1. Anti-infection
  2. Parasite
  3. Melarsoprol

Melarsoprol, a melaminophenylarsine-type trivalent organic arsenical, is an important drug for African trypanosomiasis. Melarsoprol is also active against leukemia cell lines and plasma cells from myeloma patients. Melarsoprol increases the biliary output of GSH in rats.

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Melarsoprol Chemical Structure

Melarsoprol Chemical Structure

CAS No. : 494-79-1

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  • Biological Activity

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Description

Melarsoprol, a melaminophenylarsine-type trivalent organic arsenical, is an important drug for African trypanosomiasis. Melarsoprol is also active against leukemia cell lines and plasma cells from myeloma patients. Melarsoprol increases the biliary output of GSH in rats[1].

Cellular Effect
Cell Line Type Value Description References
J774 IC50
4.3 μM
Compound: S4
Cytotoxicity against J774.1 cell line after 48 hrs
Cytotoxicity against J774.1 cell line after 48 hrs
[PMID: 16516467]
L6 IC50
0.005 μg/mL
Compound: Melarsoprol
Antitrypanosomal activity against trypomastigotes of Trypanosoma brucei rhodesiense STIB 900 infected in rat L6 cells after 72 hrs by alamar blue assay
Antitrypanosomal activity against trypomastigotes of Trypanosoma brucei rhodesiense STIB 900 infected in rat L6 cells after 72 hrs by alamar blue assay
[PMID: 22352841]
L6 EC50
0.0075 μM
Compound: melarsoprol
Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected in rat L6 cells after 72 hrs by alamar blue assay
Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected in rat L6 cells after 72 hrs by alamar blue assay
[PMID: 22390399]
L6 IC50
0.008 μM
Compound: Melarsoprol
Antimicrobial activity against trypomastigote stage of Trypanosoma brucei rhodesiense STIB900 infected in rat L6 cells after 96 hrs by Alamar Blue assay
Antimicrobial activity against trypomastigote stage of Trypanosoma brucei rhodesiense STIB900 infected in rat L6 cells after 96 hrs by Alamar Blue assay
[PMID: 24865793]
L6 IC50
0.01 μM
Compound: Melarsoprol
Antitrypanosomal activity against blood stream form of Trypanosoma brucei rhodesiense STIB 900 infected in rat L6 cells after 72 hrs by alamar blue assay
Antitrypanosomal activity against blood stream form of Trypanosoma brucei rhodesiense STIB 900 infected in rat L6 cells after 72 hrs by alamar blue assay
[PMID: 22023653]
L6 IC50
0.013 μM
Compound: Melarsoprol
Antiparasitic activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 infected in rat L6 cells after 72 hrs by Alamar blue assay
Antiparasitic activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 infected in rat L6 cells after 72 hrs by Alamar blue assay
[PMID: 21937228]
L6 IC50
1.3 μg/mL
Compound: Melarsoprol
Cytotoxicity against in rat L6 cells assessed as reduction in cell viability after 70 hrs by alamar blue assay
Cytotoxicity against in rat L6 cells assessed as reduction in cell viability after 70 hrs by alamar blue assay
[PMID: 21353728]
L6 IC50
18.3 μM
Compound: Melarsoprol
Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay
Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay
[PMID: 26237241]
L6 IC50
18.3 μM
Compound: Melarsoprol
Cytotoxicity against rat L6 cells assessed as growth inhibition after 72 hrs by inverted microscopy
Cytotoxicity against rat L6 cells assessed as growth inhibition after 72 hrs by inverted microscopy
[PMID: 23153330]
L6 IC50
19000 nM
Compound: Melarsoprol
Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by MTT assay
Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by MTT assay
[PMID: 24398295]
L6 IC50
24.2 μM
Compound: Melarsoprol
Cytotoxicity against rat L6 cells assessed as reduction in cell viability measured after 72 hrs by Alamar blue based inverted microscopy analysis
Cytotoxicity against rat L6 cells assessed as reduction in cell viability measured after 72 hrs by Alamar blue based inverted microscopy analysis
[PMID: 31784198]
L6 CC50
28.9 μM
Compound: MEL
Cytotoxicity against rat L6 cels assessed as reduction in cell viability after 72 hrs by Alamar Blue dye-based fluorometric analysis
Cytotoxicity against rat L6 cels assessed as reduction in cell viability after 72 hrs by Alamar Blue dye-based fluorometric analysis
[PMID: 30615444]
L6 IC50
29 μM
Compound: Melarsoprol
Cytotoxicity against rat L6 cells assessed as growth inhibition after 72 hrs by alamar blue assay
Cytotoxicity against rat L6 cells assessed as growth inhibition after 72 hrs by alamar blue assay
[PMID: 28284860]
L6 IC50
5.1 μM
Compound: Melarsoprol
Cytotoxicity against rat L6 cells after 3 days by Alamar blue assay
Cytotoxicity against rat L6 cells after 3 days by Alamar blue assay
[PMID: 24956553]
L6 IC50
5.12 μM
Compound: MSP
Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by Alamar blue assay
Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by Alamar blue assay
[PMID: 24268543]
L6 IC50
5.12 μM
Compound: MSP, MLSP
Cytotoxicity against rat L6 cells after 72 hrs by Alamar Blue assay
Cytotoxicity against rat L6 cells after 72 hrs by Alamar Blue assay
[PMID: 23795673]
L6 IC50
5.12 μM
Compound: Melarsoprol
Cytotoxicity against rat L6 cells measured after 70 hrs by alamar blue staining based fluorescence analysis
Cytotoxicity against rat L6 cells measured after 70 hrs by alamar blue staining based fluorescence analysis
[PMID: 27102161]
L6 IC50
7.78 mM
Compound: MLSP
Cytotoxicity against rat L6 cells after 72 hrs by Alamar blue assay
Cytotoxicity against rat L6 cells after 72 hrs by Alamar blue assay
[PMID: 23871911]
L6 IC50
7.78 μM
Compound: mel
Cytotoxicity against rat L6 cells after 70 hrs by Alamar blue assay
Cytotoxicity against rat L6 cells after 70 hrs by Alamar blue assay
[PMID: 33148495]
L6 IC50
7.78 μM
Compound: MEL
Cytotoxicity against rat L6 cells assessed as growth inhibition after 70 hrs by alamar blue assay
Cytotoxicity against rat L6 cells assessed as growth inhibition after 70 hrs by alamar blue assay
[PMID: 28031151]
L6 IC50
7.78 μM
Compound: MLSP
Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay
Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay
[PMID: 19928900]
L6 IC50
7.78 μM
Compound: MLSP
Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay
Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay
[PMID: 19606902]
L6 IC50
7.78 μM
Compound: MAP
Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay
Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay
[PMID: 19267462]
L6 IC50
7.78 μM
Compound: MEL
Cytotoxicity against rat L6 cells assessed as reduction in cell viability after 72 hrs by Alamar blue assay
Cytotoxicity against rat L6 cells assessed as reduction in cell viability after 72 hrs by Alamar blue assay
[PMID: 27344215]
L6 IC50
7.78 μM
Compound: Ml
Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay
Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay
[PMID: 25746816]
L6 IC50
7.78 μM
Compound: Mel
Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay
Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay
[PMID: 19395265]
L6 IC50
7.78 μM
Compound: Mel
Cytotoxicity against rat L6 cells after 72 hrs by microplate fluorometry
Cytotoxicity against rat L6 cells after 72 hrs by microplate fluorometry
[PMID: 23880082]
L6 IC50
7.78 μM
Compound: melarsoprol (mel)
Cytotoxicity against rat L6 cells after 72 hrs by microplate alamar blue assay
Cytotoxicity against rat L6 cells after 72 hrs by microplate alamar blue assay
[PMID: 18502136]
L6 IC50
7.78 μM
Compound: mel
Cytotoxicity against rat L6 cells after 72 hrs by microplate assay
Cytotoxicity against rat L6 cells after 72 hrs by microplate assay
[PMID: 17544672]
L6 IC50
7.8 μM
Compound: Melarsoprol
Concentration causing cytotoxicity to 50% of L-6 rat skeletal myoblasts
Concentration causing cytotoxicity to 50% of L-6 rat skeletal myoblasts
[PMID: 16107157]
L6 IC50
7.9 μM
Compound: MLS
Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay
Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay
[PMID: 20047276]
MRC5 IC50
7.4 μM
Compound: Melarsoprol
Cytotoxicity against human MRC5 SV2 cells assessed as reduction in cell growth after 72 hrs
Cytotoxicity against human MRC5 SV2 cells assessed as reduction in cell growth after 72 hrs
[PMID: 25199582]
Molecular Weight

398.34

Formula

C12H15AsN6OS2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OCC1S[As](SC1)C2=CC=C(C=C2)NC3=NC(N)=NC(N)=N3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 36 mg/mL (90.38 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5104 mL 12.5521 mL 25.1042 mL
5 mM 0.5021 mL 2.5104 mL 5.0208 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.0%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5104 mL 12.5521 mL 25.1042 mL 62.7605 mL
5 mM 0.5021 mL 2.5104 mL 5.0208 mL 12.5521 mL
10 mM 0.2510 mL 1.2552 mL 2.5104 mL 6.2760 mL
15 mM 0.1674 mL 0.8368 mL 1.6736 mL 4.1840 mL
20 mM 0.1255 mL 0.6276 mL 1.2552 mL 3.1380 mL
25 mM 0.1004 mL 0.5021 mL 1.0042 mL 2.5104 mL
30 mM 0.0837 mL 0.4184 mL 0.8368 mL 2.0920 mL
40 mM 0.0628 mL 0.3138 mL 0.6276 mL 1.5690 mL
50 mM 0.0502 mL 0.2510 mL 0.5021 mL 1.2552 mL
60 mM 0.0418 mL 0.2092 mL 0.4184 mL 1.0460 mL
80 mM 0.0314 mL 0.1569 mL 0.3138 mL 0.7845 mL
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Melarsoprol Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Melarsoprol
Cat. No.:
HY-119594
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