SB-612111 HCl is a new and highly effective opioid receptor orphan receptor (ORL-1) antagonist (inhibitor) with high affinity for hORL-1 (Ki=0.33 nM). The Kis of SB-612111 HCl for μ-, κ- and δ-receptors are 57.6 nM, 160.5 nM and 2109 nM respectively. SB-612111 HCl effectively antagonizes the nociceptin-induced nociceptive effects in acute pain models.

Physicochemical Properties

Molecular Formula	C24H30CL3NO
Molecular Weight	454.86
Related CAS #	rel-SB-612111 hydrochloride;371980-94-8;SB-612111;371980-98-2
Appearance	White to off-white 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
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
ln Vivo	SB-612111 hydrochloride (iv; 0.6-10 nmol/mouse) has an ED50 of 0.62 mg/kg and acts in a dose-dependent manner to counteract nociceptin-induced thermal hyperalgesia[1]. Rats' paw withdrawal latency was dramatically reduced by carrageenan when SB-612111 hydrochloride (intravenous injection; 0.1–5 mg/kg) was administered; untreated paws showed no effect [1].
Animal Protocol	Animal/Disease Models: Male rats[1] Doses: 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 5 mg/kg Route of Administration: intravenous (iv) injection; single dose Experimental Results: Had antihyperalgesic effects on carrageenan-induced rat paw.
References	[1]. Modification of Nociception and Morphine Tolerance by the Selective Opiate Receptor-Like Orphan Receptor Antagonist (-)-cis-1-methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol (SB-612111 hydrochloride).J Pharmacol Exp Ther. 2004 Feb;308(2):454-61.

Solubility Data

Solubility (In Vitro)

DMSO :~15.62 mg/mL (~34.34 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (5.50 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 (5.50 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 (5.50 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	2.1985 mL	10.9924 mL	21.9848 mL
	5 mM	0.4397 mL	2.1985 mL	4.3970 mL
	10 mM	0.2198 mL	1.0992 mL	2.1985 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.