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MedKoo Cat#: 461448 | Name: Melarsoprol
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Melarsoprol an organoarsenic compound, is widely used for the treatment of trypanosomiasis (human African sleeping sickness).

Chemical Structure

Melarsoprol
Melarsoprol
CAS#494-79-1

Theoretical Analysis

MedKoo Cat#: 461448

Name: Melarsoprol

CAS#: 494-79-1

Chemical Formula: C12H15AsN6OS2

Exact Mass: 397.9965

Molecular Weight: 398.33

Elemental Analysis: C, 36.18; H, 3.80; As, 18.81; N, 21.10; O, 4.02; S, 16.10

Price and Availability

Size Price Availability Quantity
5mg USD 350.00 2 Weeks
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Related CAS #
No Data
Synonym
Melarsoprol; Melarsoprolum; RP 3854; RP-3854; RP3854;
IUPAC/Chemical Name
(2-(4-((4,6-diamino-1,3,5-triazin-2-yl)amino)phenyl)-1,3,2-dithiarsolan-4-yl)methanol
InChi Key
JCYZMTMYPZHVBF-UHFFFAOYSA-N
InChi Code
InChI=1S/C12H15AsN6OS2/c14-10-17-11(15)19-12(18-10)16-8-3-1-7(2-4-8)13-21-6-9(5-20)22-13/h1-4,9,20H,5-6H2,(H5,14,15,16,17,18,19)
SMILES Code
OCC1S[As](C2=CC=C(NC3=NC(N)=NC(N)=N3)C=C2)SC1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.03.00
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 398.33 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Pyana Pati P, Van Reet N, Mumba Ngoyi D, Ngay Lukusa I, Karhemere Bin Shamamba S, Büscher P. Melarsoprol sensitivity profile of Trypanosoma brucei gambiense isolates from cured and relapsed sleeping sickness patients from the Democratic Republic of the Congo. PLoS Negl Trop Dis. 2014 Oct 2;8(10):e3212. doi: 10.1371/journal.pntd.0003212. eCollection 2014 Oct. PubMed PMID: 25275572; PubMed Central PMCID: PMC4183442. 2: Raber G, Raber T, Raml R, Murko M, Magnes C, Francesconi KA. Determination of the trypanocidal drug melarsoprol and its conversion products in biological fluids with HPLC-ICPMS/ESMS. Talanta. 2013 Nov 15;116:876-81. doi: 10.1016/j.talanta.2013.07.066. Epub 2013 Aug 7. PubMed PMID: 24148488. 3: Baumann A, Pfeifer T, Melles D, Karst U. Investigation of the biotransformation of melarsoprol by electrochemistry coupled to complementary LC/ESI-MS and LC/ICP-MS analysis. Anal Bioanal Chem. 2013 Jun;405(15):5249-58. doi: 10.1007/s00216-013-6929-7. Epub 2013 Apr 4. PubMed PMID: 23552974. 4: Kennedy PG. An alternative form of melarsoprol in sleeping sickness. Trends Parasitol. 2012 Aug;28(8):307-10. doi: 10.1016/j.pt.2012.05.003. Epub 2012 Jun 15. PubMed PMID: 22704910. 5: Baker N, de Koning HP, Mäser P, Horn D. Drug resistance in African trypanosomiasis: the melarsoprol and pentamidine story. Trends Parasitol. 2013 Mar;29(3):110-8. doi: 10.1016/j.pt.2012.12.005. Epub 2013 Jan 30. Review. PubMed PMID: 23375541; PubMed Central PMCID: PMC3831158. 6: Graf FE, Baker N, Munday JC, de Koning HP, Horn D, Mäser P. Chimerization at the AQP2-AQP3 locus is the genetic basis of melarsoprol-pentamidine cross-resistance in clinical Trypanosoma brucei gambiense isolates. Int J Parasitol Drugs Drug Resist. 2015 May 7;5(2):65-8. doi: 10.1016/j.ijpddr.2015.04.002. eCollection 2015 Aug. PubMed PMID: 26042196; PubMed Central PMCID: PMC4443405. 7: Graf FE, Ludin P, Wenzler T, Kaiser M, Brun R, Pyana PP, Büscher P, de Koning HP, Horn D, Mäser P. Aquaporin 2 mutations in Trypanosoma brucei gambiense field isolates correlate with decreased susceptibility to pentamidine and melarsoprol. PLoS Negl Trop Dis. 2013 Oct 10;7(10):e2475. doi: 10.1371/journal.pntd.0002475. eCollection 2013. PubMed PMID: 24130910; PubMed Central PMCID: PMC3794916. 8: Rodgers J, Jones A, Gibaud S, Bradley B, McCabe C, Barrett MP, Gettinby G, Kennedy PG. Melarsoprol cyclodextrin inclusion complexes as promising oral candidates for the treatment of human African trypanosomiasis. PLoS Negl Trop Dis. 2011 Sep;5(9):e1308. doi: 10.1371/journal.pntd.0001308. Epub 2011 Sep 6. PubMed PMID: 21909447; PubMed Central PMCID: PMC3167784. 9: Kuepfer I, Schmid C, Allan M, Edielu A, Haary EP, Kakembo A, Kibona S, Blum J, Burri C. Safety and efficacy of the 10-day melarsoprol schedule for the treatment of second stage Rhodesiense sleeping sickness. PLoS Negl Trop Dis. 2012 Aug;6(8):e1695. doi: 10.1371/journal.pntd.0001695. Epub 2012 Aug 28. PubMed PMID: 22970329; PubMed Central PMCID: PMC3435133. 10: Burri C. An alternative form of melarsoprol in sleeping sickness: is an old drug always the best basis for a new one? Trends Parasitol. 2012 Sep;28(9):354-5. doi: 10.1016/j.pt.2012.06.002. Epub 2012 Aug 3. PubMed PMID: 22867944. 11: Barat C, Pepin J, Tremblay MJ. HIV-1 replication in monocyte-derived dendritic cells is stimulated by melarsoprol, one of the main drugs against human African trypanosomiasis. J Mol Biol. 2011 Jul 29;410(5):1052-64. doi: 10.1016/j.jmb.2011.03.012. PubMed PMID: 21763506. 12: Baker N, Glover L, Munday JC, Aguinaga Andrés D, Barrett MP, de Koning HP, Horn D. Aquaglyceroporin 2 controls susceptibility to melarsoprol and pentamidine in African trypanosomes. Proc Natl Acad Sci U S A. 2012 Jul 3;109(27):10996-1001. doi: 10.1073/pnas.1202885109. Epub 2012 Jun 18. PubMed PMID: 22711816; PubMed Central PMCID: PMC3390834. 13: Mpia B, Pépin J. Combination of eflornithine and melarsoprol for melarsoprol-resistant Gambian trypanosomiasis. Trop Med Int Health. 2002 Sep;7(9):775-9. PubMed PMID: 12225509. 14: Bisser S, N'Siesi FX, Lejon V, Preux PM, Van Nieuwenhove S, Miaka Mia Bilenge C, Būscher P. Equivalence trial of melarsoprol and nifurtimox monotherapy and combination therapy for the treatment of second-stage Trypanosoma brucei gambiense sleeping sickness. J Infect Dis. 2007 Feb 1;195(3):322-9. Epub 2006 Dec 21. PubMed PMID: 17205469. 15: Alibu VP, Richter C, Voncken F, Marti G, Shahi S, Renggli CK, Seebeck T, Brun R, Clayton C. The role of Trypanosoma brucei MRPA in melarsoprol susceptibility. Mol Biochem Parasitol. 2006 Mar;146(1):38-44. Epub 2005 Nov 18. PubMed PMID: 16343658. 16: Keiser J, Ericsson O, Burri C. Investigations of the metabolites of the trypanocidal drug melarsoprol. Clin Pharmacol Ther. 2000 May;67(5):478-88. PubMed PMID: 10824626. 17: Matovu E, Enyaru JC, Legros D, Schmid C, Seebeck T, Kaminsky R. Melarsoprol refractory T. b. gambiense from Omugo, north-western Uganda. Trop Med Int Health. 2001 May;6(5):407-11. PubMed PMID: 11348535. 18: Balasegaram M, Harris S, Checchi F, Ghorashian S, Hamel C, Karunakara U. Melarsoprol versus eflornithine for treating late-stage Gambian trypanosomiasis in the Republic of the Congo. Bull World Health Organ. 2006 Oct;84(10):783-91. PubMed PMID: 17128358; PubMed Central PMCID: PMC2627491. 19: Robays J, Raguenaud ME, Josenando T, Boelaert M. Eflornithine is a cost-effective alternative to melarsoprol for the treatment of second-stage human West African trypanosomiasis in Caxito, Angola. Trop Med Int Health. 2008 Feb;13(2):265-71. doi: 10.1111/j.1365-3156.2007.01999.x. PubMed PMID: 18304274. 20: Jennings FW, Rodgers J, Bradley B, Gettinby G, Kennedy PG, Murray M. Human African trypanosomiasis: potential therapeutic benefits of an alternative suramin and melarsoprol regimen. Parasitol Int. 2002 Dec;51(4):381-8. PubMed PMID: 12421636.