2. GPCR/G Protein Neuronal Signaling
  3. Opioid Receptor
  4. (-)-U-50488 hydrochloride

(-)-U-50488 (hydrochloride)  (Synonyms: (-)-Trans-(1S,2S)-U-50488 (hydrochloride))

製品番号: HY-15997 純度: 98.95%
COA 取扱説明書 Technical Support

(-)-U-50488 hydrochloride ((-)-Trans-(1S,2S)-U-50488 hydrochloride) is a selective kappa-opioid receptor (KOR) agonist (b>Kd=2.2 nM) over μ-opioid receptor (MOR) (b>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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(-)-U-50488 hydrochloride

(-)-U-50488 (hydrochloride) 構造式

CAS 番号 : 114528-79-9

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 143 在庫あり
Solution
10 mM * 1 mL in DMSO USD 143 在庫あり
Solid
5 mg $130 在庫あり
10 mg $220 在庫あり
25 mg $430 在庫あり
50 mg $810 在庫あり
100 mg $1300 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 1 publication(s) in Google Scholar

Other Forms of (-)-U-50488 hydrochloride:

(-)-U-50488 (hydrochloride) 関連抗体

Top Publications Citing Use of Products

Opioid Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

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製品説明

(-)-U-50488 hydrochloride ((-)-Trans-(1S,2S)-U-50488 hydrochloride) is a selective kappa-opioid receptor (KOR) agonist (b>Kd=2.2 nM) over μ-opioid receptor (MOR) (b>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)[1].

IC50 & Target

Kd: 2.2 nM (kappa-opioid receptor (KOR))
Kd: 430 nM (μ-opioid receptor (MOR))[1]
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.

(-)-U-50488 (hydrochloride) 関連抗体
体内実験

(-)-U-50488 hydrochloride (intraperitoneal?injection?; 5mg/kg; 2 hrs before 4% paraformaldehyde (PFA)) acutely induced pMeCP2-S421 (phosphorylation of the methyl-DNA binding protein MeCP2 at Ser421) and Fos selectively in the nucleus accumbens (NAc) but does not alter MeCP2 levels in any brain region[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J mice[1]
Dosage: 5 mg/kg
Administration: Intraperitoneal injection; single dose; 2 hrs before 4% PFA
Result: Induced pMeCP2-S421 in the brain acutely.
分子量

405.79

分子式

C19H27Cl3N2O
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(N(C)[C@@H]1[C@@H](N2CCCC2)CCCC1)CC3=CC=C(Cl)C(Cl)=C3.[H]Cl
輸送条件

Room temperature in continental US; may vary elsewhere.
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)
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.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
純度とドキュメンテーション

純度: 99.71%

COA (251 KB) HNMR (264 KB) RP-HPLC (244 KB) LCMS (87 KB)

取扱説明書 (2659 KB)
参考文献

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.

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(-)-U-50488 hydrochloride Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

(-)-U-50488114528-79-9(-)-Trans-(1S,2S)-U-50488Opioid ReceptoragonistMORμ-opioid receptorbloodmonocyte-derivedmacrophageMDMHIVInhibitorinhibitorinhibit

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