| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
BNTX is highly selective for δ1 opioid receptors in the meninges of guinea pigs, with an affinity for the δ1 site that is 100 times greater than that for the δ2 site [1].
|
|---|---|
| ln Vivo |
BNTX (1.3 μmol/kg; subcutaneous injection; single dose; 1 pmol/mouse; intrathecal injection; single dose) acts as a highly selective δ1 opioid receptor antagonist in the spinal cord of mice and significantly increases the analgesic ED50 of the δ1 receptor agonist DPDPE[1].
|
| Animal Protocol |
Animal/Disease Models:ND4 Swiss-Webster (male, 20-25 g) [1]
Doses: 1.3 μmol/kg (subcutaneous pretreatment); 1 pmol/mouse (intravenous pretreatment) Route of Administration: Subcutaneous injection; single dose, 30 minutes before agonist test; intravenous injection; single dose, 10 minutes before agonist test Experimental Results: At a subcutaneous dose of 1.3 μmol/kg, the analgesic ED50 of the δ1 agonist DPDPE (intravenous) increased from 6.3 nmol/mouse to 36.1 nmol/mouse. At a subcutaneous dose of 1.3 μmol/kg, the analgesic ED50 of the δ2 receptor agonist DELT II (it), the μ receptor agonist DAMGO and morphine (it) or the κ receptor agonist U-50,488H (it) did not change significantly. Subcutaneous injection of a 1 pmol/mouse dose increased the analgesic ED50 value of DPDPE (it) from 6.3 nmol/mouse to 25.5 nmol/mouse. Subcutaneous injection of a 1 pmol/mouse dose did not significantly alter the analgesic ED50 values of DELT II (it), the μ-receptor agonist DAMGO (it), or the κ-receptor agonist U-50,488H (it). |
| References |
| Molecular Formula |
C27H27NO4
|
|---|---|
| Molecular Weight |
429.51
|
| CAS # |
129468-28-6
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O[C@]12[C@@]34C5=C(C[C@@]2([H])N(CC4)CC6CC6)C=CC(O)=C5O[C@@]3([H])C(/C(C1)=C\C7=CC=CC=C7)=O
|
| Synonyms |
7-Benzylidenenaltrexone
|
| 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)
|
| 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
|
|---|---|
| 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 | 2.3282 mL | 11.6412 mL | 23.2823 mL | |
| 5 mM | 0.4656 mL | 2.3282 mL | 4.6565 mL | |
| 10 mM | 0.2328 mL | 1.1641 mL | 2.3282 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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