Basic information Safety Supplier Related

PentaMidine-d4 2HCl

Basic information Safety Supplier Related

PentaMidine-d4 2HCl Basic information

Product Name:
PentaMidine-d4 2HCl
Synonyms:
  • PentaMidine-d4 2HCl
  • PentaMidine (dihydrochloride)
  • 4,4'-[1,5-Pentanediylbis(oxy)]bisbenzenecarboximidamide] dihydrochloride
  • Benzenecarboximidamide, 4,4'-[1,5-pentanediylbis(oxy)]bis-, dihydrochloride (9CI)
  • MP601205 dihydrochloride
  • MP601205 DIHYDROCHLORIDE;PENTAMIDINE
  • PTP1B,Pneumocystis,Parasite,Antibiotic,antitumor,Pentamidine,MP 601205,Inhibitor,Kidney,MP-601205,carinii,Bacterial,cell-cycle,pneumonia,MP601205,Phosphatase,inhibit,DNA,Pentamidine dihydrochloride,biosynthetics,Fungal,arrest
  • Pentamidine dihydrochloride, 10 mM in DMSO
CAS:
50357-45-4
MF:
C19H26Cl2N4O2
MW:
413.34134
Product Categories:
  • Inhibitors
Mol File:
50357-45-4.mol
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PentaMidine-d4 2HCl Chemical Properties

Melting point:
232-234°
storage temp. 
Store at -20°C
solubility 
Soluble in DMSO > 10 mM
form 
Powder
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Safety Information

Toxicity
LD50 in mice (mg/g): 0.028 i.v.; 0.064 s.c. (Wein)
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PentaMidine-d4 2HCl Usage And Synthesis

Uses

Pentamidine dihydrochloride (MP-601205 dihydrochloride) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine dihydrochloride inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine dihydrochloride is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine dihydrochloride has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities[1][2][3][4].

Safety Profile

A poison by subcutaneous and intravenous routes. When heated to decomposition it emits toxic vapors of NOx and HCl.

in vivo

Pentamidine (0.25 mg/mouse; intramuscular injection; every 2 days; for 4 weeks; athymic nude mice) treatment markedly inhibits the growth of WM9 human melanoma tumors in nude mice[1].

Animal Model:Athymic nude mice (6 weeks old) injected with WM9 cells[1]
Dosage:0.25 mg/mouse
Administration:Intramuscular injection; every 2 days; for 4 weeks
Result:Markedly inhibited the growth of WM9 human melanoma tumors in nude mice.

IC 50

Trypanosoma; Leishmania

References

[1] Pathak MK, et al. Pentamidine is an inhibitor of PRL phosphatases with anticancer activity. Mol Cancer Ther. 2002 Dec;1(14):1255-64. PMID:12516958
[2] Nguewa, P.A., et al., Pentamidine is an antiparasitic and apoptotic drug that selectively modifies ubiquitin. Chem Biodivers, 2005. 2(10): p. 1387-400. DOI:10.1002/cbdv.200590111
[3] Sands M, et al. Pentamidine: a review. Rev Infect Dis. 1985 Sep-Oct;7(5):625-34. DOI:10.1093/clinids/7.5.625
[4] David C. Bean, et al. Pentamidine: a drug to consider re-purposing in the targeted treatment of multi-drug resistant bacterial infections? J Lab Precis Med 2017;2:49.

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