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Z3003

Zardaverine

Name: Zardaverine
Brand: SIGMA

phosphodiesterase inhibitor

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Synonym(s):

6-(4-Difluoromethoxy-3-methoxyphenyl)-3(2H)-pyridazinone

Empirical Formula (Hill Notation):

C₁₂H₁₀F₂N₂O₃

CAS Number:

101975-10-4

Molecular Weight:

268.22

MDL number:

MFCD00867059

PubChem Substance ID:

24278784

NACRES:

NA.77

biological source

synthetic (organic)

Assay

≥98% (HPLC)

form

powder

potency

1.1 μM IC₅₀ (for PDE IV)
2.5 μM IC₅₀ (for PDE III)

SMILES string

COc1cc(ccc1OC(F)F)C2=NNC(=O)C=C2

InChI

1S/C12H10F2N2O3/c1-18-10-6-7(2-4-9(10)19-12(13)14)8-3-5-11(17)16-15-8/h2-6,12H,1H3,(H,16,17)

InChI key

HJMQDJPMQIHLPB-UHFFFAOYSA-N

Gene Information

human ... PDE3A(5139) , PDE3B(5140) , PDE4A(5141) , PDE4B(5142) , PDE4C(5143) , PDE4D(5144) , PDE5A(8654) , PDE7A(5150)
rat ... Pde2a(81743) , Pde4a(25638)

Application

Zardaverine has been used as a phosphodiesterase inhibitor:

to study its effects on human colonic epithelial cells
to study its effects on junctional proteins in Sertoli cells
to study its effects on phosphodiesterase 3 A (PDE3A) expression in various tumor cells

Biochem/physiol Actions

Zardaverine is a derivative of pyridazinone. It shows anti-tumor and anti-proliferative activity in varied cell lines. Zardaverine possesses broncho-dilatory activity and exhibits therapeutic effects against asthma.

Selective inhibitor of phosphodiesterase III/IV (PDE3/4).

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Personal Protective Equipment

dust mask type N95 (US), Eyeshields, Gloves

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Design of small-sized libraries by combinatorial assembly of linkers and functional groups to a given scaffold: application to the structure-based optimization of a phosphodiesterase 4 inhibitor.

Mireille Krier et al.

Journal of medicinal chemistry, 48(11), 3816-3822 (2005-05-27)

Combinatorial chemistry and library design have been reconciled by applying simple medicinal chemistry concepts to virtual library design. The herein reported "Scaffold-Linker-Functional Group" (SLF) approach has the aim to maximize diversity while minimizing the size of a scaffold-focused library with

Sertoli cell junctional proteins as early targets for different classes of reproductive toxicants.

Céline Fiorini et al.

Reproductive toxicology (Elmsford, N.Y.), 18(3), 413-421 (2004-04-15)

In the testis, Sertoli cells establish intercellular junctions that are essential for spermatogenesis. The SerW3 Sertoli cell line displays some features of native Sertoli cells. Western blot and immunofluorescence analyses showed that SerW3 Sertoli cells expressed typical components of tight

The effect of selective and non-selective phosphodiesterase inhibitors on allergen- and leukotriene C(4)-induced contractions in passively sensitized human airways.

D T Schmidt et al.

British journal of pharmacology, 131(8), 1607-1618 (2001-01-05)

Non-selective inhibitors of cyclic nucleotide phosphodiesterase (PDE) block allergen-induced contraction of passively sensitized human airways in vitro by a dual mechanism involving a direct relaxant effect on smooth muscle and inhibition of histamine and cysteinyl leukotriene (LT) release from airways.

Identification of PDE isozymes in human pulmonary artery and effect of selective PDE inhibitors.

K F Rabe et al.

The American journal of physiology, 266(5 Pt 1), L536-L543 (1994-05-01)

The effects of the nonselective phosphodiesterase (PDE) inhibitor 3-isobutyl-1-methylxanthine (IBMX) and the selective PDE inhibitors motapizone (type III), rolipram (type IV), zardaverine (type III/IV), and zaprinast (type V and I) on prostaglandin F2 alpha (PFG2 alpha)-induced tone in human pulmonary

Differential effects of non-selective and selective phosphodiesterase inhibitors on human eosinophil functions.

A Hatzelmann et al.

British journal of pharmacology, 114(4), 821-831 (1995-02-01)

1. The effect of non-selective (3-isobutyl-1-methylxanthine, IBMX; theophylline) and type IV- or type III/IV-selective (rolipram, RP 73401; zardaverine, tolafentrine) phosphodiesterase (PDE) inhibitors on human eosinophil functions was investigated. 2. For this purpose human eosinophils were purified from blood of healthy

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