1029939-86-3|Artefenomel|Artefenomel|-范德生物科技公司

Artefenomel

NMR下载 COA and HPLC MSDS下载
names：
Artefenomel
CAS号：
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)是一种合成的含有青蒿素药效团的抗疟疾药物。Artefenomel是一种长效青蒿素相关化合物。

货品编码	规格	纯度	价格 (¥)	现价(¥)	特价(¥)	库存描述	数量	总计 (¥)
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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中文别名	Artefenomel(1029939-86-3);OZ439;OZ-439
英文别名	Artefenomel,1029939-86-3
CAS号	1029939-86-3
SMILES	[H][C@@]1(C[C@H](C2)C3)C4([C@@]3([H])C[C@H]2C1)O[C@]5(OO4)CC[C@H](CC5)C6=CC=C(C=C6)OCCN7CCOCC7
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
闪点 FP	165.7±28.7 °C
熔点 Melting point	152-154 °C
沸点 Boiling point	608.7±55.0 °C at 760 mmHg
Polarizability极化度	51.1±0.5 10-24cm3
密度 Density	1.2±0.1 g/cm3
蒸汽压 Vapor Pressure	0.0±1.7 mmHg at 25°C
溶解度Solubility	生物体外In Vitro:DMSO溶解度4.2 mg/mL(8.94 mM;Need ultrasonic)
性状	白色至灰白色固体粉末
储藏条件 Storage conditions	-20°C，避光，在氮气下保存

Artefenomel(1029939-86-3)实验注意事项：
1.实验前需戴好防护眼镜，穿戴防护服和口罩，佩戴手套，避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生，必要时实验操作需要手套箱内完成以免对实验人员造成伤害
3.实验后产生的废弃物需分类存储，并交于专业生物废气物处理公司处理，以免造成环境污染

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.

Tag:Artefenomel(1029939-86-3),Artefenomel试剂,Artefenomel的作用,Artefenomel的纯度,Artefenomel的厂家,Artefenomel的合成,Artefenomel的价格,Artefenomel的合成,Artefenomel的注意事项,Artefenomel的MSDS

产品说明	Artefenomel(1029939-86-3)是一种合成的含有青蒿素药效团的抗疟疾药物。Artefenomel是一种长效青蒿素相关化合物。
Introduction	Artefenomel (1029939-86-3) is a synthetic antimalarial drug containing artemisinin pharmacophore. Artefenomel is a long-acting artemisinin-related compound.
Application1
Application2
Application3

警示图
危险性	warning
危险性警示	Not available
安全声明	H303吞入可能有害+H313皮肤接触可能有害+H2413吸入可能对身体有害
安全防护	P264处理后彻底清洗+P280戴防护手套/穿防护服/戴防护眼罩/戴防护面具+P305如果进入眼睛+P351用水小心冲洗几分钟+P338取出隐形眼镜（如果有）并且易于操作,继续冲洗+P337如果眼睛刺激持续+P2393获得医疗建议/护理
备注	实验过程中防止吸入、食入，做好安全防护

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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