2. GPCR/G Protein Neuronal Signaling
  3. Opioid Receptor
  4. Ro 64-6198

Ro 64-6198 is a potent, selective, nonpeptide, high-affinity, high cellular permeability and brain penetration N/OFQ receptor (NOP) agonist with an EC50 value of 25.6 nM. Ro 64-6198 is at least 100 times more selective for the NOP receptor over the classic opioid receptors. Ro 64-6198 can be used for stress and anxiety, addiction, neuropathic pain, cough, and anorexia.

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Ro 64-6198

Ro 64-6198 構造式

CAS 番号 : 280783-56-4

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 297 在庫あり
Solution
10 mM * 1 mL in DMSO USD 297 在庫あり
Solid
5 mg $270 在庫あり
10 mg $430 在庫あり
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Based on 1 publication(s) in Google Scholar

Ro 64-6198 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

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

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製品説明

Ro 64-6198 is a potent, selective, nonpeptide, high-affinity, high cellular permeability and brain penetration N/OFQ receptor (NOP) agonist with an EC50 value of 25.6 nM. Ro 64-6198 is at least 100 times more selective for the NOP receptor over the classic opioid receptors. Ro 64-6198 can be used for stress and anxiety, addiction, neuropathic pain, cough, and anorexia[1][2].

IC50 & Target

NOP Receptor/ORL1

 

Cellular Effect
Cell Line Type Value Description References
CHO EC50
21 nM
Compound: Ro-646198
Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
[PMID: 22541041]
体外実験

Ro 64-6198 also produces rapid desensitization of the NOP receptor. In vitro studies shows that treatment with Ro 64-6198 results in a functional desensitization of the receptor, a loss in binding sites, and an apparent decrease in binding affinity. The desensitization produced by Ro 64-6198 is not reversed by acidic washes[1].
Ro 64-6198 does recruit both arrestin3 (EC50 of 0.912 μM) and arrestin2 (EC50 of 1.20 μM) to the NOP receptor in a concentration-dependent manner comparably with N/OFQ[2].

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

Ro 64-6198 関連抗体
体内実験

At low doses Ro 64-6198 is anxiolytic in several neophobic tests, including the marble burying test in mice, the elevated plus maze in rats and the open field test in rats. In the marble burying test, at 1 mg/kg, i.p., Ro 64-6198 produces a decrease in the number of marbles buried, without altering locomotor activity, indicating a decrease in neophobia and anxiety. Ro 64-6198 selectively increases the number of open arm transitions and time spent in the open arms of the elevated plus maze at doses of 0.32-3 mg/kg, i.p., without affecting closed arm transitions or locomotor activity in the closed arms. In the open field test, Ro 64-6198, at doses of 0.32-3 mg/kg, attenuates the inhibition of exploration that results from the stress of a novel environment[1].

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

401.54

分子式

C26H31N3O
CAS 番号
Appearance

Solid

Color

White to yellow

SMILES

O=C1NCN(C2=CC=CC=C2)C13CCN([C@H]4CC[C@]5([H])CCCC6=C5C4=CC=C6)CC3
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: 

DMSO : 50 mg/mL (124.52 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 2.4904 mL 12.4521 mL 24.9041 mL
5 mM 0.4981 mL 2.4904 mL 4.9808 mL
10 mM 0.2490 mL 1.2452 mL 2.4904 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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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 (6.23 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: ≥99.0%

COA (258 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. 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 1 mM 2.4904 mL 12.4521 mL 24.9041 mL 62.2603 mL
5 mM 0.4981 mL 2.4904 mL 4.9808 mL 12.4521 mL
10 mM 0.2490 mL 1.2452 mL 2.4904 mL 6.2260 mL
15 mM 0.1660 mL 0.8301 mL 1.6603 mL 4.1507 mL
20 mM 0.1245 mL 0.6226 mL 1.2452 mL 3.1130 mL
25 mM 0.0996 mL 0.4981 mL 0.9962 mL 2.4904 mL
30 mM 0.0830 mL 0.4151 mL 0.8301 mL 2.0753 mL
40 mM 0.0623 mL 0.3113 mL 0.6226 mL 1.5565 mL
50 mM 0.0498 mL 0.2490 mL 0.4981 mL 1.2452 mL
60 mM 0.0415 mL 0.2075 mL 0.4151 mL 1.0377 mL
80 mM 0.0311 mL 0.1557 mL 0.3113 mL 0.7783 mL
100 mM 0.0249 mL 0.1245 mL 0.2490 mL 0.6226 mL
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Ro 64-6198 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:

Ro 64-6198280783-56-4Opioid ReceptorNonpeptideneuropathicanxietybrainpenetrationcellularpermeabilitycoughanorexiaInhibitorinhibitorinhibit

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