西帕加明

NMR下載 COA and HPLC MSDS下載
names：
Cipargamin
CAS號：
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

西帕加明(Cipargamin,1193314-23-6) has been used in trials studying the treatment of Malaria, Cure Rate, and Plasmodium Falciparum Malaria.

貨品編碼	規格	純度	價格 (￥)	現價(￥)	特價(￥)	庫存描述	數量	總計 (￥)
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

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中文別名	西帕加明(Cipargamin,1193314-23-6)(1'R,3'S)-5,7'-二氯-6'-氟-2',3',4',9'-四氫-3'-甲基螺[3H-吲哚-3,1'-[1H]吡啶并[3,4-B]吲哚]-2(1H)-酮
英文別名	Cipargamin(西帕加明,1193314-23-6)
CAS號	1193314-23-6
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
溶解度Solubility	生物體外In Vitro:DMSO溶解度50 mg/mL(128.13 mM;Need ultrasonic)H2O< 0.1 mg/mL(insoluble)
性狀	固體粉末,Power
儲藏條件 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

（西帕加明,1193314-23-6)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及有害物質產生，必要時實驗操作需要手套箱內完成以免對實驗人員造成傷害
3.實驗后產生的廢棄物需分類存儲，并交于專業生物廢氣物處理公司處理，以免造成環境污染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,西帕加明蒸汽壓,西帕加明合成,西帕加明標準,西帕加明應用,西帕加明合成,西帕加明沸點,西帕加明閃點,西帕加明用途,西帕加明溶解度,西帕加明價格,西帕加明作用,西帕加明結構式,西帕加明用處,西帕加明毒理性質,西帕加明物理性質

產品說明	西帕加明(Cipargamin,1193314-23-6) 是一種有效的抗瘧疾藥，對惡性瘧原蟲的IC50值約是 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,繼續沖洗+P337如果眼睛刺激持續+P2393獲得醫療建議/護理
備注	實驗過程中防止吸入、食入，做好安全防護

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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