Quazinone
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MedKoo CAT#: 471035

CAS#: 70018-51-8

Description: Quazinone, is a phosphodiesterase 3 (PDE3) inhibitor and novel cardiotonic agent with vasodilating properties.

Chemical Structure

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Quazinone
CAS# 70018-51-8
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 471035
Name: Quazinone
CAS#: 70018-51-8
Chemical Formula: C11H10ClN3O
Exact Mass: 235.05
Molecular Weight: 235.671
Elemental Analysis: C, 56.06; H, 4.28; Cl, 15.04; N, 17.83; O, 6.79

Price and Availability

Size Price Availability Quantity
10mg USD 250
25mg USD 480
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Synonym: Quazinone; Ro 13-6438

IUPAC/Chemical Name: (3R)-6-chloro-1,5-dihydro-3-methyl-imidazo[2,1-b]quinazolin-2(3H)-one

InChi Key: BHZFZYLBVSWUMT-ZCFIWIBFSA-N

InChi Code: InChI=1S/C11H10ClN3O/c1-6-10(16)14-11-13-9-4-2-3-8(12)7(9)5-15(6)11/h2-4,6H,5H2,1H3,(H,13,14,16)/t6-/m1/s1

SMILES Code: O=C1NC2=NC3=C(C(Cl)=CC=C3)CN2[C@@H]1C

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 and Ethanol

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO and Ethanol

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:
Product Data
Instruction:
View handling instruction
Biological target: Quazinone is a selective inhibitor of phosphodiesterase 3 (PDE3) with positive inotropic and vasodilating properties. It induces relaxation of precontracted isolated human cavernous smooth muscle. Quazinone increases myocardial contractile force in anesthetized open-chest dogs in a dose-dependent manner, as well as decreases systolic and diastolic blood pressure. It also inhibits DNA synthesis induced by the PDGF isoform PDGF-BB in bovine coronary artery smooth muscle cells in a concentration-dependent manner.
In vitro activity: Quazinone had potency at least equal to that of papaverine (a non-selective PDE inhibitor) and had a superior effect compared to Rolipram (a selective PDE IV inhibitor) and zaprinast (a selective PDE V inhibitor). The relaxation effect of PDE inhibitors was evaluated in an organ-bath study. This study provides the rationale and opens the possibility of using selective PDE inhibitors in the treatment of patients with erectile dysfunction. Reference: World J Urol. 1997;15(1):32-5. https://pubmed.ncbi.nlm.nih.gov/9066092/
In vivo activity: Quazinone increased tension development of isolated guinea pig left atria in a concentration-dependent manner with an EC50 of 30 microM, but had no stimulant effect on the spontaneous rate of right atria. In chronically instrumented, conscious dogs Quazinone increased myocardial contractility after administration of 0.03-0.3 mg/kg i.v. or 3-10 mg/kg p.o. The effects persisted for greater than 8 h after oral administration of 10 mg/kg. The inotropic effects were accompanied by a modest increase in heart rate. Reference: J Cardiovasc Pharmacol. 1984 May-Jun;6(3):511-9. https://pubmed.ncbi.nlm.nih.gov/6202980/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 5.0 21.22
Ethanol 1.0 4.24

Preparing Stock Solutions

The following data is based on the product molecular weight 235.67 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. Nazir M, Senkowski W, Nyberg F, Blom K, Edqvist PH, Jarvius M, Andersson C, Gustafsson MG, Nygren P, Larsson R, Fryknäs M. Targeting tumor cells based on Phosphodiesterase 3A expression. Exp Cell Res. 2017 Dec 15;361(2):308-315. doi: 10.1016/j.yexcr.2017.10.032. Epub 2017 Oct 26. PMID: 29107068. 2. Taher A, Meyer M, Stief CG, Jonas U, Forssmann WG. Cyclic nucleotide phosphodiesterase in human cavernous smooth muscle. World J Urol. 1997;15(1):32-5. doi: 10.1007/BF01275154. PMID: 9066092. 3. Braun S, Shargorodsky B, Talit U, Laniado S. Haemodynamic effects of Ro 13-6438, a new inotropic agent with vasodilating properties. Drugs Exp Clin Res. 1986;12(5):381-4. PMID: 3720522. 4. Eigenmann R, Gerold M, Holck M. Cardiovascular profile of Ro 13-6438, a novel positive inotropic agent with vasodilating properties. J Cardiovasc Pharmacol. 1984 May-Jun;6(3):511-9. doi: 10.1097/00005344-198405000-00021. PMID: 6202980.
In vitro protocol: 1. Nazir M, Senkowski W, Nyberg F, Blom K, Edqvist PH, Jarvius M, Andersson C, Gustafsson MG, Nygren P, Larsson R, Fryknäs M. Targeting tumor cells based on Phosphodiesterase 3A expression. Exp Cell Res. 2017 Dec 15;361(2):308-315. doi: 10.1016/j.yexcr.2017.10.032. Epub 2017 Oct 26. PMID: 29107068. 2. Taher A, Meyer M, Stief CG, Jonas U, Forssmann WG. Cyclic nucleotide phosphodiesterase in human cavernous smooth muscle. World J Urol. 1997;15(1):32-5. doi: 10.1007/BF01275154. PMID: 9066092.
In vivo protocol: 1. Braun S, Shargorodsky B, Talit U, Laniado S. Haemodynamic effects of Ro 13-6438, a new inotropic agent with vasodilating properties. Drugs Exp Clin Res. 1986;12(5):381-4. PMID: 3720522. 2. Eigenmann R, Gerold M, Holck M. Cardiovascular profile of Ro 13-6438, a novel positive inotropic agent with vasodilating properties. J Cardiovasc Pharmacol. 1984 May-Jun;6(3):511-9. doi: 10.1097/00005344-198405000-00021. PMID: 6202980.

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1. Lau, H. Y. A., et al.: Inflamm. Res., 54, S5-S6 (2005); Rickards, K. J., et al.: J. Vet. Pharmacol. Ther., 26, 277 (2003)

2. Osinski, M.T., and Schrör, K. Inhibition of platelet-derived growth factor-induced mitogenesis by phosphodiesterase 3 inhibitors: Role of protein kinase A in vascular smooth muscle cell mitogenesis. Biochem. Pharmacol. 60(3), 381-387 (2000).

3. Taher, A., Meyer, M., Stief, C.G., et al. Cyclic nucleotide phosphodiesterase in human cavernous smooth muscle. World J. Urol. 15(1), 32-35 (1997).

4. Eigenmann, R., Gerold, M., and Holck, M. Cardiovascular profile of Ro 13-6438, a novel positive inotropic agent with vasodilating properties. J. Cardiovasc. Pharmacol. 6(3), 511-519 (1984)