Unii-950o97nupo Property

Density 

1.47±0.1 g/cm3(Predicted)

storage temp. 

-20°

solubility 

Soluble in DMSO (up to 5 mg/ml with warming).

form 

solid

pka

6.42±0.40(Predicted)

color 

Beige

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H319Causes serious eye irritation

H361Suspected of damaging fertility or the unborn child

H372Causes damage to organs through prolonged or repeated exposure

H410Very toxic to aquatic life with long lasting effects

Precautionary statements

P201Obtain special instructions before use.

P202Do not handle until all safety precautions have been read and understood.

P260Do not breathe 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.

P273Avoid release to the environment.

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

P281Use personal protective equipment as required.

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

P308+P313IF exposed or concerned: Get medical advice/attention.

P314Get medical advice/attention if you feel unwell.

P391Collect spillage. Hazardous to the aquatic environment

P405Store locked up.

P501Dispose of contents/container to..…

Unii-950o97nupo Chemical Properties,Usage,Production

Description

Preladenant is an orally bioavailable antagonist of the adenosine A_2A receptor (K_is = 1.1 and 2.5 nM for human and rat receptors, respectively). It is selective for A_2A receptors over A₁, A_2B, and A₃ receptors (K_is = >1,000, >1,700, and >1,000 nM, respectively) as well as a panel of 59 receptors, enzymes, and ion channels. Preladenant inhibits adenylate cyclase activity (K_bs = 1.3 and 0.7 nM for human and rat receptors, respectively) induced by the A_2A receptor agonist CGS 21680 . It inhibits catalepsy induced by haloperidol in rats by 77 and 70% after 1 and 4 hours, respectively, when administered at a dose of 1 mg/kg. Preladenant also increases the efficacy of L-DOPA when used in combination with eltoprazine in a 6-OHDA rat lesion model of Parkinson’s disease dyskinesia.

Uses

A potent and selective antagonist at the adenosine A2A receptor. It is being researched as a potential treatment for Parkinson''s disease.

target

adenosine A2A receptor

References

1)?Hodgson?et al.?(2009), Characterization of the potent and selective A2A receptor antagonists preladenant and SCH 412348 [7-[2-[4-2,4-difluorophenyl]-1-piperazinyl]ethyl]-2-(2-furanyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimodin-5-amine] in rat models of movement disorders and depression;?J.Pharmacol.Exp.Ther.?330294 2)?Hodgson?et al.?(2010), Preladenant, a selective A(2A) receptor antagonist, is active in primate models of movement disorders;?Exp.Neurol.?225384 3)?Pinna?et al.?(2016), Antidyskinetic effect of A2A and 5HT1A/B receptor ligands in two animal models of Parkinson’s disease;?Mov.Disord.?31501 4)?Beavis?et al.?(2013), Blockade of A2A receptors potently suppresses the metastasis of CD73+ tumors;?Proc.Natl.Acad.Sci USA.?11014711 5)?Hatfield and Sitkovsky (2016), A2A adenosine receptor antagonist to weaken the hypoxia-HIF-1a driven immunosuppression and improve immunotherapies of cancer;?Curr.Opin.Pharmacol.?2990 6)?Ohta?et al.?(2016), A metabolic immune checkpoint: adenosine in the tumor microenvironment;?Front.Immunol.?71 7)?NCT03099161