-
西帕加明
- names:
Cipargamin
- CAS号:
1193314-23-6
MDL Number: MFCD25976667 - MF(分子式): C19H14Cl2FN3O MW(分子量): 390.24
- EINECS:NA Reaxys Number:1193314-23-6
- Pubchem ID:24662493 Brand:BIOFOUNT
货品编码 | 规格 | 纯度 | 价格 (¥) | 现价(¥) | 特价(¥) | 库存描述 | 数量 | 总计 (¥) |
---|---|---|---|---|---|---|---|---|
YZM000763-5mg | 5mg | >98.0% | ¥ 1822.00 | ¥ 1822.00 | 2-3天 | ¥ 0.00 | ||
YZM000763-2mg | 2mg | >98.0% | ¥ 975.00 | ¥ 975.00 | 2-3天 | ¥ 0.00 |
中文别名 | 西帕加明(Cipargamin,1193314-23-6)(1'R,3'S)-5,7'-二氯-6'-氟-2',3',4',9'-四氢-3'-甲基螺[3H-吲哚-3,1'-[1H]吡啶并[3,4-B]吲哚]-2(1H)-酮 |
英文别名 | Cipargamin(西帕加明,1193314-23-6) |
CAS号 | 1193314-23-6 |
SMILES | FC1=C(Cl)C=C(NC2=C3C[C@H](C)N[C@@]2(C4=C(C=CC(Cl)=C4)N5)C5=O)C3=C1 |
Inchi | InChI=1S/C19H14Cl2FN3O/c1-8-4-11-10-6-14(22)13(21)7-16(10)23-17(11)19(25-8)12-5-9(20)2-3-15(12)24-18(19)26/h2-3,5-8,23,25H,4H2,1H3,(H,24,26)/t8-,19+/m0/s1 |
InchiKey | CKLPLPZSUQEDRT-WPCRTTGESA-N |
分子式 Formula | C19H14Cl2FN3O |
分子量 Molecular Weight | 390.24 |
闪点 FP | 329.6±31.5 °C |
熔点 Melting point | No data available |
沸点 Boiling point | 621.3±55.0 °C at 760 mmHg |
Polarizability极化度 | 39.3±0.5 10-24cm3 |
密度 Density | 1.6±0.1 g/cm3 |
蒸汽压 Vapor Pressure | 0.0±1.8 mmHg at 25°C |
溶解度Solubility | 生物体外In Vitro:DMSO溶解度50 mg/mL(128.13 mM;Need ultrasonic)H2O< 0.1 mg/mL(insoluble) |
性状 | 固体粉末,Power |
储藏条件 Storage conditions | -20°C 3 years年 4°C 2 years年 / In solvent溶液中:-80°C 6 months月 -20°C 1 month月 |
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:西帕加明MSDS,西帕加明蒸汽压,西帕加明合成,西帕加明标准,西帕加明应用,西帕加明合成,西帕加明沸点,西帕加明闪点,西帕加明用途,西帕加明溶解度,西帕加明价格,西帕加明作用,西帕加明结构式,西帕加明用处,西帕加明毒理性质,西帕加明物理性质
产品说明 | 西帕加明(Cipargamin,1193314-23-6) 是一种有效的抗疟疾药,对恶性疟原虫的IC50值约是 1 nM |
Introduction | 西帕加明(Cipargamin,1193314-23-6) is an potent antimalarial compound, withIC50of appr 1 nM againstP. falciparum. |
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 |
A phase 1 evaluation of the pharmacokinetic/pharmacodynamic interaction of the antimalarial agents KAE609 and piperaquine (PPQ) Malaria Journal |
Comparative chemical genomics reveal that the spiroindolone antimalarial KAE609 (Cipargamin) is a P-type ATPase inhibitor Scientific Reports 2016/PMID: 27291296 |
A new lead in malaria/Science-Business eXchange/2010 |
A first-in-human randomized, double-blind, placebo-controlled, single- and multiple-ascending oral dose study of novel spiroindolone KAE609, to assess the safety, tolerability and pharmacokinet/PMID: |
Challenges to replace ACT as first-line drug Malaria Journal/2017/PMID: 28738892 |
Spiroindolone KAE609 for falciparum and vivax malaria
Abstract
Background: KAE609 (cipargamin; formerly NITD609, Novartis Institute for Tropical Diseases) is a new synthetic antimalarial spiroindolone analogue with potent, dose-dependent antimalarial activity against asexual and sexual stages of Plasmodium falciparum.
Methods: We conducted a phase 2, open-label study at three centers in Thailand to assess the antimalarial efficacy, safety, and adverse-event profile of KAE609, at a dose of 30 mg per day for 3 days, in two sequential cohorts of adults with uncomplicated P. vivax malaria (10 patients) or P. falciparum malaria (11). The primary end point was the parasite clearance time.
Results: The median parasite clearance time was 12 hours in each cohort (interquartile range, 8 to 16 hours in patients with P. vivax malaria and 10 to 16 hours in those with P. falciparum malaria). The median half-lives for parasite clearance were 0.95 hours (range, 0.68 to 2.01; interquartile range, 0.85 to 1.14) in the patients with P. vivax malaria and 0.90 hours (range, 0.68 to 1.64; interquartile range, 0.78 to 1.07) in those with P. falciparum malaria. By comparison, only 19 of 5076 patients with P. falciparum malaria (<1%) who were treated with oral artesunate in Southeast Asia had a parasite clearance half-life of less than 1 hour. Adverse events were reported in 14 patients (67%), with nausea being the most common. The adverse events were generally mild and did not lead to any discontinuations of the drug. The mean terminal half-life for the elimination of KAE609 was 20.8 hours (range, 11.3 to 37.6), supporting a once-daily oral dosing regimen.
Conclusions: KAE609, at dose of 30 mg daily for 3 days, cleared parasitemia rapidly in adults with uncomplicated P. vivax or P. falciparum malaria. (Funded by Novartis and others; ClinicalTrials.gov number, NCT01524341.).
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