(±)-U-50488 hydrochloride (Synonyms: (±)-Trans-(1R,2R)-U-50488 hydrochloride) |
カタログ番号GC15885 |
κ-オピオイド受容体アゴニスト、選択的
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 67197-96-0
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
(±)-U-50488塩酸塩は、κオピオイド受容体に対する選択的アゴニストです[1]。
κ-オピオイド受容体(KOR)は、オピオイドペプチドダイノルフィンのための一種のオピオイド受容体であり、中毒を制御します。また、KORはストレス、不安、無楽感症、うつ病および薬物探求行動の増加に重要な役割を果たしています。
(±)-U-50488塩酸塩は、選択的なKORアゴニストです[1]。孤立したラットDRGニューロンでは、U-50488(0.3?40μM)が電圧非依存性Ca2 +チャネル電流を阻害しました。 KORを発現しないHeLa細胞では、U-50488(20μM)がCa2 +チャネルをブロックしました[2]。
リス猿では、U-50488は強力な抗痛覚作用を示し、利尿作用を引き起こしました[1]。ウサギの精巣静脈に電気刺激を与えた場合、U-50488はIC50値が26.5 nMであるという条件下で収縮を増強しました。マウスでは、U-50488はED50値が15.3 mg/kgで運動機能を低下させ、自発活動も減少させました[3]。成体ラットでは、U-50488は自己刺激反応の維持に必要な閾値を上昇させるうつ状態のような効果があります。ただし、オスは閾値上昇効果に対して女性よりも有意に敏感でした[4]。
References:
[1].? Tang AH, Collins RJ. Behavioral effects of a novel kappa opioid analgesic, U-50488, in rats and rhesus monkeys. Psychopharmacology (Berl), 1985, 85(3): 309-314.
[2].? Hassan B, Ruiz-Velasco V. The κ-opioid receptor agonist U-50488 blocks Ca2+ channels in a voltage- and G protein-independent manner in sensory neurons. Reg Anesth Pain Med, 2013, 38(1): 21-27.
[3].? Lu SN, Ma SC, Zhang KG, et al. Comparison of pharmacological profile of selective kappa-opioid agonist K-II and U-50488. Yao Xue Xue Bao, 1991, 26(3): 171-174.
[4].? Russell SE, Rachlin AB, Smith KL, et al. Sex differences in sensitivity to the depressive-like effects of the kappa opioid receptor agonist U-50488 in rats. Biol Psychiatry, 2014, 76(3): 213-222.
Cas No. | 67197-96-0 | SDF | |
同義語 | (±)-Trans-(1R,2R)-U-50488 hydrochloride | ||
Chemical Name | 2-(3,4-dichlorophenyl)-N-methyl-N-((1R,2R)-2-(pyrrolidin-1-yl)cyclohexyl)acetamide hydrochloride | ||
Canonical SMILES | CN(C(CC1=CC(Cl)=C(Cl)C=C1)=O)[C@]2([H])CCCC[C@@]2([H])N3CCCC3.Cl | ||
Formula | C19H26Cl2N2O.HCl | M.Wt | 405.79 |
溶解度 | 20mg/mL in DMSO, 20mg/mL in DMF, 20mg/mL in Ethanol | Storage | Desiccate 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 | 2.4643 mL | 12.3216 mL | 24.6433 mL |
5 mM | 0.4929 mL | 2.4643 mL | 4.9287 mL |
10 mM | 0.2464 mL | 1.2322 mL | 2.4643 mL |
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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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