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Merck
CN

SML3083

Palovarotene

≥98% (HPLC)

别名:

(E)-4-(2-(3-((1H-Pyrazol-1-yl)methyl)-5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)vinyl)benzoic acid, 4-[(1E)-2-[5,6,7,8-Tetrahydro-5,5,8,8-tetramethyl-3-(1H-pyrazol-1-ylmethyl)-2-naphthalenyl]ethenyl]benzoic acid, 4-[(E)-2-(5,5,8,8-Tetramethyl-3-pyrzol-1-ylmethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)vinyl]benzoic acid, R 667, R-667, R667, RG 667, RG-667, RG667, RO 3300074, RO-3300074, RO3300074

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关于此项目

经验公式（希尔记法）:
C27H30N2O2
化学文摘社编号:
410528-02-8
分子量:
414.54
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD10565968

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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 string

CC1(C2=CC(CN3C=CC=N3)=C(/C=C/C4=CC=C(C=C4)C(O)=O)C=C2C(C)(CC1)C)C

InChI key

YTFHCXIPDIHOIA-DHZHZOJOSA-N

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Quality Level

100

相关类别

Biochem/physiol Actions

Orally active, selective retinoic acid receptor gamma (RARγ) agonist that reduces heterotopic ossification (HO) in cultures and in animal models in vivo.
Palovarotene is an orally active, selective retinoic acid receptor gamma (RARγ) agonist that reduces heterotopic ossification (HO) in cultures (15-300 nM) and in murine and rat fibrodysplasia ossificans progressiva (FOP) models in vivo (1 mg/kg rat, 0.27-2.49 mg/kg mouse or 15-100 μg/mouse via daily p.o.).

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000130224
0000130223
0000127846

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Benjamin M Wheatley et al.
Journal of orthopaedic research : official publication of the Orthopaedic Research Society, 36(4), 1135-1144 (2017-09-30)
Heterotopic ossification (HO) develops in the extremities of wounded service members and is common in the setting of high-energy penetrating injuries and blast-related amputations. No safe and effective prophylaxis modality has been identified for this patient population. Palovarotene has been
William P Shield et al.
Journal of orthopaedic research : official publication of the Orthopaedic Research Society, 38(5), 1045-1051 (2019-12-07)
Chondrosarcoma is the second most common primary bone sarcoma. Treatment of chondrosarcoma is limited to surgery due to radiation and chemotherapy resistance of this cancer. An ideal treatment for chondrosarcoma would be a well-tolerated, minimally invasive local or systemic treatment
Sayantani Sinha et al.
Bone, 90, 59-68 (2016-02-20)
Heterotopic ossification (HO) consists of ectopic cartilage and bone formation following severe trauma or invasive surgeries, and a genetic form of it characterizes patients with Fibrodysplasia Ossificans Progressiva (FOP). Recent mouse studies showed that HO was significantly inhibited by systemic
Carter M Lindborg et al.
Bone, 109, 153-157 (2017-10-01)
Genesis of a cartilaginous scaffold is an obligate precursor to bone formation in heterotopic endochondral ossification (HEO). We tested the hypothesis that cartilage-derived retinoic acid-sensitive protein (CD-RAP) can serve as a plasma biomarker for the pre-osseous cartilaginous stage of HEO.
Sonia A Garcia et al.
International journal of molecular sciences, 21(8) (2020-04-17)
Osteochondromas are cartilage-capped growths located proximate to the physis that can cause skeletal deformities, pain, limited motion, and neurovascular impingement. Previous studies have demonstrated retinoic acid receptor gamma (RARγ) agonists to inhibit ectopic endochondral ossification, therefore we hypothesize that RARγ
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