palovarotene Chemical Properties

Melting point:

249-252°C

Boiling point:

592.3±50.0 °C(Predicted)

Density 

1.11

storage temp. 

Refrigerator

solubility 

DMSO (Slightly), Ethyl Acetate (Slightly, Heated), Methanol (Slightly, Heated)

pka

4.26±0.10(Predicted)

form 

Solid

color 

White to Off-White

palovarotene Usage And Synthesis

Description

Palovarotene an orally bioavailable retinoic acid receptor γ (RARγ) agonist. It increases retinoic acid response element (RARE) activity and decreases NF-κB activity induced by IL-1β in primary mouse stromal cells in reporter assays when used at a concentration of 60 nM. Palovarotene (10 nM) inhibits activin A-induced chondrogenic and osteogenic differentiation of mouse fibro/adipogenic progenitors (FAPs) expressing a mutated form of human activin A receptor type I (ACVR1^R206H). It inhibits heterotopic ossification and preserves limb movement and growth in a ACVR1^R206H fibrodysplasia ossificans progressiva (FOP) mouse model. Palovarotene (1 mg/kg per day for 14 days) decreases heterotopic ossification by 50 to 60% in a rat model of traumatic blast injury.

Uses

Palovarotene, is a highly selective retinoic acid receptor gamma (RAR-γ) agonist that is under investigation as a potential treatment for emphysema.

Definition

ChEBI: Palovarotene is a stilbenoid.

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