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| Targets |
TAN67 targets the δ-opioid receptor, specifically the δ1 subtype, with very high affinity and selectivity. It has Ki values of 1.12 nM at δ1, 2320 nM at μ, and 1790 nM at κ receptors. It is a potent and selective nonpeptidic agonist of the δ-opioid receptor. By activating the δ-opioid receptor, it mediates neuroprotective effects.
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| ln Vitro |
On human delta-opioid receptors produced by intact Chinese hamster cells, TAN-67 (SB-205607) dihydrobromide potently (EC50 = 1.72 nM) suppresses the buildup of cAMP induced by forskolin, but not on human mu-opioid receptors. In intact B82 murine fibroblasts, the in vivo effectiveness is minimal (EC50 = 1520 nM) [1].
In vitro, TAN-67 potently suppresses forskolin-induced cAMP accumulation on human delta-opioid receptors produced by intact Chinese hamster cells, with an EC50 of 1.72 nM. It does not affect human mu-opioid receptors. In intact B82 murine fibroblasts, the in vivo effectiveness is minimal (EC50 = 1520 nM). It is a potent and selective nonpeptidic agonist of the δ-opioid receptor with a Ki of 0.647 nM. |
| ln Vivo |
In I/R-induced brain injury, TAN-67 (SB-205607; 1.5-4.5 mg/kg; iv; Once) dihydrobromide decreases cerebral infarct volume [2]. At early time points (6 h), TAN-67 (3 mg/kg; iv; Once; free C57BL/6J candle model) dihydrobromide raises total APP and mature APP.
In vivo, TAN-67 decreases cerebral infarct volume in I/R-induced brain injury in a dose-dependent manner (1.5-4.5 mg/kg, i.v.). At 3 mg/kg (i.v.), it reduces neuronal cell death, increases total APP and mature APP levels, and diminishes β-secretase activity. It also promotes faster functional recovery than vehicle-treated mice. |
| Enzyme Assay |
In vitro receptor binding assays for TAN67 involve measuring affinity for δ, μ, and κ opioid receptors. Membrane preparations from cells expressing recombinant opioid receptors are incubated with radiolabeled ligands and varying concentrations of TAN67. Non-specific binding is determined in the presence of excess unlabeled ligand. Bound radioactivity is collected by filtration and quantified by scintillation counting. Ki values are calculated from competition curves.
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| Cell Assay |
For in vitro cell-based assays, cells expressing human delta-opioid receptors are cultured and treated with TAN67 at various concentrations. Receptor activation is measured by assessing inhibition of forskolin-induced cAMP accumulation. EC50 values are calculated from concentration-response curves. Cell viability is assessed using standard assays.
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| Animal Protocol |
Animal/Disease Models: I/R-induced brain injury in adult C57BL /6J male mice[2]
Doses: 1.5, 3.0 and 4.5 mg/kg Route of Administration: intravenous (iv) (iv)injection; (APPm) level and APP treatment[2]. Experimental Results: Infarct volume was diminished in a dose-dependent manner. Animal/Disease Models: Adult C57BL/6J male I/R brain-injured mice [2] Doses: 3.0 mg/kg Route of Administration: intravenous (iv) (iv)injection; Experimental Results: faster functional recovery than vehicle-treated mice. Reduce neuronal cell death. Animal/Disease Models: Adult C57BL/6J male mouse transient middle cerebral artery occlusion (MCAO) ischemic stroke model [2] Doses: 3.0 mg/kg Route of Administration: intravenous (iv) (iv)injection; intravenous (iv) (iv)injection. Experimental Results: Both total APP and mature APP (APPm) levels increased. β-secretase activity is diminished. In vivo animal studies for TAN67 use rodent models of ischemic stroke. Adult C57BL/6J male mice are subjected to transient middle cerebral artery occlusion (MCAO) to induce I/R-induced brain injury. TAN67 is administered intravenously at doses of 1.5, 3.0, and 4.5 mg/kg. Infarct volume is measured, and functional recovery is assessed. Neuronal cell death and APP levels are evaluated. |
| ADME/Pharmacokinetics |
TAN67 (CAS 1217628-73-3) has a molecular formula of C23H26Br2N2O and a molecular weight of 506.28. It is a white to off-white solid powder. It should be stored under recommended conditions. Detailed pharmacokinetic parameters are not extensively characterized in the available literature.
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| Toxicity/Toxicokinetics |
Specific toxicity data for TAN67 are not extensively provided. As a δ-opioid receptor agonist, it would be expected to have a safety profile related to modulation of opioid signaling. The compound is for research use only and is not for human or clinical use. Standard toxicology assessments would be required for therapeutic development.
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| References |
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| Additional Infomation |
TAN67 (SB-205607) is a potent, selective, non-peptide δ-opioid receptor agonist with neuroprotective effects. It has been studied for its potential in ischemic stroke research. It is the first described non-peptide δ1 opioid receptor agonist. No approved therapeutic status is reported.
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| Molecular Formula |
C23H26BR2N2O
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|---|---|
| Molecular Weight |
506.28
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| Exact Mass |
504.041
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| CAS # |
1217628-73-3
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| PubChem CID |
56972161
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
28
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| Complexity |
510
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CN1CC[C@@]2(CC3=NC4=CC=CC=C4C=C3C[C@H]2C1)C5=CC(=CC=C5)O.Br.Br
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| InChi Key |
GWXFBFMLKRAWEU-YJKXCHRFSA-N
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| InChi Code |
InChI=1S/C23H24N2O.2BrH/c1-25-10-9-23(18-6-4-7-20(26)13-18)14-22-17(12-19(23)15-25)11-16-5-2-3-8-21(16)24-22;;/h2-8,11,13,19,26H,9-10,12,14-15H2,1H3;2*1H/t19-,23+;;/m0../s1
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| Chemical Name |
3-[(4aS,12aR)-2-methyl-1,3,4,5,12,12a-hexahydropyrido[3,4-b]acridin-4a-yl]phenol;dihydrobromide
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| Synonyms |
TAN 67; TAN-67; TAN67
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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 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)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9752 mL | 9.8760 mL | 19.7519 mL | |
| 5 mM | 0.3950 mL | 1.9752 mL | 3.9504 mL | |
| 10 mM | 0.1975 mL | 0.9876 mL | 1.9752 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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