Pentamidine isethionate

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Chemical Structure| 140-64-7 同义名 : 喷他脒羟乙磺酸盐 ;MP-601205 isethionate
CAS号 : 140-64-7
货号 : A668797
分子式 : C23H36N4O10S2
纯度 : 99%+
分子量 : 592.683
MDL号 : MFCD00079213
存储条件:

Pure form Inert atmosphere,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(177.16 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 100 mg/mL(168.72 mM),配合低频超声助溶

动物实验配方:
生物活性
描述 Pentamidine isethionate, an aromatic diamidine, is an antiprotozoal agent proven to decrease mortality from Pneumocystis carinii pneumonia in debilitated infants and immunodeficient adults and children[3]. The use of intramuscular pentamidine isethionate in the treatment of Leishmania guyanensis cutaneous leishmaniasis is associated with more treatment failures than intravenous pentamidine isethionate[4]. PI (Pentamidine Isethionate) is a safe drug and its efficacy varied with the number of doses. The administration of PI in patients with ACL (American Cutaneous Leishmaniasis), predominantly caused by L. guyanensis, was mostly efficient in three or two doses of 7 mg/kg[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00141037 Kidney Diseases ... 展开 >> Kidney Transplantation Kidney Transplant Renal Transplantation Renal Transplant 收起 << Phase 1 Phase 2 Completed - United States, Alabama ... 展开 >> University of Alabama - Pediatric Nephrology Birmingham, Alabama, United States, 35233 United States, California Maxine Dunitz Children's Health Center Cedars-Sinai Los Angeles, California, United States, 90048 UCLA - Department of Pediatrics, Division of Nephrology Los Angeles, California, United States, 90095-1752 Stanford University Medical Center, Lucile Packard Children's Hospital Palo Alto, California, United States, 94304 UCSF Children's Hospital San Francisco, California, United States, 94143 United States, Florida University of Florida - Pediatric Nephrology Gainesville, Florida, United States, 32610-0296 United States, Louisiana Children's Hospital of New Orleans-Department of Pediatric Nephrology New Orleans, Louisiana, United States, 70118 United States, Massachusetts Children's Hospital Boston - Division of Nephrology Boston, Massachusetts, United States, 02115 United States, Michigan University of Michigan Medical Center, C.S. Mott Children's Hospital- Division of Nephrology & Transplantation Ann Arbor, Michigan, United States, 48109 United States, Missouri Children's Mercy Hospital - Department of Nephrology Kansas City, Missouri, United States, 64108 United States, Pennsylvania The Children's Hospital of Philadelphia-Department of Nephrology Philadelphia, Pennsylvania, United States, 19104 United States, Washington Children's Hospital & Regional Medical Center - Division of Nephrology Seattle, Washington, United States, 98105 收起 <<
NCT00014911 Diabetes Mellitus, Insulin-Dep... 展开 >>endent 收起 << Phase 2 Completed - United States, Florida ... 展开 >> University of Miami Miami, Florida, United States, 33136 United States, Massachusetts Massachusetts General Hospital Boston, Massachusetts, United States, 02114 United States, Minnesota University of Minnesota Minneapolis, Minnesota, United States, 55455 United States, Missouri Washington University St. Louis, Missouri, United States, 63110 United States, Washington Benaroya Research Institute at Virginia Mason Research Center Seattle, Washington, United States, 98101 Canada, Alberta University of Alberta Edmonton, Alberta, Canada Germany Justus-Leibig University Giessen, Germany, 35385 Italy University of Milan Milan, Italy Switzerland University of Geneva Geneva, Switzerland 收起 <<
NCT00141037 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.69mL

0.34mL

0.17mL

8.44mL

1.69mL

0.84mL

16.87mL

3.37mL

1.69mL

参考文献

[1]Nguewa PA, Fuertes MA, et al. Pentamidine is an antiparasitic and apoptotic drug that selectively modifies ubiquitin. Chem Biodivers. 2005 Oct;2(10):1387-400.

[2]Sands M, Kron MA, et al. Pentamidine: a review. Rev Infect Dis. 1985 Sep-Oct;7(5):625-34.

[3]Goa KL, Campoli-Richards DM. Pentamidine isethionate. A review of its antiprotozoal activity, pharmacokinetic properties and therapeutic use in Pneumocystis carinii pneumonia. Drugs. 1987;33(3):242–258

[4]Christen JR, Bourreau E, Demar M, et al. Use of the intramuscular route to administer pentamidine isethionate in Leishmania guyanensis cutaneous leishmaniasis increases the risk of treatment failure. Travel Med Infect Dis. 2018;24:31–36

[5]Gadelha EPN, Ramasawmy R, da Costa Oliveira B, et al. An open label randomized clinical trial comparing the safety and effectiveness of one, two or three weekly pentamidine isethionate doses (seven milligrams per kilogram) in the treatment of cutaneous leishmaniasis in the Amazon Region. PLoS Negl Trop Dis. 2018;12(10):e0006850. Published 2018 Oct 31