GR103545 fumarate

Name: GR103545 fumarate
Brand: MedChemExpress
SKU: HY-145128
Rating: 4.5 (0 reviews)

Cat. No.: HY-145128 Pureza: 99.75%: Ficha de datos
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GR103545 is a potent and selective agonist of the κ-opioid receptor (κ-OR). ¹¹GR103545 is a radiotracer for imaging κ-OR in vivo^[1]

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GR103545 fumarate Estructura química

No. CAS : 126766-43-6

Tamaño	Stock	Cantidad
1 mg	En stock	Estimated Time of Arrival: December 31
2 mg	En stock	Estimated Time of Arrival: December 31
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	Obtener un presupuesto	Estimated Time of Arrival: December 31
50 mg	Obtener un presupuesto	Estimated Time of Arrival: December 31
100 mg	Obtener un presupuesto	Estimated Time of Arrival: December 31
200 mg	Obtener un presupuesto
500 mg	Obtener un presupuesto

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Based on 1 Customer Validation

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•Related Screening Libraries:

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•Related Proteins:

Ver todos los productos específicos de isoformas Opioid Receptor:

Ver todas las isoformas

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

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Revisión del cliente

Descripciòn

GR103545 is a potent and selective agonist of the κ-opioid receptor (κ-OR). ¹¹GR103545 is a radiotracer for imaging κ-OR in vivo^[1][2].

IC₅₀ & Target

κ Opioid Receptor/KOR

Peso molecular

530.40

Fòrmula

C₂₃H₂₉Cl₂N₃O₇

No. CAS

126766-43-6

Appearance

Solid

Color

White to off-white

SMILES

OC(/C=C/C(O)=O)=O.ClC(C=C1CC(N2[C@@H](CN(CC2)C(OC)=O)CN3CCCC3)=O)=C(C=C1)Cl

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (188.54 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	1.8854 mL	9.4268 mL	18.8537 mL
5 mM	0.3771 mL	1.8854 mL	3.7707 mL
10 mM	0.1885 mL	0.9427 mL	1.8854 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculadora de molaridad
Calculadora de dilución

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 (4.71 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 (4.71 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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.

Pureza y Documentación

Purity: 99.75%

Select Batch:

Ficha de datos (271 KB) SDS (252 KB)

COA (248 KB) HNMR (185 KB) LCMS (153 KB)

Instrucciones de manejo (2659 KB)

Referencias

[1]. Hayes AG, et, al. A series of novel, highly potent and selective agonists for the kappa-opioid receptor. Br J Pharmacol. 1990 Dec;101(4):944-8. [Content Brief]

[2]. Talbot PS, et, al. 11C-GR103545, a radiotracer for imaging kappa-opioid receptors in vivo with PET: synthesis and evaluation in baboons. J Nucl Med. 2005 Mar;46(3):484-94. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.8854 mL	9.4268 mL	18.8537 mL	47.1342 mL
	5 mM	0.3771 mL	1.8854 mL	3.7707 mL	9.4268 mL
	10 mM	0.1885 mL	0.9427 mL	1.8854 mL	4.7134 mL
	15 mM	0.1257 mL	0.6285 mL	1.2569 mL	3.1423 mL
	20 mM	0.0943 mL	0.4713 mL	0.9427 mL	2.3567 mL
	25 mM	0.0754 mL	0.3771 mL	0.7541 mL	1.8854 mL
	30 mM	0.0628 mL	0.3142 mL	0.6285 mL	1.5711 mL
	40 mM	0.0471 mL	0.2357 mL	0.4713 mL	1.1784 mL
	50 mM	0.0377 mL	0.1885 mL	0.3771 mL	0.9427 mL
	60 mM	0.0314 mL	0.1571 mL	0.3142 mL	0.7856 mL
	80 mM	0.0236 mL	0.1178 mL	0.2357 mL	0.5892 mL
	100 mM	0.0189 mL	0.0943 mL	0.1885 mL	0.4713 mL