SR17018

Name: SR17018
Brand: MedChemExpress
SKU: HY-111454
Rating: 4.5 (1 reviews)

Art. -Nr.: HY-111454 Reinheit: 99.22%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

SR17018 is an mu-opioid-receptor (MOR) agonist, binding with GTPγS, with an EC₅₀ of 97 nM.

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SR17018 Chemische Struktur

CAS. Nr. : 2134602-45-0

Größe	Verfügbarkeit	Menge
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	Auf Lager	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	Auf Lager	Estimated Time of Arrival: December 31
Solid
5 mg	Auf Lager	Estimated Time of Arrival: December 31
10 mg	Auf Lager	Estimated Time of Arrival: December 31
25 mg	Auf Lager	Estimated Time of Arrival: December 31
50 mg	Auf Lager	Estimated Time of Arrival: December 31
100 mg	Auf Lager	Estimated Time of Arrival: December 31
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500 mg	Angebot einholen

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

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Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE SR17018

•Authorea. 2021 Jan 10.

Spezialitätsempfehlungen

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Alle Opioid Receptor Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen

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

Biologische Aktivität
Reinheit & Dokumentation
Verweise
Kundenbewertung

Beschreibung

SR17018 is an mu-opioid-receptor (MOR) agonist, binding with GTPγS, with an EC₅₀ of 97 nM.

IC₅₀ & Target

μ Opioid Receptor/MOR

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	97 1 Compound: 27; SR-17018	Agonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay Agonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay	[PMID: 29939744]
CHO	EC₅₀	97 1 Compound: 27; SR-17018	Agonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay Agonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay	[PMID: 29939744]
CHO	EC₅₀	97 1 Compound: 27; SR-17018	Agonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay Agonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay	[PMID: 29939744]
U2OS	EC₅₀	>10 3 Compound: 27; SR-17018	Agonist activity at human mu opioid receptor expressed in human U2OS cells co-transfected with beta-arrestin-2 assessed as increase in beta-arrestin-2 recruitment after 90 mins by BRET assay Agonist activity at human mu opioid receptor expressed in human U2OS cells co-transfected with beta-arrestin-2 assessed as increase in beta-arrestin-2 recruitment after 90 mins by BRET assay	[PMID: 29939744]
U2OS	EC₅₀	> 10000 1 Compound: 27; SR-17018	Agonist activity at human mu opioid receptor expressed in human U2OS cells co-transfected with beta-arrestin-2 assessed as increase in beta-arrestin-2 recruitment after 90 mins by BRET assay Agonist activity at human mu opioid receptor expressed in human U2OS cells co-transfected with beta-arrestin-2 assessed as increase in beta-arrestin-2 recruitment after 90 mins by BRET assay	[PMID: 29939744]
U2OS	EC₅₀	> 10000 1 Compound: 27; SR-17018	Agonist activity at human mu opioid receptor expressed in human U2OS cells co-transfected with beta-arrestin-2 assessed as increase in beta-arrestin-2 recruitment after 90 mins by BRET assay Agonist activity at human mu opioid receptor expressed in human U2OS cells co-transfected with beta-arrestin-2 assessed as increase in beta-arrestin-2 recruitment after 90 mins by BRET assay	[PMID: 29939744]

In Vitro

SR17018 is an mu-opioid-receptor (MOR) agonist, binding with GTPγS, with an EC₅₀ of 97 nM. SR17018 shows no obvious effect on inducing βarrestin2 recruitment to the MOR at below 10 μM. SR17018 promotes signaling through G proteins or βarrestin2^[1].

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

Molekulargewicht

410.72

Formel

C₁₉H₁₈Cl₃N₃O

CAS. Nr.

2134602-45-0

Appearance

Solid

Color

White to off-white

SMILES

O=C1NC2=CC(Cl)=C(Cl)C=C2N1C3CCN(CC4=CC=C(Cl)C=C4)CC3

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 12.5 mg/mL (30.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4347 mL	12.1737 mL	24.3475 mL
5 mM	0.4869 mL	2.4347 mL	4.8695 mL
10 mM	0.2435 mL	1.2174 mL	2.4347 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner
Verdünnungsrechner

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: ≥ 1.25 mg/mL (3.04 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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% Corn Oil
Solubility: ≥ 1.25 mg/mL (3.04 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

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.

Reinheit & Dokumentation

Purity: 99.22%

Select Batch:

Data Sheet (275 KB) SDS (643 KB)

COA (253 KB) HNMR (255 KB) RP-HPLC (263 KB)

Handling Instructions (2659 KB)

Verweise

[1]. Schmid CL, et al. Bias Factor and Therapeutic Window Correlate to Predict Safer Opioid Analgesics. Cell. 2017 Nov 16;171(5):1165-1175.e13. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.4347 mL	12.1737 mL	24.3475 mL	60.8687 mL
	5 mM	0.4869 mL	2.4347 mL	4.8695 mL	12.1737 mL
	10 mM	0.2435 mL	1.2174 mL	2.4347 mL	6.0869 mL
	15 mM	0.1623 mL	0.8116 mL	1.6232 mL	4.0579 mL
	20 mM	0.1217 mL	0.6087 mL	1.2174 mL	3.0434 mL
	25 mM	0.0974 mL	0.4869 mL	0.9739 mL	2.4347 mL
	30 mM	0.0812 mL	0.4058 mL	0.8116 mL	2.0290 mL

SR17018 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:

SR170182134602-45-0SR 17018SR-17018Opioid ReceptorInhibitorinhibitorinhibit

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SR17018

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SR17018 Related Antibodies

1 Publications Citing Use of MCE SR17018

Spezialitätsempfehlungen

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Alle Opioid Receptor Isoform-spezifische Produkte anzeigen:

Biologische Aktivität

Reinheit & Dokumentation

Verweise

Kundenbewertung

SR17018 Related Antibodies

Molaritätsrechner

Verdünnungsrechner

Complete Stock Solution Preparation Table

SR17018 Related Classifications

Keywords:

Ihre kürzlich angesehenen Produkte:

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SAFETY DATA SHEET (SDS)

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