MedKoo Cat#: 526618 | Name: PWZ-029

Description:

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

PWZ-029 IS an inverse agonist selective for α₅ GABAA receptors with nootropic effects. PWZ-029 improves object recognition, but not water-maze memory in normal and scopolamine-treated rats. PWZ-029 acts as a subtype-selective, mixed agonist-inverse agonist at the benzodiazepine binding site on the GABAA receptor, acting as a partial inverse agonist at the α5 subtype and a weak partial agonist at the α3 subtype. This gives it a mixed pharmacological profile, producing at low doses memory-enhancing effects but with no convulsant or anxiogenic effects or muscle weakness, although at higher doses it produces some sedative effects

Chemical Structure

PWZ-029
PWZ-029
CAS#164025-33-6

Theoretical Analysis

MedKoo Cat#: 526618

Name: PWZ-029

CAS#: 164025-33-6

Chemical Formula: C14H14ClN3O2

Exact Mass: 291.0775

Molecular Weight: 291.74

Elemental Analysis: C, 57.64; H, 4.84; Cl, 12.15; N, 14.40; O, 10.97

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
Synonym
PWZ-029; PWZ 029; PWZ029.
IUPAC/Chemical Name
8-chloro-3-(methoxymethyl)-5-methyl-4H-imidazo[1,5-a][1,4]benzodiazepin-6-one
InChi Key
FXIDXTIMKAEBGY-UHFFFAOYSA-N
InChi Code
InChI=1S/C14H14ClN3O2/c1-17-6-13-11(7-20-2)16-8-18(13)12-4-3-9(15)5-10(12)14(17)19/h3-5,8H,6-7H2,1-2H3
SMILES Code
O=C1N(C)CC2=C(COC)N=CN2C3=CC=C(Cl)C=C13
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, not in water
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

Preparing Stock Solutions

The following data is based on the product molecular weight 291.74 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
1: Clayton T, Poe MM, Rallapalli S, Biawat P, Savić MM, Rowlett JK, Gallos G, Emala CW, Kaczorowski CC, Stafford DC, Arnold LA, Cook JM. A Review of the Updated Pharmacophore for the Alpha 5 GABA(A) Benzodiazepine Receptor Model. Int J Med Chem. 2015;2015:430248. doi: 10.1155/2015/430248. Epub 2015 Nov 10. Review. PubMed PMID: 26682068; PubMed Central PMCID: PMC4657098. 2: Timić Stamenić T, Joksimović S, Biawat P, Stanković T, Marković B, Cook JM, Savić MM. Negative modulation of α₅ GABAA receptors in rats may partially prevent memory impairment induced by MK-801, but not amphetamine- or MK-801-elicited hyperlocomotion. J Psychopharmacol. 2015 Sep;29(9):1013-24. doi: 10.1177/0269881115590601. Epub 2015 Jun 23. PubMed PMID: 26105958. 3: Martínez-Cué C, Delatour B, Potier MC. Treating enhanced GABAergic inhibition in Down syndrome: use of GABA α5-selective inverse agonists. Neurosci Biobehav Rev. 2014 Oct;46 Pt 2:218-27. doi: 10.1016/j.neubiorev.2013.12.008. Epub 2014 Jan 9. Review. PubMed PMID: 24412222. 4: Soto PL, Ator NA, Rallapalli SK, Biawat P, Clayton T, Cook JM, Weed MR. Allosteric modulation of GABA(A) receptor subtypes:effects on visual recognition and visuospatial working memory in rhesus monkeys [corrected]. Neuropsychopharmacology. 2013 Oct;38(11):2315-25. doi: 10.1038/npp.2013.137. Epub 2013 May 31. Erratum in: Neuropsychopharmacology. 2013 Nov;38(12):2553. PubMed PMID: 23722241; PubMed Central PMCID: PMC3773684. 5: Milić M, Timić T, Joksimović S, Biawat P, Rallapalli S, Divljaković J, Radulović T, Cook JM, Savić MM. PWZ-029, an inverse agonist selective for α₅ GABAA receptors, improves object recognition, but not water-maze memory in normal and scopolamine-treated rats. Behav Brain Res. 2013 Mar 15;241:206-13. doi: 10.1016/j.bbr.2012.12.016. Epub 2012 Dec 20. PubMed PMID: 23261875; PubMed Central PMCID: PMC3556169. 6: Savić MM, Clayton T, Furtmüller R, Gavrilović I, Samardzić J, Savić S, Huck S, Sieghart W, Cook JM. PWZ-029, a compound with moderate inverse agonist functional selectivity at GABA(A) receptors containing alpha5 subunits, improves passive, but not active, avoidance learning in rats. Brain Res. 2008 May 7;1208:150-9. doi: 10.1016/j.brainres.2008.02.020. Epub 2008 Feb 19. PubMed PMID: 18394590; PubMed Central PMCID: PMC2577822.