7-Methyl-5-[(3-piperazin-1-ylMethyl)-1,2,4-oxadiazol-5-yl-]-2-[4-(trifluoroMethoxy)benzyl]-2,3-dihydro-1H-isoindol-1-one Methanesulphonate Property

Boiling point:

676.8±55.0 °C(Predicted)

Density 

1.37±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

insoluble in H2O; insoluble in EtOH; ≥19.8 mg/mL in DMSO

form 

solid

pka

4.06±0.10(Predicted)

color 

White to gray

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

7-Methyl-5-[(3-piperazin-1-ylMethyl)-1,2,4-oxadiazol-5-yl-]-2-[4-(trifluoroMethoxy)benzyl]-2,3-dihydro-1H-isoindol-1-one Methanesulphonate Chemical Properties,Usage,Production

Uses

AZD 1981 is an orally available selective DP2 antagonist in the treatment of asthma.

Biological Activity

azd1981 is a selective, orally bioavailable and potent antagonist of the chemoattractant receptor-homologous expressed on th2 lymphocytes receptor (crth2 or dp2) with an ic50 value of 4 nm [1].azd1981 has shown to inhibit eosinophil migration with a pic50 value of 7.6±0.1. azd1981 could block chemotaxis of dp2+ t-cell lines with a pic50 value of 7.5±0.1. azd1981 has been demonstrated to inhibit pgd2 binding to mouse, rat, rabbit, dog, guinea pig and human dp2. azd1981 could inhibit shape change induced by dp2 in dog and guinea pig granulocytes as well as in human eosinophils and basophils in blood [2].

References

[1] luker t1, bonnert r, brough s, cook ar, dickinson mr, dougall i, logan c, mohammed rt, paine s, sanganee hj, sargent c, schmidt ja,teague s, thom s. substituted indole-1-acetic acids as potent and selective crth2 antagonists-discovery of azd1981. bioorg med chem lett. 2011 nov 1;21(21):6288-92.
[2] schmidt ja1, bell fm, akam e, marshall c, dainty ia, heinemann a, dougall ig, bonnert rv, sargent ca. biochemical and pharmacological characterization of azd1981, an orally available selective dp2 antagonist in clinical development for asthma. br j pharmacol. 2013 apr;168(7):1626-38.