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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Purity: ≥98%
Palovarotene (formerly RO-3300074; R-667; Sohonos) is a novel, potent and highly selective retinoic acid receptor gamma (RAR-γ) agonist that is being investigated as a potential treatment for emphysema. Palovarotene effectively inhibited HO in injury-induced and genetic mouse models of the disease. It additionally prevents spontaneous HO, using a novel conditional-on knock-in mouse line carrying the human ACVR1(R206H) mutation for classic FOP. In addition, palovarotene restored long bone growth, maintained growth plate function, and protected growing mutant neonates when given to lactating mothers. Importantly, palovarotene maintained joint, limb, and body motion, providing clear evidence for its encompassing therapeutic potential as a treatment for FOP. Palovarotene (Sohonos) was approved in 2023 by FDA for treating Fibrodysplasia ossificans progressiva.
ln Vivo |
Palovarotene inhibits trauma-induced ectopic bone development and mediates osteogenesis and post-traumatic bone formation. Palovarotene is used to monitor intraoperative and subcutaneous heterotopic ossification (HO) following trauma. During the first 14 days of the trial, palovarotene was given orally at a dose of 1 mg/kg/day beginning on day 1 or day 5. H2O volume, wound breakdown, and associated processes were periodically observed for up to 84 days. When compared to vehicle animals, palovarotene dramatically lowers H2O by 50% to 60% per dosage [1]. Half of the Acvr1cR206H/+ mice got daily treatment with palovarotene for 14 days starting on the first day of damage, while the other half were given a vehicle as a control. Large tissue masses were seen in the target legs of the vector-acvr1cR206H/+ mutation, according to analysis of mCT and 3D image formation reconstructions after 14 days. However, palovarotene-treated partners showed significantly lower HO, as measured by bone volume/total volume formation, which improved by more than 80%[2].
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References |
[1]. Pavey GJ, et al. Targeted stimulation of retinoic acid receptor-γ mitigates the formation of heterotopic ossification in an established blast-related traumatic injury model. Bone. 2016 Sep;90:159-67.
[2]. Chakkalakal SA, et al. Palovarotene Inhibits Heterotopic Ossification and Maintains Limb Mobility and Growth in Mice With the Human ACVR1(R206H) Fibrodysplasia Ossificans Progressiva (FOP) Mutation. J Bone Miner Res. 2016 Sep;31(9):1666-75. [3]. Lees-Shepard JB, et al. Palovarotene reduces heterotopic ossification in juvenile FOP mice but exhibits pronounced skeletal toxicity. Elife. 2018 Sep 18;7. pii: e40814 |
Molecular Formula |
C27H30N2O2
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Molecular Weight |
414.54
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CAS # |
410528-02-8
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SMILES |
O=C(O)C1=CC=C(/C=C/C2=C(CN3N=CC=C3)C=C4C(C)(C)CCC(C)(C)C4=C2)C=C1
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InChi Key |
YTFHCXIPDIHOIA-DHZHZOJOSA-N
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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+
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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
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Synonyms |
RO-3300074; R-667; RO 3300074; R 667; RO3300074; R667; Sohonos
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~25 mg/mL (~60.31 mM)
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4123 mL | 12.0616 mL | 24.1231 mL | |
5 mM | 0.4825 mL | 2.4123 mL | 4.8246 mL | |
10 mM | 0.2412 mL | 1.2062 mL | 2.4123 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Injury-induced heterotopic ossification inAcvr1cR206H/+mutant mice is inhibited by the RARγ agonist Palovarotene. th> |
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Palovarotene preserves long bone growth and growth plate organization inPrrx1-R206Hmice.J Bone Miner Res.2016 Sep;31(9):1666-75. td> |
Chondrocyte proliferation and progression are altered inPrrx1-R206Hgrowth plates.J Bone Miner Res.2016 Sep;31(9):1666-75. td> |