PalovaroteneCAS# 410528-02-8 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 410528-02-8 | SDF | Download SDF |
| PubChem ID | 10295295 | Appearance | Powder |
| Formula | C27H30N2O2 | M.Wt | 414.54 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | R 667; Ro 3300074 | ||
| Solubility | DMSO : 30 mg/mL (72.37 mM; Need ultrasonic) | ||
| Chemical Name | 4-[(E)-2-[5,5,8,8-tetramethyl-3-(pyrazol-1-ylmethyl)-6,7-dihydronaphthalen-2-yl]ethenyl]benzoic acid | ||
| SMILES | CC1(CCC(C2=C1C=C(C(=C2)C=CC3=CC=C(C=C3)C(=O)O)CN4C=CC=N4)(C)C)C | ||
| Standard InChIKey | YTFHCXIPDIHOIA-DHZHZOJOSA-N | ||
| Standard InChI | 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+ | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Palovarotene is a nuclear retinoic acid receptor γ (RAR-γ) agonist.In Vivo:Palovarotene suppresses post-traumatic chondrogenesis and osteogenesis and mitigated trauma-induced ectopic bone formation. Palovarotene inhibits subcutaneous and intramuscular heterotopic ossification (HO) in mice. Palovarotene is given orally for 14 days at 1 mg/kg/day starting on post-operative day (POD) 1 or POD-5, and HO amount, wound dehiscence and related processes are monitored for up to 84 days post injury. Compared to vehicle-control animals, Palovarotene significantly decreases HO by 50 to 60% regardless of when the treatment started and if infection is present[1]. Starting from day 1 of injury, half of the Acvr1cR206H/+ mice are treated with Palovarotene by daily gavage for 14 days and the other half received vehicle as control. Analysis by mCT and 3D image reconstruction at day 14 shows that large HO tissue masses have formed in the targeted leg of Acvr1cR206H/+ mutant mice receiving vehicle, but HO formation is greatly diminished in Palovarotene-treated companions by more than 80% based on bone volume/total volume quantification[2]. References: | |||||
Palovarotene Dilution Calculator
Palovarotene Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.4123 mL | 12.0616 mL | 24.1231 mL | 48.2462 mL | 60.3078 mL |
| 5 mM | 0.4825 mL | 2.4123 mL | 4.8246 mL | 9.6492 mL | 12.0616 mL |
| 10 mM | 0.2412 mL | 1.2062 mL | 2.4123 mL | 4.8246 mL | 6.0308 mL |
| 50 mM | 0.0482 mL | 0.2412 mL | 0.4825 mL | 0.9649 mL | 1.2062 mL |
| 100 mM | 0.0241 mL | 0.1206 mL | 0.2412 mL | 0.4825 mL | 0.6031 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Palovarotene (R-667, RO-3300074) is a selective retinoic acid receptor gamma(RAR-γ) agonist for the treatment of emphysema.
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Palovarotene Inhibits Heterotopic Ossification and Maintains Limb Mobility and Growth in Mice With the Human ACVR1(R206H) Fibrodysplasia Ossificans Progressiva (FOP) Mutation.[Pubmed:26896819]
J Bone Miner Res. 2016 Sep;31(9):1666-75.
Fibrodysplasia ossificans progressiva (FOP), a rare and as yet untreatable genetic disorder of progressive extraskeletal ossification, is the most disabling form of heterotopic ossification (HO) in humans and causes skeletal deformities, movement impairment, and premature death. Most FOP patients carry an activating mutation in a bone morphogenetic protein (BMP) type I receptor gene, ACVR1(R206H) , that promotes ectopic chondrogenesis and osteogenesis and, in turn, HO. We showed previously that the retinoic acid receptor gamma (RARgamma) agonist Palovarotene effectively inhibited HO in injury-induced and genetic mouse models of the disease. Here we report that the drug 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. (c) 2016 American Society for Bone and Mineral Research.
Palovarotene, a novel retinoic acid receptor gamma agonist for the treatment of emphysema.[Pubmed:19876792]
Curr Opin Investig Drugs. 2009 Nov;10(11):1243-50.
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. Based on this hypothesis, Roche Holding AG is developing Palovarotene (R-667, RO-3300074), a selective retinoic acid receptor gamma agonist for the treatment of emphysema. In small animal studies, Palovarotene was claimed to reverse the structural, functional and inflammatory features of cigarette smoke-induced 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. Unlike all-trans retinoic acid, the pharmacokinetic profile of Palovarotene appears to be dose-proportional. At the time of publication, a phase II, placebo-controlled trial was ongoing, and was expected to report prospective measurements of exercise, gas transfer and lung densitometry endpoints. The development of a selective retinoic acid receptor gamma agonist for the treatment of emphysema represents the first of a new class of small-molecule regenerative therapies that may prove useful for the treatment of destructive or age-related lung disease.
