A RARγ agonist
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Palovarotene

Item No. 28460

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
CAS Number
410528-02-8
Synonyms
  • Ro 3300074
Molecular Formula
C27H30N2O2
Formula Weight
414.5
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 20 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.3 mg/mlEthanol: 3 mg/ml
λmax
321 nm
SMILES
CC1(C)CCC(C)(C)C2=C1C=C(CN3C=CC=N3)C(/C=C/C4=CC=C(C(O)=O)C=C4)=C2
InChi Code
InChI=1S/C27H30N2O2/c1-26(2)12-13-27(3,4)24-17-22(18-29-15-5-14-28-29)21(16-23(24)26)11-8-19-6-9-20(10-7-19)25(30)31/h5-11,14-17H,12-13,18H2,1-4H3,(H,30,31)/b11-8+
InChi Key
YTFHCXIPDIHOIA-DHZHZOJOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $90

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    10 mg

    $168

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    25 mg

    $370

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    Product Description

    Palovarotene an orally bioavailable retinoic acid receptor γ (RARγ) agonist.1 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.2 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).3 It inhibits heterotopic ossification and preserves limb movement and growth in a ACVR1R206H fibrodysplasia ossificans progressiva (FOP) mouse model.4 Palovarotene (1 mg/kg per day for 14 days) decreases heterotopic ossification by 50 to 60% in a rat model of traumatic blast injury.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hind, M., and Stinchcombe, S. Palovarotene, a novel retinoic acid receptor gamma agonist for the treatment of emphysema. Curr. Opin. Investig. Drugs 10(11), 1243-1250 (2009).

    2. Sinha, S., Uchibe, K., Usami, Y., et al. Effectiveness and mode of action of a combination therapy for heterotopic ossification with a retinoid agonist and an anti-inflammatory agent. Bone 90, 59-68 (2016).

    3. Lees-Shepard, J.B., Nicholas, S.-A.E., Stoessel, S.J., et al. Palovarotene reduces heterotopic ossification in juvenile FOP mice but exhibits pronounced skeletal toxicity. Elife 7, e40814 (2018).

    4. Chakkalakal, S.A., Uchibe, K., Convente, M.R., et al. Palovarotene inhibits heterotopic ossification and maintains limb mobility and growth in mice with the human ACVR1R206H fibrodysplasia ossificans progressiva (FOP) mutation. J. Bone Miner. Res. 31(9), 1666-1675 (2016).

    5. Pavey, G.J., Qureshi, A.T., Tomasino, A.M., et al. Targeted stimulation of retinoic acid receptor-γ mitigates the formation of heterotopic ossification in an established blast-related traumatic injury model. Bone 90, 159-167 (2016).