| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| ln Vitro |
CYP2Ds in rats or mice are not inhibited by coroplastine A. While it has a minor inhibitory effect on 2B6 and 2E1, coroprine A exhibits no inhibitory activity against human recombinant CYP1A2, 2A6, 2C8, 2C19, 3A4, or 3A5. Guanfu basic A has strong CYP2D6 inhibitory effects, as evidenced by its IC50 values of roughly 0.46 μM in HLM (dextromethorphan 5 μM) and 0.12 μM in rCYP2D6 (bufurolol 5 μM) [1]. The whole-cell patch-clamp approach was employed to investigate the function of guanfu base A in human embryonic kidney 293 (HEK293) cells that were transiently transfected with HERG complementary DNA. With an IC50 of 1.64 mM, guanfu base A suppresses HERG channel current in a concentration-, voltage-, and time-dependent manner. While having no influence on the inactivation curve, coroplastine A accelerates channel inactivation and alters the activation curve in a negative direction [2].
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| ln Vivo |
Coronaphylline was administered beforehand to Beagle dogs. Dextromethorphan (2 mg/mL) is administered intravenously and as an injection. The metabolic activity of CYP2D was decreased. Dextrorphan had a Cmax that was one-third that of the group receiving regular saline therapy. Plasma concentration-time Comparing the area under the curve to the saline treatment group, it was half [1].
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| References |
[1]. Sun J, et al. Guanfu base A, an antiarrhythmic alkaloid of Aconitum coreanum, Is a CYP2D6 inhibitor of human, monkey, and dog isoforms. Drug Metab Dispos. 2015 May;43(5):713-24.
[2]. Huang X, et al. Comparative effects of Guanfu base A and Guanfu base G on HERG K+ channel. J Cardiovasc Pharmacol. 2012 Jan;59(1):77-83. |
| Molecular Formula |
C24H31NO6
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|---|---|
| Molecular Weight |
429.5060
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| CAS # |
1394-48-5
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| SMILES |
O[C@@]12[C@]3([H])[C@]45C[C@H](C[C@]6(C)CN3[C@@]([H])(C[C@]31CC(=C)[C@@]([H])(C2OC(C)=O)[C@H]([C@@]43[H])O)[C@@]56[H])OC(C)=O
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~100 mg/mL (~232.82 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.82 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 (5.82 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 (5.82 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 | 2.3282 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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