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Size | Price | Stock |
---|---|---|
5mg | $95 | 3-6 Days |
10mg | $140 | 3-6 Days |
25mg | $240 | 3-6 Days |
50mg | $415 | 3-6 Days |
100mg | $650 | 3-6 Days |
250mg | $1080 | 3-6 Days |
500mg | $1750 | 3-6 Days |
Cat #: V3311 CAS #: 2170608-82-7 Purity ≥ 98%
Description: PZ-2891 (PZ2891) is an orally bioavailable, and brain penetrant allosteric activator of Pantothenate kinase (PANK) with neuroprotective activity. It acts as both an orthosteric inhibitor with IC50 of 1.3 nM and an allosteric activator of PANK3 in the presence of acetyl-CoA in biochemical assays. 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). PZ-2891 occupies the pantothenate pocket and engages the dimer interface to form a PANK•ATP•Mg2+•PZ-2891 complex. The binding of PZ-2891 to one protomer locks the opposite protomer in a catalytically active conformation that is refractory to acetyl-CoA inhibition. 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.
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Molecular Weight (MW) | 349.44 |
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Molecular Formula | C20H23N5O |
CAS No. | 2170608-82-7 |
Storage | -20℃ for 3 years in powder form |
-80℃ for 2 years in solvent | |
Solubility In Vitro | DMSO: 10mM |
Water: N/A | |
Ethanol: N/A | |
SMILES Code | N#CC1=NN=C(N2CCN(C(CC3=CC=C(C(C)C)C=C3)=O)CC2)C=C1 |
Synonyms | PZ2891; PZ 2891; PZ-2891 |
Solvent volume to be added | Mass (the weight of a compound) | |||
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Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 2.8617 mL | 14.3086 mL | 28.6172 mL | 57.2344 mL |
5mM | 0.5723 mL | 2.8617 mL | 5.7234 mL | 11.4469 mL |
10mM | 0.2862 mL | 1.4309 mL | 2.8617 mL | 5.7234 mL |
20mM | 0.1431 mL | 0.7154 mL | 1.4309 mL | 2.8617 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.