(-)-U-50488 hydrochloride
Based on 1 publication(s) in Google Scholar
(-)-U-50488 hydrochloride ((-)-Trans-(1S,2S)-U-50488 hydrochloride) is a selective kappa-opioid receptor (KOR) agonist (Kd=2.2 nM) over μ-opioid receptor (MOR) (Kd=430 nM). (-)-U-50488 hydrochloride is a more active enantiomer than (+) trans-(1R,2R) U-50488 (HY-15997A) or the (±) trans-racemic mixture U-50488 (HY-15997B). (-)-U-50488 hydrochloride has a potent and sustained anti-HIV effect in fected blood monocyte-derived macrophages (MDM).
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 98.95%
- CAS 番号: 114528-79-9
- 分子式: C19H27Cl3N2O
- 分子量:405.79
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保管条件:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 (-)-U-50488 hydrochloride
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生物活性
製品説明
IC50 & Target
Kd: 2.2 nM (kappa-opioid receptor (KOR))Kd: 430 nM (μ-opioid receptor (MOR))[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
17 nM
Compound: U50,488H
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Agonist activity at mouse kappa opioid receptor-1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis
Agonist activity at mouse kappa opioid receptor-1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis
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[PMID: 27556704] |
| CHO | EC50 |
35.8 nM
Compound: U50488
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Agonist activity at human kappa opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
Agonist activity at human kappa opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
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[PMID: 32530286] |
| HEK293 | EC50 |
0.4 nM
Compound: 16
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Activity at kappa opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding
Activity at kappa opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding
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[PMID: 19683449] |
体外実験
(-)-U-50488 hydrochloride (1 pM-100 nM; 7 days) exhibits a concentration-dependent inhibition of HIV-1 expression, the maximal inhibition at 10 13 M (approximately 73% suppression) in acutely infected blood monocyte-derived macrophages (MDM)[2]. (-)-U-50488 hydrochloride (10-13 M; 7-14 days) (10 13 M) markedly inhibits HIV-1 expression both at 7 and 14 days after infection, it has a sustained inhibitory effect on HIV-1 infection in MDM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice[1]
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Dosage:5 mg/kg
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Administration:Intraperitoneal injection; single dose; 2 hrs before 4% PFA
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Result:Induced pMeCP2-S421 in the brain acutely.
化学情報
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CAS 番号 114528-79-9
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性状 Solid
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分子量 405.79
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分子式 C19H27Cl3N2O
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Color White to off-white
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SMILES
O=C(N(C)[C@@H]1[C@@H](N2CCCC2)CCCC1)CC3=CC=C(Cl)C(Cl)=C3.[H]Cl
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別名
(-)-Trans-(1S,2S)-U-50488 hydrochloride
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (1)
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Journal Impact Factor
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Most Recent
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ACS Cent Sci
An Epigenetic Switch for Sex-Specific Brain Resilience in Stroke: Targeting HDAC2 to Amplify Endogenous Oxytocin Signaling. [Abstract]2026 Mar 25;12(4):497-523. PMID: 42038487
溶剤 & 溶解度
体外:
DMSO : ≥ 100 mg/mL (246.43 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 50 mg/mL (123.22 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.16 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.16 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
プロトコル
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Primary monocyte-to-macrophage differentiation
Primary human monocytes can be differentiated ex vivo into monocyte-derived macrophages by culturing purified blood monocytes for approximately 5-7 days in macrophage-supporting cytokine conditions; M-CSF commonly yields CD14^high/CD163^high macrophages, while GM-CSF yields a phenotypically distinct macrophage population, so the cytokine condition should be chosen according to the downstream model. The readout of successful differentiation is a combined change in morphology, adherence, surface phenotype, and function: differentiated macrophages become adherent, enlarge, acquire macrophage-associated markers such as CD14, CD68, CD163, CD206, or HLA-DR depending on culture condition, and show increased phagocytic capacity compared with starting monocytes.
純度とドキュメンテーション
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データシート (278 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Kirti Kumari Sharma, et al. The search for the "next" euphoric non-fentanil novel synthetic opioids on the illicit drugs market: current status and horizon scanning. Forensic Toxicol. 2019;37(1):1-16. [Content Brief]
[2]. Anthony S Zannas, ET AL. Regulation and function of MeCP2 Ser421 phosphorylation in U50488-induced conditioned place aversion in mice. Psychopharmacology (Berl). 2017 Mar;234(6):913-923. [Content Brief]
[3]. C C Chao,et al. U50488 inhibits HIV-1 expression in acutely infected monocyte-derived macrophages. Drug Alcohol Depend. 2001 Apr 1;62(2):149-54. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.4643 mL | 12.3216 mL | 24.6433 mL | 61.6082 mL |
| 5 mM | 0.4929 mL | 2.4643 mL | 4.9287 mL | 12.3216 mL | |
| 10 mM | 0.2464 mL | 1.2322 mL | 2.4643 mL | 6.1608 mL | |
| 15 mM | 0.1643 mL | 0.8214 mL | 1.6429 mL | 4.1072 mL | |
| 20 mM | 0.1232 mL | 0.6161 mL | 1.2322 mL | 3.0804 mL | |
| 25 mM | 0.0986 mL | 0.4929 mL | 0.9857 mL | 2.4643 mL | |
| 30 mM | 0.0821 mL | 0.4107 mL | 0.8214 mL | 2.0536 mL | |
| 40 mM | 0.0616 mL | 0.3080 mL | 0.6161 mL | 1.5402 mL | |
| 50 mM | 0.0493 mL | 0.2464 mL | 0.4929 mL | 1.2322 mL | |
| 60 mM | 0.0411 mL | 0.2054 mL | 0.4107 mL | 1.0268 mL | |
| 80 mM | 0.0308 mL | 0.1540 mL | 0.3080 mL | 0.7701 mL | |
| 100 mM | 0.0246 mL | 0.1232 mL | 0.2464 mL | 0.6161 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
(-)-U-50488 hydrochloride 関連分類
HY-15997 関連分類
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