An orally bioavailable RARγ agonist; increases RARE activity and decreases IL-1β-induced NF-κB activity in primary mouse stromal cells at 60 nM; inhibits activin A-induced chondrogenic and osteogenic differentiation of mouse FAPs expressing ACVR1R206H at 10 nM; inhibits heterotopic ossification and preserves limb movement and growth in a ACVR1R206H FOP mouse model; decreases heterotopic ossification by 50 to 60% in a rat model of traumatic blast injury at 1 mg/kg per day for 14 days

Palovarotene – 5 mg

Brand:
Cayman
CAS:
410528-02-8
Storage:
-20
UN-No:
Non-Hazardous - /

Palovarotene an orally bioavailable retinoic acid receptor γ (RARγ) agonist.{48611} 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.{48612} 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 (ACVR1R206H).{48613} It inhibits heterotopic ossification and preserves limb movement and growth in a ACVR1R206H fibrodysplasia ossificans progressiva (FOP) mouse model.{48614} Palovarotene (1 mg/kg per day for 14 days) decreases heterotopic ossification by 50 to 60% in a rat model of traumatic blast injury.{48615}  

 

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SKU: 28460 - 5 mg Category:

Description

An orally bioavailable RARγ agonist; increases RARE activity and decreases IL-1β-induced NF-κB activity in primary mouse stromal cells at 60 nM; inhibits activin A-induced chondrogenic and osteogenic differentiation of mouse FAPs expressing ACVR1R206H at 10 nM; inhibits heterotopic ossification and preserves limb movement and growth in a ACVR1R206H FOP mouse model; decreases heterotopic ossification by 50 to 60% in a rat model of traumatic blast injury at 1 mg/kg per day for 14 days

Formal name: 4-[(1E)-2-[5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-3-(1H-pyrazol-1-ylmethyl)-2-naphthalenyl]ethenyl]-benzoic acid

Synonyms:  Ro 3300074

Molecular weight: 414.5

CAS: 410528-02-8

Purity: ≥98%

Formulation: A solid

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