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Zaprinast

Zaprinast structure

CAS No:
37762-06-4
Formula:
C13H13N5O2
Chemical Name:
Zaprinast
Synonyms:
7H-1,2,3-Triazolo[4,5-d]pyrimidin-7-one,3,6-dihydro-5-(2-propoxyphenyl)-;7H-1,2,3-Triazolo[4,5-d]pyrimidin-7-one,1,4-dihydro-5-(2-propoxyphenyl)-;3,6-Dihydro-5-(2-propoxyphenyl)-7H-1,2,3-triazolo[4,5-d]pyrimidin-7-one;8-Aza-2-(2-propoxyphenyl)-6-purinone;2-(o-Propoxyphenyl)-8-azapurin-6-one;M&B 22,948;M and B 22948;Zaprinast;2-(2-Propoxyphenyl)-8-aza-6-purinone;5-(2-Propoxyphenyl)-1H-[1,2,3]triazolo[4,5-d]pyrimidin-7(4H)-one;M&B 22948;55122-20-8;68560-67-8
Categories:
Active Pharmaceutical Ingredients > Antiallergic Drugs

Description

Zaprinast (M&B 22948) is an inhibitor of cGMP-selective Phosphodiesterases(PDEs)[1]. Zaprinast is a G protein-coupled receptor (GPR) 35 agonist which activates rat GPR35 strongly and activates human GPR35 moderately[2]. Zaprinast reduces vessel remodeling through antiproliferative and proapoptotic effects[3].

5-(2-propoxyphenyl)-2,3-dihydrotriazolo[4,5-d]pyrimidin-7-one is a member of triazolopyrimidines.

Zaprinast Basic Attributes

Molecular Weight：

271.27

Exact Mass：

271.27

EC Number：

253-655-1

UNII：

GXT25D5DS0

NSC Number：

757885

DSSTox ID：

DTXSID8045224

Characteristics

PSA：

87.4

XLogP3：

0.17

Appearance：

white solid

Density：

1.484g/cm3

Melting Point：

241 °C (decomp)

Boiling Point：

406.3±47.0 °C at 760 mmHg

Flash Point：

199.5±29.3 °C

Refractive Index：

1.719

Water Solubility：

soluble to 100 mM in DMSO;45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: 0.11 mg/mL

Storage Conditions：

Store at RT

Collision Cross Section：

159.2 Å² [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

Safety Information

Transport codes：

NONH for all modes of transport

wgk germany：

hazard class code：

36/37/38

safety instructions：

26-36

RTECS Number：

XZ6157358

Marks：

Precautionary statement(s)：

P261-P305 + P351 + P338

Hazard Statements：

H315-H319-H335

GHS Classification：

|Warning|H315 (100%): Causes skin irritation [Warning Skin corrosion/irritation]|P261, P264, P271, P280, P302+P352, P304+P340, P305+P351+P338, P312, P321, P332+P313, P337+P313, P362, P403+P233, P405, and P501|Aggregated GHS information provided by 38 companies from 1 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

MeSH：

Compounds which inhibit or antagonize the biosynthesis or actions of phosphodiesterases. (See all compounds classified as Phosphodiesterase Inhibitors.)

MeSH Entry Terms：

2-(2-propoxyphenyl)-8-azapurin-6-one

Zaprinast Use and Manufacturing

A selective inhibitor of cyclic-GMP phosphodiesterase (PDE V, calmodulin insensitive). Since cGMP mediates the vasorelaxant action of nitric oxide, as well as the natriuretic and diuretic effect of atrial natriuretic factor (ANF) through the activation of PKG (cGMP dependent protein kinase), such inhibitors may display vasodilating, relaxant, and diuretic effects.These compounds may prove useful in treating hypertension and congestive heart failure.

Computed Properties

Molecular Weight:271.27
XLogP3:1.6
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:5
Rotatable Bond Count:4
Exact Mass:271.10692467
Monoisotopic Mass:271.10692467
Topological Polar Surface Area:92.3
Heavy Atom Count:20
Complexity:400
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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Zaprinast

CAS No.: 37762-06-4

Content: 98%

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