SL-327 |
カタログ番号GC15359
One-Click Copy Product Info
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SL-327はMEK1とMEK2の選択的な阻害剤であり、IC50値はそれぞれ0.18μMと0.22μMである。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 305350-87-2
Sample solution is provided at 25 µL, 10mM.
SL-327はMEK1とMEK2の選択的な阻害剤であり、IC50値はそれぞれ0.18μMと0.22μMである[1]。SL-327は、癲癇ラットで、発作間欠期スパイクと行動におけるMAPKシグナル伝達経路の役割の研究に使われる[2]。SL-327は、血液脳関門を通過でき、虚血脳損傷のマウスで、神経保護作用を発揮できる[3]。
In vitro（体外）実験で、黒色腫細胞（MV3とA375細胞）をSL-327（1.25µM）で48時間処理したところ、TBMS1処理により阻害された細胞成長曲線が回復し、TBMS1に阻害された細胞コロニーの形成能力が回復し、TBMS1で誘発されたLC3B-IIとp62の高い発現レベルが逆転した[4]。
In vivo（体内）実験で、雄のSwissアルビノCD1中年マウスに、SL-327（20mg/kg）を腹腔内注射したところ、放射状アーム迷路テストで、マウスに対する成長ホルモン（GH）の正の作用が遮断された[5]。SwissマウスにSL-327（1、5mg/kg）を腹腔内注射し、続いて行動試験を行ったところ、マウスで抗不安行動が誘発され、ジアゼパムと併用の場合、高架式十字迷路（EPM）テストでその抗不安特性は特に著しかった[6]。
References:
[1] Moranta D, Esteban S, García‐Sevilla J A. Acute, chronic and withdrawal effects of the cannabinoid receptor agonist WIN55212‐2 on the sequential activation of MAPK/Raf‐MEK‐ERK signaling in the rat cerebral frontal cortex: short‐term regulation by intrinsic and extrinsic pathways[J]. Journal of neuroscience research, 2007, 85(3): 656-667.
[2] Glazova M V, Nikitina L S, Hudik K A, et al. Inhibition of ERK 1/2 signaling prevents epileptiform behavior in rats prone to audiogenic seizures[J]. Journal of neurochemistry, 2015, 132(2): 218-229.
[3] Wang X, Wang H, Xu L, et al. Significant neuroprotection against ischemic brain injury by inhibition of the MEK1 protein kinase in mice: exploration of potential mechanism associated with apoptosis[J]. The Journal of pharmacology and experimental therapeutics, 2003, 304(1): 172-178.
[4] Du J, Dong Z, Tan L, et al. Tubeimoside I inhibits cell proliferation and induces a partly disrupted and cytoprotective autophagy through rapidly hyperactivation of MEK1/2-ERK1/2 cascade via promoting PTP1B in melanoma[J]. Frontiers in cell and developmental biology, 2020, 8: 607757.
[5] Ramis M, Sarubbo F, Sola J, et al. Cognitive improvement by acute growth hormone is mediated by NMDA and AMPA receptors and MEK pathway[J]. Progress in Neuro-Psychopharmacology and Biological Psychiatry, 2013, 45: 11-20.
[6] Michalak A, Wnorowski A, Berardinelli A, et al. Diazepam and SL-327 synergistically attenuate anxiety-like behaviours in mice–Possible hippocampal MAPKs specificity[J]. Neuropharmacology, 2020, 180: 108302.
| 動物実験 [1]: | |
動物モデル | 雄のSwissアルビノCD1中年マウス |
準備方法 | 雄のSwissアルビノCD1中年マウスを使用した。マウスのグループを生理食塩水と成長ホルモン（GH）（1mg/kg、腹腔内注射）で処理し、1時間後にワーキングメモリテストを行った。異なるグループのマウスには、MEK阻害剤SL-327（ジメチルスルホキシドに溶解された20mg/kg、腹腔内注射）を注射し、30分後にGHを投与し、よってマウスにおけるGHのみの効果と比較した。 |
投与形態 | 20mg/kg；腹腔内注射 |
アプリケーション | GHで処理されたマウスは、放射状アーム迷路テストで、エラー（未訪問のアーム、再び訪問したアーム）の数が減少した。しかし、GHの投与の30分前に、MEK阻害剤SL-327を腹腔内注射したところ、放射状アーム迷路テストに対するGHの正の作用が遮断された。 |
References: | |
| Cas No. | 305350-87-2 | SDF | |
| Chemical Name | (Z)-3-amino-3-(4-aminophenyl)sulfanyl-2-[2-(trifluoromethyl)phenyl]prop-2-enenitrile | ||
| Canonical SMILES | C1=CC=C(C(=C1)C(=C(N)SC2=CC=C(C=C2)N)C#N)C(F)(F)F | ||
| Formula | C16H12F3N3S | M.Wt | 335.35 |
| 溶解度 | ≥ 16.75mg/mL in DMSO | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.982 mL | 14.9098 mL | 29.8196 mL |
| 5 mM | 596.4 μL | 2.982 mL | 5.9639 mL |
| 10 mM | 298.2 μL | 1.491 mL | 2.982 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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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 saline, 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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)