| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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Bulleyaconitine A (also known as Bulleyaconi cine A) is a potent analgesic and antiinflammatory drug isolated from aconitum plant displays long-acting local anesthetic properties in vitro and in vivo.
| ln Vitro |
BLA at 10 μM did not affect neuronal Na+ currents in clonal GH3 cells when stimulated infrequently to +50 mV. When stimulated at 2 Hz for 1,000 pulses (+50 mV for 4 ms), BLA reduced the peak Na+ currents by >90%. This use-dependent reduction of Na+ currents by BLA reversed little after washing. [2]
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| ln Vivo |
Single injections of BLA (0.2 ml at 0.375 mM) into the rat sciatic notch not only blocked sensory and motor functions of the sciatic nerve but also induced hyperexcitability, followed by sedation, arrhythmia, and respiratory distress. When BLA at 0.375 mM was co-injected with 2% lidocaine (~80 mM) or epinephrine (1:100,000) to reduce drug absorption by the blood-stream, the sensory and motor functions of the sciatic nerve remained fully blocked for ~4 hrs and regressed completely after ~7 hrs with minimal systemic effects.[2]
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| Animal Protocol |
At the time of injection, rats weighed approximately 250–300g. All rats were anesthetized by inhalation of a small amount of sevoflurane . After induction of inhalation anesthesia, BLA in a volume of 200 μl was injected at the sciatic notch of the left hind limb with a 27-G needle connected to a tuberculin syringe. BLA at a 50 mM stock solution was diluted in 0.9% NaCl saline, in 2% lidocaine, or in (1:100,000) epinephrine solution. The final BLA concentrations were 0.375 mM and 0.75 mM. All drug solutions were freshly prepared before injections, and the pH ranged from 5.0 to 6.5 (the pH was not adjusted because it was buffered quickly by the pH of 7.4 of the tissue fluid).[2]
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| References |
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| Molecular Formula |
C35H49NO9
|
|---|---|
| Molecular Weight |
627.7649
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| Exact Mass |
627.34
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| CAS # |
107668-79-1
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| PubChem CID |
45358113
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
690.9±55.0 °C at 760 mmHg
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| Flash Point |
371.7±31.5 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.590
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| LogP |
1.05
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
45
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| Complexity |
1180
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| Defined Atom Stereocenter Count |
13
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| SMILES |
CCN1C[C@@]2(CC[C@H]([C@@]34[C@@H]2[C@H]([C@@H]([C@H]31)[C@]5(C[C@@H]([C@]6(C[C@@H]4[C@@H]5[C@H]6C(=O)C7=CC=C(C=C7)OC)O)OC)OC(=O)C)OC)OC)COC
|
| InChi Key |
YRECILNLFWZVRM-XTNYDWJGSA-N
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| InChi Code |
InChI=1S/C35H49NO9/c1-8-36-17-32(18-40-3)14-13-23(42-5)35-22-15-33(39)24(43-6)16-34(45-19(2)37,27(31(35)36)29(44-7)30(32)35)25(22)26(33)28(38)20-9-11-21(41-4)12-10-20/h9-12,22-27,29-31,39H,8,13-18H2,1-7H3/t22-,23-,24+,25-,26+,27+,29+,30-,31-,32+,33+,34-,35+/m1/s1
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| Chemical Name |
[(1S,2R,3R,4R,5R,6S,8R,9R,10R,13S,16R,17R,18R)-11-ethyl-5-hydroxy-6,16,18-trimethoxy-4-(4-methoxybenzoyl)-13-(methoxymethyl)-11-azahexacyclo[7.7.2.12,5.01,10.03,8.013,17]nonadecan-8-yl] acetate
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~20.83 mg/mL (~33.18 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.31 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 20.8 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: ≥ 2.08 mg/mL (3.31 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 20.8 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: ≥ 2.08 mg/mL (3.31 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 | 1.5930 mL | 7.9648 mL | 15.9297 mL | |
| 5 mM | 0.3186 mL | 1.5930 mL | 3.1859 mL | |
| 10 mM | 0.1593 mL | 0.7965 mL | 1.5930 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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