肝脏、肾脏和肺脏损害及全身炎症[5]。Pentamidine（0.8, 4mg/kg）处理dextran sodium sulphate (DSS)诱导的急性结肠炎CD-1小鼠，小鼠与结肠炎相关的肠道症状得到全面改善，并能保持结肠长度并防止小鼠的脾肿大[7]。
| 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 | |
| 别名 | 喷他脒; MP-601205 | ||
| 化学名 | 4-[5-(4-carbamimidoylphenoxy)pentoxy]benzenecarboximidamide | ||
| Canonical SMILES | C1=CC(=CC=C1C(=N)N)OCCCCCOC2=CC=C(C=C2)C(=N)N | ||
| 分子式 | C19H24N4O2 | 分子量 | 340.42 |
| 溶解度 | ≥ 13.5mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet