Benflumetol - CAS 82186-77-4
Catalog number: 82186-77-4
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C30H32Cl3NO
Molecular Weight:
528.94
COA:
Inquire
Targets:
Others
Description:
Benflumetol, also known as HSDB 7210, is an antimalarial drug used to treat acute uncomplicated malaria. It is used in combination with Artemether for improved efficacy. It inhibits hemozoin formation. It is is an antimalarial for the treatment of multi-drug resistant strains of falciparum malaria.
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Purity:
>98%
Appearance:
Yellow Solid
Synonyms:
Lumefantrine;(9Z)-2,7-Dichloro-9-[(4-chlorophenyl)methylene]-a-[(dibutylamino)methyl]-9H-fluorene-4-methanol;2-Dibutylamino-1-[2,7-dichloro-9-[1-(4-chlorophenyl)meth-(Z)-ylidene]-9H-fluoren-4-yl]ethanol;(Z)-2-(Dibutylamino)-1-(2,7-dichloro-9-(4-chlorobenzylidene)-9H-fluoren-4-yl)ethanol 2-(dibutylamino)-1-[(9Z)-2,7-dichloro-9-[(4-chlorophenyl)methylidene]fluoren-4-yl]ethanol
Solubility:
10 mM in DMSO
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
Benflumetol is used in combination with Artemether for improved efficacy. It inhibits hemozoin formation. It is is an antimalarial for the treatment of multi-drug resistant strains of falciparum malaria.
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Kilogram to ton
Boiling Point:
642.5±55.0 °C | Condition: Press: 760 Torr
Melting Point:
129-131°C
Density:
1.252±0.06 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
InChIKey:
DYLGFOYVTXJFJP-MYYYXRDXSA-N
InChI:
InChI=1S/C30H32Cl3NO/c1-3-5-13-34(14-6-4-2)19-29(35)28-18-23(33)17-27-25(15-20-7-9-21(31)10-8-20)26-16-22(32)11-12-24(26)30(27)28/h7-12,15-18,29,35H,3-6,13-14,19H2,1-2H3/b25-15-
Canonical SMILES:
CCCCN(CCCC)CC(C1=C2C3=C(C=C(C=C3)Cl)C(=CC4=CC=C(C=C4)Cl)C2=CC(=C1)Cl)O
Current Developer:
Benflumetol has been listed.
1.Primaquine plus artemisinin combination therapy for reduction of malaria transmission: promise and risk.
John CC1. BMC Med. 2016 Apr 1;14(1):65. doi: 10.1186/s12916-016-0611-9.
Reduction of gametocyte transmission from humans to mosquitoes is a key component of malaria elimination. The study by Gonçalves and colleagues provides valuable new data on how the addition of low-dose primaquine to artemether-lumefantrine affects reduction of gametocytemia and transmission of gametocytes to mosquitoes in asymptomatically Plasmodium falciparum-infected children without G6PD deficiency, and on the degree to which low-dose primaquine affects hemoglobin levels in these children. The study sets the stage for future research required for consideration of an artemisinin combination therapy (ACT)-primaquine regimen in mass drug administration campaigns. Future studies will need to evaluate toxicity in adults and G6PD deficient persons, assess gametocyte transmission from adults, evaluate different ACT drugs with primaquine, and assess the implications of "rare" toxicities in large treatment populations, such as hemolysis requiring blood transfusion.
2.CRISPR-Cas9-modified pfmdr1 protects Plasmodium falciparum asexual blood stages and gametocytes against a class of piperazine-containing compounds but potentiates artemisinin-based combination therapy partner drugs.
Ng CL1, Siciliano G2, Lee MC1, de Almeida MJ, Corey VC3, Bopp SE3, Bertuccini L4, Wittlin S5, Kasdin RG1, Le Bihan A6, Clozel M6, Winzeler EA3, Alano P2, Fidock DA1,7. Mol Microbiol. 2016 Apr 12. doi: 10.1111/mmi.13397. [Epub ahead of print]
Emerging resistance to first-line antimalarial combination therapies threatens malaria treatment and the global elimination campaign. Improved therapeutic strategies are required to protect existing drugs and enhance treatment efficacy. We report that the piperazine-containing compound ACT-451840 exhibits single-digit nanomolar inhibition of the Plasmodium falciparum asexual blood stages and transmissible gametocyte forms. Genome sequence analyses of in vitro-derived ACT-451840-resistant parasites revealed single nucleotide polymorphisms in pfmdr1, which encodes a digestive vacuole membrane-bound ABC transporter known to alter P. falciparum susceptibility to multiple first-line antimalarials. CRISPR-Cas9 based gene editing confirmed that PfMDR1 point mutations mediated ACT-451840 resistance. Resistant parasites demonstrated increased susceptibility to the clinical drugs lumefantrine, mefloquine, quinine, and amodiaquine. Stage V gametocytes harboring Cas9-introduced pfmdr1 mutations also acquired ACT-451840 resistance.
3.Quality Assessment of Artemether-Lumefantrine Samples and Artemether Injections Sold in the Cape Coast Metropolis.
Prah J1, Ameyaw EO2, Afoakwah R2, Fiawoyife P3, Oppong-Danquah E3, Boampong JN2. J Trop Med. 2016;2016:8602619. doi: 10.1155/2016/8602619. Epub 2016 Feb 23.
Most prescribers and patients in Ghana now opt for the relatively expensive artemether/lumefantrine rather than artesunate-amodiaquine due to undesirable side effects in the treatment of uncomplicated malaria. The study sought to determine the existence of substandard and/or counterfeit artemether-lumefantrine tablets and suspension as well as artemether injection on the market in Cape Coast. Six brands of artemether-lumefantrine tablets, two brands of artemether-lumefantrine suspensions, and two brands of artemether injections were purchased from pharmacies in Cape Coast for the study. The mechanical properties of the tablets were evaluated. The samples were then analyzed for the content of active ingredients using High Performance Liquid Chromatography with a variable wavelength detector. None of the samples was found to be counterfeit. However, the artemether content of the samples was variable (93.22%-104.70% of stated content by manufacturer).
4.Risk factors for Plasmodium falciparum and Plasmodium vivax gametocyte carriage in Papua New Guinean children with uncomplicated malaria.
Karl S1, Laman M2, Moore BR3, Benjamin JM2, Salib M2, Lorry L2, Maripal S2, Siba P2, Robinson LJ4, Mueller I1, Davis TM5. Acta Trop. 2016 Apr 4;160:1-8. doi: 10.1016/j.actatropica.2016.04.002. [Epub ahead of print]
There are limited data on gametocytaemia risk factors before/after treatment with artemisinin combination therapy in children from areas with transmission of multiple Plasmodium species. We utilised data from a randomised trial comparing artemether-lumefantrine (AL) and artemisinin-naphthoquine (AN) in 230 Papua New Guinean children aged 0.5-5 years with uncomplicated malaria in whom determinants of gametocytaemia by light microscopy were assessed at baseline using logistic regression and during follow-up using multilevel mixed effects modelling. Seventy-four (32%) and 18 (8%) children presented with P. falciparum and P. vivax gametocytaemia, respectively. Baseline P. falciparum gametocytaemia was associated with Hackett spleen grade 1 (odds ratio (95% CI) 4.01 (1.60-10.05) vs grade 0; P<0.001) and haemoglobin (0.95 (0.92-0.97) per 1g/L increase; P<0.001), and P. falciparum asexual parasitaemia in slide-positive cases (0.36 (0.19-0.
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CAS 82186-77-4 Benflumetol

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