| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
NOP Receptor/ORL1
SB-612111 hydrochloride selectively targets the NOP receptor (nociceptin/orphanin FQ receptor). It acts as a competitive antagonist at this receptor. Its Ki values are 0.33 nM for the NOP receptor, 57.6 nM for the micro-opioid receptor, 160.5 nM for the kappa-opioid receptor, and 2109 nM for the delta-opioid receptor, demonstrating excellent selectivity for the NOP subtype. |
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| ln Vitro |
SB-612111 hydrochloride is a selective antagonist of NOP receptors that mediate GIRK channel activation. An in vitro study on rat periaqueductal gray slices showed that SB-612111 is a potent (IC50: 87.7 nM), selective, competitive antagonist of NOP receptors. It effectively antagonizes the pronociceptive action of nociceptin in pain models.
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| 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].
In vivo, SB-612111 hydrochloride blocks hyperalgesia in an inflammatory pain model and potentiates the action of morphine in morphine-tolerant animals. These results indicate that it can antagonize the effects of endogenous nociceptin, thereby enhancing opioid analgesic efficacy. This makes it a valuable tool for studying the interaction between the NOP and opioid systems in pain pathways and for exploring therapeutic strategies for pain and opioid tolerance. |
| Enzyme Assay |
A typical radioligand binding assay is used to determine NOP receptor affinity. Membranes from CHO cells expressing the human NOP receptor are incubated with [3H]-nociceptin (0.5-2 nM) in the presence of increasing concentrations (0.01-10000 nM) of SB-612111 hydrochloride in binding buffer. Non-specific binding is determined using 10 uM unlabeled nociceptin. After incubation at 25degC for 60 min, bound radioligand is separated by filtration through GF/B filters. The IC50 is calculated, and the Ki is determined using the Cheng-Prusoff equation.
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| Cell Assay |
SB-612111 hydrochloride is used in cell-based functional assays to measure NOP receptor antagonism. Cells expressing the human NOP receptor are loaded with a calcium-sensitive fluorescent dye (e.g., Fluo-4 AM). Cells are pre-incubated with varying concentrations of SB-612111 hydrochloride (0.1-1000 nM) for 10-15 min. The NOP agonist nociceptin (10-50 nM) is then added, and the change in intracellular calcium is measured using a fluorescence plate reader. The IC50 for antagonism is calculated from the inhibition of the calcium response.
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| 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. The compound can be tested in a mouse model of acute pain, such as the tail-flick or hot plate test. Male Swiss-Webster mice (20-30 g) are pre-treated with SB-612111 hydrochloride (0.1-10 mg/kg) via intraperitoneal (i.p.) or subcutaneous (s.c.) injection. After 15-30 min, baseline latencies are recorded. Nociceptin (1-10 ug/mouse) is then administered i.c.v. (intracerebroventricularly), and latency is re-measured. SB-612111 is expected to reverse the pronociceptive action of nociceptin, which is measured as a decrease in tail-flick latency. |
| ADME/Pharmacokinetics |
SB-612111 hydrochloride has a molecular weight of 454.86 and the molecular formula C24H29Cl2NO.HCl. It should be stored at -20degC in a sealed container. The compound is soluble in DMSO at a maximum concentration of 45.49 mg/mL (100 mM) and in ethanol at 22.74 mg/mL (50 mM). For in vivo studies, it is typically formulated in DMSO or a saline-based vehicle.
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| Toxicity/Toxicokinetics |
Detailed toxicity data are not provided. As a highly selective NOP receptor antagonist, its primary safety concerns are related to the potential blockade of endogenous nociceptin signaling, which may influence pain perception, stress responses, and reward pathways. In animal studies, it was well-tolerated at the doses used (0.1-10 mg/kg). No significant acute toxicity was observed. Standard safety precautions for handling research chemicals should be followed.
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| References | |
| Additional Infomation |
SB-612111 hydrochloride is a research-grade compound and is not approved for clinical use. It is a potent and selective NOP receptor antagonist that has been invaluable for understanding the physiological role of the nociceptin system, particularly in pain modulation and opioid tolerance. It is sold under a license from GlaxoSmithKline for research purposes only. This product is for research use only and not for human therapeutic applications.
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| Molecular Formula |
C24H30CL3NO
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|---|---|
| Molecular Weight |
454.86
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| Exact Mass |
453.139
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| Related CAS # |
rel-SB-612111 hydrochloride;371980-94-8;SB-612111;371980-98-2
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| PubChem CID |
21061234
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
29
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| Complexity |
485
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC1=C2CC[C@@H](C[C@@H](C2=CC=C1)O)CN3CCC(CC3)C4=C(C=CC=C4Cl)Cl.Cl
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| InChi Key |
DCKUVQADDNMWEF-DQFHVVJASA-N
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| InChi Code |
InChI=1S/C24H29Cl2NO.ClH/c1-16-4-2-5-20-19(16)9-8-17(14-23(20)28)15-27-12-10-18(11-13-27)24-21(25)6-3-7-22(24)26;/h2-7,17-18,23,28H,8-15H2,1H3;1H/t17-,23-;/m0./s1
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| Chemical Name |
(5S,7S)-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-1-methyl-6,7,8,9-tetrahydro-5H-benzo[7]annulen-5-ol;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO :~15.62 mg/mL (~34.34 mM)
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| 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. View More
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. |
| 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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