PZ-II-029
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 530932

CAS#: 164025-44-9

Description: PZ-II-029 is a α6β3γ2-selective GABAA channel modulator.


Chemical Structure

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PZ-II-029
CAS# 164025-44-9

Theoretical Analysis

MedKoo Cat#: 530932
Name: PZ-II-029
CAS#: 164025-44-9
Chemical Formula: C18H15N3O3
Exact Mass: 321.11
Molecular Weight: 321.340
Elemental Analysis: C, 67.28; H, 4.71; N, 13.08; O, 14.94

Price and Availability

Size Price Availability Quantity
25mg USD 750 2 Weeks
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Synonym: PZ-II-029; PZII-029; PZ II-029; PZ-II029; PZII029; PZ II029;

IUPAC/Chemical Name: 2,5-Dihydro-7-methoxy-2-(4-methoxyphenyl)-3H-pyrazolo[4,3-c]quinolin-3-one

InChi Key: IPYGULVOAIXELM-UHFFFAOYSA-N

InChi Code: InChI=1S/C18H15N3O3/c1-23-12-5-3-11(4-6-12)21-18(22)15-10-19-16-9-13(24-2)7-8-14(16)17(15)20-21/h3-10,19H,1-2H3

SMILES Code: O=C1N(C2=CC=C(OC)C=C2)N=C3C1=CNC4=C3C=CC(OC)=C4

Appearance: Solid powder

Purity: >98% (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: >2 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:

Product Data:
Biological target: PZ-II-029 is a specific postitive modulator of GABAA channels composed of α6β3γ2 subunits.
In vitro activity: To be determined
In vivo activity: In male Sprague-Dawley rats, PZ-II-029 and its deuterated analogues are not prone to untoward interactions with benzodiazepines and may indeed completely abolish their ataxic action, seen at therapeutic, and especially toxic concentrations. They showed a safe behavioral profile and prevented the ataxic effects of benzodiazepines like diazepam, suggesting their potential to counteract such effects at therapeutic and potentially toxic concentrations. Reference: Basic Clin Pharmacol Toxicol. 2022 Dec;131(6):514-524. https://pubmed.ncbi.nlm.nih.gov/36180380/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 10.0 31.12

Preparing Stock Solutions

The following data is based on the product molecular weight 321.34 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.

Recalculate based on batch purity %
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. Divović Matović B, Knutson D, Mitrović J, Stevanović V, Stanojević B, Savić S, Cook JM, Savić MM. Behavioural interaction of pyrazoloquinolinone positive allosteric modulators at α6GABAA receptors and diazepam in rats: Anti-diazepam-induced ataxia action as a structure-dependent feature. Basic Clin Pharmacol Toxicol. 2022 Dec;131(6):514-524. doi: 10.1111/bcpt.13801. Epub 2022 Oct 8. PMID: 36180380.
In vitro protocol: To be determined
In vivo protocol: 1. Divović Matović B, Knutson D, Mitrović J, Stevanović V, Stanojević B, Savić S, Cook JM, Savić MM. Behavioural interaction of pyrazoloquinolinone positive allosteric modulators at α6GABAA receptors and diazepam in rats: Anti-diazepam-induced ataxia action as a structure-dependent feature. Basic Clin Pharmacol Toxicol. 2022 Dec;131(6):514-524. doi: 10.1111/bcpt.13801. Epub 2022 Oct 8. PMID: 36180380.

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Varagic et al (2013) Subtype selectivity of α+β- site ligands of GABAA receptors: identification of the first highly specific positive modulators at α6β2/3γ2 receptors. Br.J.Pharmacol. 169 384 PMID: 23472935