Ro 64-6198

Name: Ro 64-6198
Brand: MedChemExpress
SKU: HY-12844
Rating: 4.5 (1 reviews)

Cat. No.: HY-12844 Purity: 99.82%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

For research use only. We do not sell to patients.

Ro 64-6198 Chemical Structure

CAS No. : 280783-56-4

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 424	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 424	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 480	In-stock	Estimated Time of Arrival: December 31
10 mg		Get quote
50 mg		Get quote

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE Ro 64-6198

•Br J Pharmacol. 2021 Oct 27. [Abstract]

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View All Opioid Receptor Isoform Specific Products:

View All Isoforms

μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

Biological Activity
Purity & Documentation
References
Customer Review

Description

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]

In Vitro

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.

In Vivo

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.

Molecular Weight

401.54

Formula

C₂₆H₃₁N₃O

CAS No.

280783-56-4

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

Animal weight
(per animal)

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.

Purity & Documentation

Purity: 99.82%

Select Batch:

Data Sheet (281 KB) SDS (251 KB)

COA (258 KB) HNMR (142 KB) RP-HPLC (140 KB) LCMS (204 KB)

Handling Instructions (2659 KB)

References

[1]. Shoblock JR. The pharmacology of Ro 64-6198, a systemically active, nonpeptide NOP receptor (opiate receptor-like 1, ORL-1) agonist with diverse preclinical therapeutic activity. CNS Drug Rev. 2007 Spring;13(1):107-36. [Content Brief]

[2]. Chang SD, et al. Novel Synthesis and Pharmacological Characterization of NOP Receptor Agonist 8-[(1S,3aS)-2,3,3a,4,5,6-Hexahydro-1H-phenalen-1-yl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one (Ro 64-6198). ACS Chem Neurosci. 2015 Dec 16;6(12):1956-64. [Content Brief]

Complete Stock Solution Preparation Table

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

Ro 64-6198 Related Classifications

Neurological Disease

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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Ro 64-6198

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Ro 64-6198 Related Antibodies

1 Publications Citing Use of MCE Ro 64-6198

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•Related Screening Libraries:

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References

Customer Review

Ro 64-6198 Related Antibodies

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Complete Stock Solution Preparation Table

Ro 64-6198 Related Classifications

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