PZ-2891 | CAS#2170608-82-7 | PANK modulator

MedKoo Cat#: 555470 | Name: PZ-2891

Description:

WARNING: This product is for research use only, not for human or veterinary use.

PZ-2891 is a potent and selective, orally active Pantothenate kinase (PANK) modulator, acting as both an orthosteric inhibitor (IC50=1.3 nM, hPANK3) and an allosteric activator of PANK3 activity in the presence of acetyl-CoA in biochemical assays.

Chemical Structure

PZ-2891

CAS#2170608-82-7

Theoretical Analysis

MedKoo Cat#: 555470

Name: PZ-2891

CAS#: 2170608-82-7

Chemical Formula: C20H23N5O

Exact Mass: 349.1903

Molecular Weight: 349.44

Elemental Analysis: C, 68.74; H, 6.63; N, 20.04; O, 4.58

Price and Availability

Size	Price	Availability
5mg	USD 90.00	Ready to Ship
10mg	USD 150.00	Ready to ship
25mg	USD 250.00	Ready to ship
50mg	USD 425.00	Ready to ship
100mg	USD 750.00	Ready to ship
200mg	USD 1,350.00	Ready to ship
500mg	USD 2,950.00	Ready to ship
1g	USD 4,650.00	2 Weeks

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Related CAS #

No Data

Synonym

PZ-2891; PZ 2891; PZ2891;

IUPAC/Chemical Name

6-(4-(2-(4-isopropylphenyl)acetyl)piperazin-1-yl)pyridazine-3-carbonitrile

InChi Key

LGWDVWIZDPGCFG-UHFFFAOYSA-N

InChi Code

InChI=1S/C20H23N5O/c1-15(2)17-5-3-16(4-6-17)13-20(26)25-11-9-24(10-12-25)19-8-7-18(14-21)22-23-19/h3-8,15H,9-13H2,1-2H3

SMILES Code

N#CC1=NN=C(N2CCN(C(CC3=CC=C(C(C)C)C=C3)=O)CC2)C=C1

Appearance

Solid powder

Purity

>97% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Pantothenate kinase (PANK) is a metabolic enzyme that regulates cellular coenzyme A (CoA) levels. There are three human PANK genes, and inactivating mutations in PANK2 lead to pantothenate kinase associated neurodegeneration (PKAN)

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#T9Z04C27

QC Data

View QC data: current batch, Lot#T9Z04C27

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

PZ-2891 inhibits human pantothenate kinases PANK1β, PANK2, and PANK3 with IC50s of 40.2 nM, 0.7 nM and 1.3 nM, respectively.

In vitro activity:

To be determined

In vivo activity:

PZ-2891 demonstrated promising therapeutic potential for pantothenate kinase-associated neurodegeneration (PKAN) in a mouse model. Oral administration of PZ-2891 increased CoA levels in the liver and the brain. PZ-2891 treatment ameliorated severe symptoms associated with brain CoA deficiency, including weight loss and locomotor impairment, ultimately leading to improved overall health and extended lifespan in the treated mice. Reference: Nat Commun. 2018 Oct 23;9(1):4399. https://pubmed.ncbi.nlm.nih.gov/30352999/

	Solvent	mg/mL	mM
Solubility
	DMSO	75.0	214.64

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 349.44 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Simão-Gurge RM, Thakre N, Strickland J, Isoe J, Delacruz LR, Torrevillas BK, Rodriguez AM, Riehle MA, Luckhart S. Activation of Anopheles stephensi Pantothenate Kinase and Coenzyme A Biosynthesis Reduces Infection with Diverse Plasmodium Species in the Mosquito Host. Biomolecules. 2021 May 29;11(6):807. doi: 10.3390/biom11060807. PMID: 34072373; PMCID: PMC8228300. 2. Sharma LK, Subramanian C, Yun MK, Frank MW, White SW, Rock CO, Lee RE, Jackowski S. A therapeutic approach to pantothenate kinase associated neurodegeneration. Nat Commun. 2018 Oct 23;9(1):4399. doi: 10.1038/s41467-018-06703-2. PMID: 30352999; PMCID: PMC6199309.

In vitro protocol:

To be determined

In vivo protocol:

1: Sharma LK, Subramanian C, Yun MK, Frank MW, White SW, Rock CO, Lee RE, Jackowski S. A therapeutic approach to pantothenate kinase associated neurodegeneration. Nat Commun. 2018 Oct 23;9(1):4399. doi: 10.1038/s41467-018-06703-2. PubMed PMID: 30352999; PubMed Central PMCID: PMC6199309.