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Artefenomel

NMR下載 COA and HPLC MSDS下載
names：
Artefenomel
CAS號：
1029939-86-3
MDL Number：
MF(分子式)： C28H39NO5 MW(分子量)： 469.61
EINECS: Reaxys Number:
Pubchem ID:24999143 Brand:BIOFOUNT

Artefenomel(1029939-86-3)是一種合成的含有青蒿素藥效團的抗瘧疾藥物。Artefenomel是一種長效青蒿素相關(guān)化合物。

貨品編碼	規(guī)格	純度	價格 (￥)	現(xiàn)價(￥)	特價(￥)	庫存描述	數(shù)量	總計 (￥)
YZM000800-10mg	10mg	99.4%	￥ 7590.00	￥ 7590.00		2-3天	- +	￥ 0.00
YZM000800-5mg	5mg	99.4%	￥ 4388.00	￥ 4388.00		2-3天	- +	￥ 0.00

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中文別名	Artefenomel(1029939-86-3);OZ439;OZ-439
英文別名	Artefenomel,1029939-86-3
CAS號	1029939-86-3
Inchi	InChI=1S/C28H39NO5/c1-3-26(31-14-11-29-9-12-30-13-10-29)4-2-22(1)23-5-7-27(8-6-23)32-28(34-33-27)24-16-20-15-21(18-24)19-25(28)17-20/h1-4,20-21,23-25H,5-19H2/t20,21,23-,24,25,27+,28
InchiKey	XLCNVWUKICLURR-BGJLAERMSA-N
分子式 Formula	C28H39NO5
分子量 Molecular Weight	469.61
溶解度Solubility	生物體外In Vitro:DMSO溶解度4.2 mg/mL(8.94 mM;Need ultrasonic)
性狀	白色至灰白色固體粉末
儲藏條件 Storage conditions	-20°C，避光，在氮氣下保存

Artefenomel(1029939-86-3)實驗注意事項：
1.實驗前需戴好防護眼鏡，穿戴防護服和口罩，佩戴手套，避免與皮膚接觸。
2.實驗過程中如遇到有毒或者刺激性物質(zhì)及有害物質(zhì)產(chǎn)生，必要時實驗操作需要手套箱內(nèi)完成以免對實驗人員造成傷害
3.實驗后產(chǎn)生的廢棄物需分類存儲，并交于專業(yè)生物廢氣物處理公司處理，以免造成環(huán)境污染

Artefenomel(1029939-86-3) Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.

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產(chǎn)品說明	Artefenomel(1029939-86-3)是一種合成的含有青蒿素藥效團的抗瘧疾藥物。Artefenomel是一種長效青蒿素相關(guān)化合物。
Introduction	Artefenomel (1029939-86-3) is a synthetic antimalarial drug containing artemisinin pharmacophore. Artefenomel is a long-acting artemisinin-related compound.
Application1
Application2
Application3

警示圖
危險性	warning
危險性警示	Not available
安全聲明	H303吞入可能有害+H313皮膚接觸可能有害+H2413吸入可能對身體有害
安全防護	P264處理后徹底清洗+P280戴防護手套/穿防護服/戴防護眼罩/戴防護面具+P305如果進入眼睛+P351用水小心沖洗幾分鐘+P338取出隱形眼鏡（如果有）并且易于操作,繼續(xù)沖洗+P337如果眼睛刺激持續(xù)+P2393獲得醫(yī)療建議/護理
備注	實驗過程中防止吸入、食入，做好安全防護

In vitro activity of anti-malarial ozonides against an artemisinin-resistant isolate(Malaria Journal,2017)

Anti-malarial ozonides OZ439 and OZ609 tested at clinically relevant compound exposure parameters in a novel ring-stage survival assay(Malaria Journal,2019)

African isolates show a high proportion of multiple copies of the Plasmodium falciparum plasmepsin-2 gene, a piperaquine resistance marker

Spray drying OZ439 nanoparticles to form stable, water-dispersible powders for oral malaria therapy(Journal of Translational Medicine,2019)

Road Towards Development of New Antimalarial: Organelle Associated Metabolic Pathways in Plasmodium as Drug Targets and Discovery of Lead Drug Candidates

Contemporary Approaches for Malaria Drug Discovery
Abstract:Malaria is a major global health problem, caused by Plasmodium sps. Clinical symptoms of the disease are associated with asexual stages of parasite life cycle in human erythrocytes whereas transmission of disease is attributed to sexual stages in mosquito. Increasing resistance to known antimalarial drugs has resulted in the evolution of newer approaches of drug discovery against the disease. The conventional phenotypic screening approaches of drug discovery enable high-throughput screening of a library of chemical compounds for antimalarial effect followed by target identification and its experimental validation. Alternatively, target-based approach for drug discovery involves screening of compounds against known parasite targets by in vitro and in vivo studies. This chapter focuses on the contemporary approaches in antimalarial drug discovery that promise the development of an effective strategy to combat malaria.

New endoperoxides highly active in vivo and in vitro against artemisinin-resistant Plasmodium falciparum
Background:The emergence and spread of Plasmodium falciparum resistance to artemisinin-based combination therapy in Southeast Asia prompted the need to develop new endoperoxide-type drugs.
Methods:A chemically diverse library of endoperoxides was designed and synthesized. The compounds were screened for in vitro and in vivo anti-malarial activity using, respectively, the SYBR Green I assay and a mouse model. Ring survival and mature stage survival assays were performed against artemisinin-resistant and artemisinin-sensitive P. falciparum strains. Cytotoxicity was evaluated against mammalian cell lines V79 and HepG2, using the MTT assay.
Results:The synthesis and anti-malarial activity of 21 new endoperoxide-derived compounds is reported, where the peroxide pharmacophore is part of a trioxolane (ozonide) or a tetraoxane moiety, flanked by adamantane and a substituted cyclohexyl ring. Eight compounds exhibited sub-micromolar anti-malarial activity (IC50 0.3–71.1 nM), no cross-resistance with artemisinin or quinolone derivatives and negligible cytotoxicity towards mammalian cells. From these, six produced ring stage survival < 1% against the resistant strain IPC5202 and three of them totally suppressed Plasmodium berghei parasitaemia in mice after oral administration.
Conclusion:The investigated, trioxolane–tetrazole conjugates LC131 and LC136 emerged as potential anti-malarial candidates; they show negligible toxicity towards mammalian cells, ability to kill intra-erythrocytic asexual stages of artemisinin-resistant P. falciparum and capacity to totally suppress P. berghei parasitaemia in mice.

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