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Tarenflurbil/R-氟比洛芬/51543-40-9




货号:HY-10291

规格:1G

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DeepBio得分:5567.2
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目录号: HY-10291 纯度: 99.99% ee.: 99.09%

Description

Tarenflurbil ((R)-Flurbiprofen) is the R-enantiomer of the racemate NSAID Flurbiprofen, Tarenflurbil ((R)-Flurbiprofen) inhibits the binding of [3H]9-cis-RA to RXRα LBD with IC50 of 75 μM.

IC50 & Target

IC50: 75 μM (RXRα)[1]

In Vitro

Tarenflurbil ((R)-Flurbiprofen) can significantly reduce Aβ secretion, but at the same time, increases the level of intracellular Aβ. The binding between [3H]9-cis-RA and RXRα is competitively inhibited by both unlabeled (R)-Flurbiprofen and 9-cis-RA. (R)-Flurbiprofen can interfere with the interaction between RXRα and 9-cis-retinoid acid (9-cis-RA), and that 9-cis-RA decreases Tarenflurbil ((R)-Flurbiprofen)’s reduction of Aβ secretion. Tarenflurbil ((R)-Flurbiprofen) treatment significantly increases the levels of intracellular Aβ species[1]. The well characterized, nonsteroidal anti-inflammatory drug (nonsteroidal anti-inflammatory drug), Tarenflurbil ((R)-Flurbiprofen) affects only Aβ and not Notch β formation, indicating that second generation GSMs and nonsteroidal anti-inflammatory drug-based GSMs have different modes of action regarding Notch processing[2].

In Vivo

Effects of the early and late onset of treatment with Tarenflurbil ((R)-Flurbiprofen) are assessed in C57BL6/J mice that develop a non-remitting form of the disease, and in SJL mice that develop a relapsing-remitting (RR)-EAE. Tarenflurbil ((R)-Flurbiprofen) completely prevents the development of clinical EAE scores in C57BL6/J mice when the treatment is started within 3 days after immunization. This regimen is referred to as preventive treatment. The effect is dose-dependent, and the minimum daily dose for complete prevention is 5 mg/kg/day. Effects of Tarenflurbil ((R)-Flurbiprofen) are comparable to those of Fingolimod (FTY720, 0.5 mg/kg/day), which is used as the positive control. Tarenflurbil ((R)-Flurbiprofen) also significantly reduces clinical EAE scores in C57BL6/J mice when treatment is started shortly before onset of clinical manifestations, referred to as semi-therapeutic (10 mg/kg/day) and reduces clinical scores when the treatment is initiated after full development of the disease on day 13 (5 mg/g/day)[3].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT00380276 Myrexis Inc. Alzheimer´s Disease September 2006 Phase 3
NCT02206854 Gerd Geisslinger|Fraunhofer Institute for Molecular Biology and Applied Ecology|Goethe University Healthy Volunteers June 2014 Phase 1
NCT00045123 Myrexis Inc.|National Cancer Institute (NCI) Prostate Cancer February 2002 Phase 2
Molecular Weight

244.26

Formula

C₁₅H₁₃FO₂

CAS No.

51543-40-9

SMILES

O=C(O)[C@H](C)C1=CC=C(C2=CC=CC=C2)C(F)=C1

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (204.70 mM)

* "≥" means soluble, but saturation unknown.

Preparing 
Stock Solutions
ConcentrationSolventMass 1 mg 5 mg 10 mg
1 mM 4.0940 mL 20.4700 mL 40.9400 mL
5 mM 0.8188 mL 4.0940 mL 8.1880 mL
10 mM 0.4094 mL 2.0470 mL 4.0940 mL
* 请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液,并请注意储备液的保存方式和期限。
In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案,配制前请先配制澄清的储备液,再依次添加助溶剂 (为保证实验结果的可靠性,体内实验的工作
液,建议您现用现配,当天使用;澄清的储备液可以根据储存条件,适当保存;以下溶剂前的百分比是指该溶剂在您配制终溶液中的体积占比):

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (10.23 mM); Clear solution

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (10.23 mM); Clear solution

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (10.23 mM); Clear solution

*以上所有助溶剂都可在 MCE 网站选购。
References