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PZ-2891

Name: PZ-2891
Brand: TargetMol
SKU: T5185
Price: 34 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T5185Cas No. 2170608-82-7

PZ-2891 is an orally bioavailable, brain-penetrant pantothenate kinase (PANK) modulator, with an IC50 of 1.3 nM for hPANK3.

PZ-2891

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Purity: 97.16%

Catalog No. T5185Cas No. 2170608-82-7

PZ-2891 is an orally bioavailable, brain-penetrant pantothenate kinase (PANK) modulator, with an IC50 of 1.3 nM for hPANK3.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$34	-	In Stock
2 mg	$48	-	In Stock
5 mg	$80	-	In Stock
10 mg	$122	-	In Stock
25 mg	$222	-	In Stock
50 mg	$369	-	In Stock
100 mg	$549	-	In Stock
1 mL x 10 mM (in DMSO)	$89	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:97.16%

Appearance:Solid

Color:White

Resource Download

COA LCMS HNMR

Product Introduction

Bioactivity

Description	PZ-2891 is an orally bioavailable, brain-penetrant pantothenate kinase (PANK) modulator, with an IC50 of 1.3 nM for hPANK3.
Targets&IC50	PANK2 (human):0.7±0.08 nM (IC50), PANK3 (human):1.3±0.2 nM (IC50), PANK1β (human):40.2±4.4 nM (IC50)
In vivo	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.
Animal Research	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

Chemical Properties

Molecular Weight	349.43
Formula	C₂₀H₂₃N₅O
Cas No.	2170608-82-7
Smiles	CC(C)c1ccc(CC(=O)N2CCN(CC2)c2ccc(nn2)C#N)cc1
Relative Density.	1.23 g/cm3 (Predicted)

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 75 mg/mL (214.64 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Corn Oil: 3.3 mg/mL (9.44 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.8618 mL	14.3090 mL	28.6180 mL	143.0902 mL
5 mM	0.5724 mL	2.8618 mL	5.7236 mL	28.6180 mL
10 mM	0.2862 mL	1.4309 mL	2.8618 mL	14.3090 mL
20 mM	0.1431 mL	0.7155 mL	1.4309 mL	7.1545 mL
50 mM	0.0572 mL	0.2862 mL	0.5724 mL	2.8618 mL
100 mM	0.0286 mL	0.1431 mL	0.2862 mL	1.4309 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc