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PZ-2891

产品编号 T5185 CAS 2170608-82-7

PZ-2891 是可口服，能渗透血脑屏障的泛酸激酶调节剂。它抑制人泛酸激酶 PANK1β，PANK2 和 PANK3，IC50分别为 40.2 nM，0.7 nM 和 1.3 nM。它在高浓度下充当正构抑制剂，在较低亚饱和浓度下充当变构激活剂。

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PZ-2891, CAS 2170608-82-7

规格	价格/CNY	货期
1 mg	￥ 397	现货
2 mg	￥ 582	现货
5 mg	￥ 937	现货
10 mg	￥ 1,580	现货
25 mg	￥ 2,430	现货
50 mg	￥ 3,590	现货
100 mg	￥ 5,130	现货
1 mL * 10 mM (in DMSO)	￥ 995	现货

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	PZ-2891 is an orally bioavailable, brain penetrant pantothenate kinase (PANK) modulator(hPANK3,IC50:1.3 nM).
靶点活性	PANK1β (human):40.2±4.4 nM (IC50), PANK2 (human):0.7±0.08 nM (IC50), PANK3 (human):1.3±0.2 nM (IC50)
体内活性	Oral administration of PZ-2891 increases CoA levels in mouse liver and brain.?A knockout mouse model of brain CoA deficiency exhibited weight loss, severe locomotor impairment and early death.?Knockout mice on PZ-2891 therapy gain weight, and have improved locomotor activity and life span establishing pantazines as novel therapeutics for the treatment of PKAN.
动物实验	C57Bl6/J mice (8-week-old) ?pantothenic acid-supplemented diet (1000 ppm) for 2 weeks prior to the experiment.?The mice were maintained at room temperature 72° ± 2 °F, humidity 50 ± 10% and a 14 h light /10 h dark cycle with the dark cycle starting at 18:00 h. Water was supplied ad libitum.?The mice were randomized into the treatment arms to achieve a normal weight distribution.?PZ-2891 was formulated in 30% Captisol, and was administered by oral gavage at 12 h intervals for 5 doses.?The mice were euthanized and tissues harvested 4 h after the last dose.?The tissue samples were used for total CoA, pantothenate and pantazine determinations.?Blood was collected from euthanized animals, plasma or serum was prepared and stored frozen until analysis.?Organs, including liver, forebrain, and hindbrain were quickly excised from euthanized animals and immediately flash frozen in liquid N2 or immersed in RNAlater overnight prior to freezing.?Forebrain and hindbrain regions were identified.?Total CoA was determined using 20–50 mg of tissue (liver, forebrain or hindbrain) homogenized in 2 ml of 1 mM KOH.?The pH was adjusted to 12.0 with 0.25 M KOH, and incubated at 55 °C for 2 h.?The pH of the sample was adjusted to 8.0, and the samples were derivatized with monobromobimane (mBBr) and analyzed by HPLC equipped with a fluorescence detector

分子量	349.43
分子式	C20H23N5O
CAS No.	2170608-82-7

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 75 mg/mL (214.64 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.8618 mL	14.309 mL	28.618 mL	71.5451 mL
	5 mM	0.5724 mL	2.8618 mL	5.7236 mL	14.309 mL
	10 mM	0.2862 mL	1.4309 mL	2.8618 mL	7.1545 mL
	20 mM	0.1431 mL	0.7155 mL	1.4309 mL	3.5773 mL
	50 mM	0.0572 mL	0.2862 mL	0.5724 mL	1.4309 mL
	100 mM	0.0286 mL	0.1431 mL	0.2862 mL	0.7155 mL

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参考文献

1. Lalit, Kumar, Sharma, et al. A therapeutic approach to pantothenate kinase associated neurodegeneration.[J]. Nature communications, 2018.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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