AM251

製品コードS2819 バッチS281901

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C22H21Cl2IN4O
分子量 555.24 CAS No. 183232-66-8
Solubility (25°C)* 体外 DMSO 40 mg/mL (72.04 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
1.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 AM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain.
in vitro AM251 reduces veratridine-dependent (tetrodotoxin suppressible) release of L-glutamic acid and GABA from synaptosomes with IC50 of 8.5 μM and 9.2 μM, respectively. AM251 increases (by 2.3 times) the Kd of radioligand without altering Bmax. AM251 inhibits equilibrium binding by allosterically accelerating the dissociation of the [3H]-batrachotoxinin A 20-alpha-benzoate:sodium channel complex. [1] AM251 reduces cholesteryl ester synthesis in unstimulated and acetylated LDL-stimulated Raw 264.7 macrophages, CB2+/+ and CB2 −/− peritoneal macrophages. [2]
in vivo AM251 causes a sustained reduction of daily food intake in the rat. [3] AM251 produces food avoidance and behaviors associated with nausea but does not impair feeding efficiency in rats. [4] AM251 disrupts memory consolidation of the inhibitory avoidance task. [5] AM251 has caused a significative decrease in the test step-down latency when compared to the control group, but no differences are detected in the open field habituation task, including the number of crossings, i.e. there are no motor effects. [6] AM251 (4.0 mg/kg) reduces freezing during a conditioned tone cue played within a novel context. [7]
特徴 A selective cannabinoid 1 blocker.

プロトコル(参考用のみ)

キナーゼアッセイ Caspase-3 assay
Macrophages are seeded (2 × 106/well) in 12-well culture plates. AM-25 are added from 4 mM stock solutions prepared in DMSO, 1 hour prior to the addition of 7-ketocholesterol from a 2 mg/mL ethanol stock solution. Controls are adjusted to receive equivalent volumes of DMSO and ethanol. After 16 hours, caspase-3 activity is determined. All treatments are done in triplicate and the data presented as the mean RFLU/mg protein.
動物実験 動物モデル Moderately obese male Lewis rats
投薬量 1.25 mg/kg, 2.5 mg/kg and 5 mg/kg
投与方法 i.p.

カスタマーフィードバック

, , Tumour Biol, 2016, DOI: 10.1007/s13277-016-5447-6

Data from [Data independently produced by , , Neuropharmacology, 2018, 133:242-253]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Wwl70-induced ABHD6 inhibition attenuates memory deficits and pathological phenotypes in APPswe/PS1dE9 mice [ Pharmacol Res, 2023, 194:106864] PubMed: 37480972
The endocannabinoid system's involvement in motor development relies on cannabinoid receptors, TRP channels, and Sonic Hedgehog signaling [ Physiol Rep, 2023, 11(1):e15565] PubMed: 36636759
Medium-throughput zebrafish optogenetic platform identifies deficits in subsequent neural activity following brief early exposure to cannabidiol and Δ9-tetrahydrocannabinol [ Sci Rep, 2021, 11(1):11515] PubMed: 34075141
Early suppression of the endocannabinoid degrading enzymes FAAH and MAGL alters locomotor development in zebrafish [ J Exp Biol, 2021, jeb.242635] PubMed: 34151979
Embryonic exposure to cannabidiol disrupts active neural circuits, an effect increased by Δ□-tetrahydrocannabinol and involving CB1R and CB2R in zebrafish [ BioRxiv, 2021, 10.1101/2021.01.04.425279] PubMed: none
N-linoleyltyrosine protects PC12 cells against oxidative damage via autophagy: Possible involvement of CB1 receptor regulation [ Int J Mol Med, 2020, 46(5):1827-1837] PubMed: 33000188
Rimonabant suppresses RNA transcription of hepatitis B virus by inhibiting hepatocyte nuclear factor 4α. [ Microbiol Immunol, 2020, 10.1111/1348-0421.12777] PubMed: 31981244
CB1 and CB2 receptors play differential roles in early zebrafish locomotor development. [ J Exp Biol, 2019, 222(Pt 16)] PubMed: 31253713
CB1 and CB2 receptors play differential roles in early zebrafish locomotor development [ J Exp Biol, 2019, 222(Pt 16)jeb206680] PubMed: 31253713
Impaired glucocorticoid-mediated HPA axis negative feedback induced by juvenile social isolation in male rats [Boero G Neuropharmacology, 2018, 133:242-253] PubMed: 29407214

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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