36167-63-2|盐酸卤泛群|Halofantrine hydrochloride|MFCD00879136-范德生物科技公司

盐酸卤泛群

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names：
Halofantrine hydrochloride
CAS号：
36167-63-2
MDL Number： MFCD00879136
MF(分子式)： C26H31Cl3F3NO MW(分子量)： 536.88
EINECS:252-895-4 Reaxys Number:
Pubchem ID:37392 Brand:BIOFOUNT

盐酸卤泛群(36167-63-2,Halofantrine hydrochloride)是一种通过抑制人ERG通道来延迟整流钾电流的阻滞剂，是一种有效的抗疟疾产品。

货品编码	规格	纯度	价格 (¥)	现价(¥)	特价(¥)	库存描述	数量	总计 (¥)
YZM000818-10mg	10mg	>98.0%	¥ 2328.00	¥ 2328.00		2-3天	- +	¥ 0.00
YZM000818-5mg	5mg	>98.0%	¥ 1268.00	¥ 1268.00		2-3天	- +	¥ 0.00

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中文别名	盐酸卤泛群(36167-63-2,Halofantrine hydrochloride);卤泛群盐酸盐
英文别名	Halofantrine hydrochloride(36167-63-2)
CAS号	36167-63-2
SMILES	OC(CCN(CCCC)CCCC)C1=CC2=C(Cl)C=C(Cl)C=C2C3=CC(C(F)(F)F)=CC=C31.[H]Cl
Inchi	InChI=1S/C26H30Cl2F3NO.ClH/c1-3-5-10-32(11-6-4-2)12-9-25(33)23-16-22-21(14-18(27)15-24(22)28)20-13-17(26(29,30)31)7-8-19(20)23;/h7-8,13-16,25,33H,3-6,9-12H2,1-2H3;1H
InchiKey	WANGFTDWOFGECH-UHFFFAOYSA-N
分子式 Formula	C26H31Cl3F3NO
分子量 Molecular Weight	536.88
闪点 FP	NA
熔点 Melting point	198-200 °C
沸点 Boiling point	NA
Polarizability极化度	NA
密度 Density	NA
蒸汽压 Vapor Pressure	NA
溶解度Solubility	生物体外In Vitro:DMSO溶解度30 mg/mL(55.88 mM;Need ultrasonic)
性状	白色至灰白色固体粉末
储藏条件 Storage conditions	-20°C 3 years年 4°C 2 years年 /溶液中:-80°C 6 months月 -20°C 1 month月

盐酸卤泛群(36167-63-2,Halofantrine hydrochloride)毒性测试：

生物	测试类型	路线	报告剂量（标准化剂量）	影响	参考
man	TDLo	oral	7143ug/kg (7.143mg/kg)	LIVER: LIVER FUNCTION TESTS IMPAIRED KIDNEY, URETER, AND BLADDER: URINE VOLUME DECREASED KIDNEY, URETER, AND BLADDER: HEMATURIA	Lancet. Vol. 340, Pg. 909, 1992.
man	TDLo	oral	7143ug/kg (7.143mg/kg)	LIVER: "JAUNDICE, OTHER OR UNCLASSIFIED" BLOOD: OTHER HEMOLYSIS WITH OR WITHOUT ANEMIA KIDNEY, URETER, AND BLADDER: URINE VOLUME DECREASED	Lancet. Vol. 340, Pg. 909, 1992.
man	TDLo	oral	18mg/kg/D (18mg/kg)	GASTROINTESTINAL: OTHER CHANGES GASTROINTESTINAL: NAUSEA OR VOMITING	Drugs of the Future. Vol. 5, Pg. 547, 1980.
rat	LD50	intraperitoneal	2050mg/kg (2050mg/kg)		Acta Tropica. Vol. 37, Pg. 232, 1980.
rat	LD50	intraperitoneal	2050mg/kg (2050mg/kg)	GASTROINTESTINAL: NAUSEA OR VOMITING	Acta Tropica. Vol. 37, Pg. 232, 1980.
rat	LD50	oral	3400mg/kg (3400mg/kg)		Acta Tropica. Vol. 37, Pg. 232, 1980.
rat	LD50	oral	3400mg/kg (3400mg/kg)	GASTROINTESTINAL: NAUSEA OR VOMITING	Acta Tropica. Vol. 37, Pg. 232, 1980.
women	LDLo	oral	72mg/kg/3D-I (72mg/kg)	CARDIAC: CARDIOMYOPATHY INCLUDING INFARCTION	Lancet. Vol. 341, Pg. 1054, 1993.

盐酸卤泛群(36167-63-2,Halofantrine hydrochloride)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

Halofantrine hydrochloride(36167-63-2) 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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产品说明	盐酸卤泛群(36167-63-2,Halofantrine hydrochloride)是一种通过抑制人ERG通道来延迟整流钾电流的阻滞剂，是一种有效的抗疟疾产品。
Introduction	Halofantrine hydrochloride (36167-63-2,盐酸卤泛群) is a blocker that delays rectifying potassium current by inhibiting human ERG channels and is an effective anti-malarial product.
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

Some haematological parameters of albino mice experimentally inoculated with Trypanosoma brucei brucei after administration of Halofantrine hydrochloride, chloroquine and diaminazine aceturate

Plasma concentrations of the enantiomers of halofantrine and its main metabolite in malaria patients(European Journal of Clinical Pharmacology,1994)

Effect of kolanut on the pharmacokinetics of the antimalarial drug halofantrine(European Journal of Clinical Pharmacology,2007)

Pharmacokinetics of halofantrine and n-desbutylhalofantrine in patients with falciparum malaria following a multiple dose regimen of halofantrine

Drug Solubilization Behavior During in Vitro Digestion of Suspension Formulations of Poorly Water-Soluble Drugs in Triglyceride Lipids

High-level artemisinin-resistance with quinine co-resistance emerges in P. falciparum malaria under in vivo artesunate pressure
Background:Humanity has become largely dependent on artemisinin derivatives for both the treatment and control of malaria, with few alternatives available. A Plasmodium falciparum phenotype with delayed parasite clearance during artemisinin-based combination therapy has established in Southeast Asia, and is emerging elsewhere. Therefore, we must know how fast, and by how much, artemisinin-resistance can strengthen.
Methods:P. falciparum was subjected to discontinuous in vivo artemisinin drug pressure by capitalizing on a novel model that allows for long-lasting, high-parasite loads. Intravenous artesunate was administered, using either single flash-doses or a 2-day regimen, to P. falciparum-infected humanized NOD/SCID IL-2Rγ−/−immunocompromised mice, with progressive dose increments as parasites recovered. The parasite’s response to artemisinins and other available anti-malarial compounds was characterized in vivo and in vitro.
Results:Artemisinin resistance evolved very rapidly up to extreme, near-lethal doses of artesunate (240 mg/kg), an increase of > 3000-fold in the effective in vivo dose, far above resistance levels reported from the field. Artemisinin resistance selection was reproducible, occurring in 80% and 41% of mice treated with flash-dose and 2-day regimens, respectively, and the resistance phenotype was stable. Measuring in vitro sensitivity proved inappropriate as an early marker of resistance, as IC50 remained stable despite in vivo resistance up to 30 mg/kg (ART-S: 10.7 nM (95% CI 10.2–11.2) vs. ART-R30: 11.5 nM (6.6–16.9), F = 0.525, p = 0.47). However, when in vivo resistance strengthened further, IC50 increased 10-fold (ART-R240 100.3 nM (92.9–118.4), F = 304.8, p < 0.0001), reaching a level much higher than ever seen in clinical samples. Artemisinin resistance in this African P. falciparum strain was not associated with mutations in kelch-13, casting doubt over the universality of this genetic marker for resistance screening. Remarkably, despite exclusive exposure to artesunate, full resistance to quinine, the only other drug sufficiently fast-acting to deal with severe malaria, evolved independently in two parasite lines exposed to different artesunate regimens in vivo, and was confirmed in vitro.
Conclusion:P. falciparum has the potential to evolve extreme artemisinin resistance and more complex patterns of multidrug resistance than anticipated. If resistance in the field continues to advance along this trajectory, we will be left with a limited choice of suboptimal treatments for acute malaria, and no satisfactory option for severe malaria.

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