Nociceptin (1-13), amide TFA is a potent opioid receptor ORL1 (OP4) receptor agonist/activator with pEC50 of 7.9 for mouse vas deferens and a Ki of 0.75 nM for rat forebrain membrane binding.

Physicochemical Properties

Molecular Formula	C63H101F3N22O17
Molecular Weight	1495.61
Related CAS #	Nociceptin (1-13), amide;178064-02-3
Appearance	Solid powder
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	NOP Receptor/ORL1
References	[1]. Nociceptin receptor binding in mouse forebrain membranes: thermodynamic characteristics and structure activity relationships. Br J Pharmacol. 1998 Dec;125(7):1485-90. [2]. Pharmacology of nociceptin and its receptor: a novel therapeutic target. Br J Pharmacol. 2000 Apr;129(7):1261-83.

Solubility Data

Solubility (In Vitro)

DMSO :≥ 100 mg/mL (~66.86 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (1.67 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (1.67 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (1.67 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	0.6686 mL	3.3431 mL	6.6862 mL
	5 mM	0.1337 mL	0.6686 mL	1.3372 mL
	10 mM	0.0669 mL	0.3343 mL	0.6686 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.