1. Neuronal Signaling
  2. Sigma Receptor
  3. Dimemorfan phosphate

Dimemorfan phosphate is a sigma 1 receptor agonist, used as a potent antitussive.

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Dimemorfan phosphate

Dimemorfan phosphate 構造式

CAS 番号 : 36304-84-4

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
USD 55 在庫あり
Solution
10 mM * 1 mL in Water USD 55 在庫あり
Solid
50 mg $50 在庫あり
100 mg $75 在庫あり
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製品説明

Dimemorfan phosphate is a sigma 1 receptor agonist, used as a potent antitussive.

IC50 & Target

Sigma 1 Receptor

 

体外実験

Dimemorfan (5-20?μM) inhibits both fMLP- and PMA-induced ROS production in a concentration-dependent manner and is relatively more potent in inhibiting fMLP-induced ROS production with an IC50 value of 7.0?μM. Dimemorfan (10-50?μM) does not display significant activity in scavenging free radicals by xanthine/xanthine oxidase system. Dimemorfan significantly suppressed Mac-1 upregulation both in PMA- and fMLP-activated groups. Dimemorfan (10-20?μM) significantly suppresses LPS-induced ROS and NO production, and suppresses LPS-induced iNOS protein expression, and both the percentage of the positively stained population and the MCF intensities of MCP-1 and TNF-α in BV2 cytosol. Dimemorfan (20?μM) significantly blocks the degradation of cytosolic Iκ-Bα and nuclear translocation of NF-κB p65, as well as the transcriptional activity of NF-κB[2].

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

体内実験

Dimemorfan (6.25 or 12.5 mg/kg, s.c.) significantly attenuates the BAY k-8644-induced convulsive behaviors, in a dose-related manner (6.25 mg/kg dimemorfan+BAY k-8644 or 12.5 mg/kg dimemorfan+BAY k-8644 versus Saline+BAY k-8644, P<0.05 and P<0.01, respectively). Dimemorfan significantly attenuates BAY k-8644-induced increases in the c-fos and c-jun protein expression in a dose-dependent manner. Dimemorfan does not significantly affect locomotor activity or produce significant circling behavior in any locomotor pattern in mice[1]. Dimemorfan (1 and 5?mg/kg, i.p.) surpresses the incarease of the plasma levels of TNF-α in mice. The infiltration of neutrophils into lung and liver as well as the production of oxidative stress (EB staining) in these tissues induced by LPS is markedly inhibited by the treatment with dimemorfan[2].

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

分子量

353.39

分子式

C18H28NO4P

CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=P(O)(O)O.CN1[C@](CC2=CC=C(C)C=C32)([H])[C@](CCCC4)([H])[C@]34CC1

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

H2O : 10 mg/mL (28.30 mM; ultrasonic and warming and heat to 60°C)

DMSO : 1 mg/mL (2.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8297 mL 14.1487 mL 28.2973 mL
5 mM 0.5659 mL 2.8297 mL 5.6595 mL
10 mM 0.2830 mL 1.4149 mL 2.8297 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. 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)

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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

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体積 (開始)

V1

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濃度 (終了)

C2

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体積 (終了)

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体内:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 16.67 mg/mL (47.17 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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(per animal)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
純度とドキュメンテーション

純度: 99.94%

参考文献
動物実験
[1]

C57BL/6 mice receive each morphinan (dextromethorphan, dextrorphan or dimemorfan) compound (20 or 40 mg/kg, i.p. per day) or PCP (2.5 or 5 mg/kg, i.p. per day) once a day for 7 days. Ten minutes after the last treatment with each drug, locomotor activity is measured for 30 min using an automated video-tracking system. Eight test boxes (40 cm×40 cm×30 cm high) are operated simultaneously by an IBM computer. Animals are studied individually during locomotion in each test box, where they are adapted for 10 min before starting the experiment. A printout for each session showed the pattern of the ambulatory movements of the test box. The distance traveled in cm by the animals in horizontal locomotor activity is analyzed. Data are collected and analyzed between 09:00 and 17:00 h.

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。

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. 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
DMSO / H2O 1 mM 2.8297 mL 14.1487 mL 28.2973 mL 70.7434 mL
H2O 5 mM 0.5659 mL 2.8297 mL 5.6595 mL 14.1487 mL
10 mM 0.2830 mL 1.4149 mL 2.8297 mL 7.0743 mL
15 mM 0.1886 mL 0.9432 mL 1.8865 mL 4.7162 mL
20 mM 0.1415 mL 0.7074 mL 1.4149 mL 3.5372 mL
25 mM 0.1132 mL 0.5659 mL 1.1319 mL 2.8297 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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  • Molarity Calculator

  • Dilution Calculator

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

質量   濃度   体積   分子量 *
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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.

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製品名:
Dimemorfan phosphate
製品番号:
HY-B2215
数量:
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