1. Metabolic Enzyme/Protease
  2. RAR/RXR

Palovarotene (Synonyms: R 667; Ro 3300074)

Cat. No.: HY-14799 Purity: 99.16%
Handling Instructions

Palovarotene is a nuclear retinoic acid receptor γ (RAR-γ) agonist.

For research use only. We do not sell to patients.

Palovarotene Chemical Structure

Palovarotene Chemical Structure

CAS No. : 410528-02-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 440 In-stock
Estimated Time of Arrival: December 31
5 mg USD 400 In-stock
Estimated Time of Arrival: December 31
10 mg USD 742 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2280 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Palovarotene is a nuclear retinoic acid receptor γ (RAR-γ) agonist.

IC50 & Target

RAR-γ[1]

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].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : 19.5 mg/mL (47.04 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Palovarotene is prepared as follows: 0.0735 mg/mL palovarotene in 0.735% DMSO with 4% Tween 80 in PBS (pH 7.4); 0.147 mg/mL palovarotene in 1.47% DMSO with 4% Tween 80 in PBS (pH 7.4)[3].

References
Animal Administration
[1][2]

Rats[1]
A total of 110 young adult pathogen-free male Sprague Dawley rats (Rattus norvegicus; 400-600 g) are used. Rats receive via oral gavage (100 μL) either Palovarotene (1.0 mg/kg) or vehicle as control (5% DMSO in corn oil) prepared every other day for 14 days, starting at postoperative day 1 (POD-1) or POD-5. Rats are euthanized at indicated time points post-injury for ex vivo end point analysis by micro-computed CT (μCT), histology and RT-PCR gene transcript expression.
Mice[2]
One-month-old Acvr1cR206H/+ mice are provided doxycycline chow for 3 days to induce mutant gene expression globally. Mouse quadriceps muscles are injured by injection with 50 mL of 10mM cardiotoxin. Beginning on the day of injury, Palovarotene or vehicle (1:4 DMSO in corn oil) is administered daily for 14 days by oral gavage (100 mg/mouse from days 1 to 3 and 15mg/mouse from days 4 to 14) using a 20-gauge gavage needle. Palovarotene solution in DMSO is stored at -20°C under argon and diluted (1:4) with corn oil for administration.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

414.54

Formula

C₂₇H₃₀N₂O₂

CAS No.

410528-02-8

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.16%

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Product Name:
Palovarotene
Cat. No.:
HY-14799
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Palovarotene

Cat. No.: HY-14799