Palovarotene
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MedKoo CAT#: 319875

CAS#: 410528-02-8

Description: Palovarotene, also known as RO-3300074 and R-667, is a highly selective retinoic acid receptor gamma (RAR-γ) agonist that is under investigation as a potential treatment for emphysema. Phase I clinical trials of palovarotene in patients with emphysema demonstrated that the drug is well tolerated, with improvements observed in markers of emphysema progression. Emphysema is characterized by the destruction of alveoli and alveolar ducts within the lungs. Retinoid signaling is believed to play a role in alveologenesis, with the retinoic acid receptor gamma thought to be required for alveolar formation.


Price and Availability

Size Price Shipping out time Quantity
5mg USD 245 2 Weeks
10mg USD 415 2 Weeks
25mg USD 730 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-07-15. Prices are subject to change without notice.

Palovarotene, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 319875
Name: Palovarotene
CAS#: 410528-02-8
Chemical Formula: C27H30N2O2
Exact Mass: 414.2307
Molecular Weight: 414.549
Elemental Analysis: C, 78.23; H, 7.29; N, 6.76; O, 7.72


Synonym: RO-3300074; RO 3300074; RO3300074; R-667; R 667; R667; Palovarotene

IUPAC/Chemical Name: 4-((1E)-2-(5,5,8,8-Tetramethyl-3-(1H-pyrazol-1-ylmethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)ethenyl)benzoic acid

InChi Key: YTFHCXIPDIHOIA-DHZHZOJOSA-N

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+

SMILES Code: O=C(O)C1=CC=C(/C=C/C2=C(CN3N=CC=C3)C=C4C(C)(C)CCC(C)(C)C4=C2)C=C1


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001


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).