22(R)-hydroxy Cholesterol (Synonyms: Narthesterol) |
カタログ番号GC14972 |
LXRsの内因性アゴニスト
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Cas No.: 17954-98-2
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
EC50:325ナノモル
22(R)-ヒドロキシコレステロールは、肝X受容体(LXR)の内因性アゴニストです。
肝X受容体であるLXRRとLXRαは、ファルネソイドX受容体(FXR)と共に、これらの孤児受容体のサブファミリーを形成しています。最近報告された研究によれば、LXRとFXRはそれぞれオキシステロールおよび胆汁酸のホルモン受容体であることがわかっています。
In vitro:以前の研究では、22(R)-ヒドロキシコレステロールは、プレグネノロン生合成の中間体として副腎にしか存在せず、24(R)、25-エポキシコレステロールや20(S)-ヒドロキシコレステロールとは類似しないことがわかっています。さらに、22(R)-ヒドロキシコレステロールおよびそのアナログである23(S)-ヒドロキシコレステロールおよび24(S)-ヒドロキシコレステロールの水酸基はすべてTrp443から2.0〜2.5の位置にあります[1]。別の研究では、培養されたマクロファージで22(R)-hydroxycholesterolと9-cis-retinoic acidを加算的に誘導することができ、肝X受容体および視黄酸X受容体ファミリーの核内受容体による誘導を示唆しています。さらに、上流プロモーターはRAWマクロファージに転染された場合、22(R)-hydroxycholesterol処理で7倍誘導されました[2]。
「In vivo:現時点では、動物のin vivoデータは報告されていません。」
臨床試験:現時点では、22(R)-ヒドロキシコレステロールはまだ前臨床開発段階にあります。
References:
[1] T. A. Spencer, L. Dansu, J. S. Russel, et al. Pharmacophore analysis of the nuclear oxysterol receptor LXRα. Journal of Medicinal Chemistry 44, 886-897(2001).
[2] Costet P, Luo Y, Wang N, Tall AR. Sterol-dependent transactivation of the ABC1 promoter by the liver X receptor/retinoid X receptor. J Biol Chem. 2000 Sep 8;275(36):28240-5.
Cas No. | 17954-98-2 | SDF | |
同義語 | Narthesterol | ||
Chemical Name | cholest-5-ene-3β,22R-diol | ||
Canonical SMILES | CC(C)CC[C@@H](O)[C@@H](C)C1CCC2C3CC=C4C[C@@H](O)CC[C@]4(C)C3CC[C@@]21C | ||
Formula | C27H46O2 | M.Wt | 402.7 |
溶解度 | ≤20mg/ml in ethanol;0.1mg/ml in DMSO;2mg/ml in dimethyl formamide | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.4832 mL | 12.4162 mL | 24.8324 mL |
5 mM | 0.4966 mL | 2.4832 mL | 4.9665 mL |
10 mM | 0.2483 mL | 1.2416 mL | 2.4832 mL |
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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