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| Targets |
Songorine is a GABAA receptor antagonist. By blocking the GABAA receptor, the primary inhibitory neurotransmitter receptor in the brain, Songorine exerts a stimulant effect on the CNS. It also functions as an adrenergic and serotonergic stimulant. Its antiarrhythmic activity is likely related to its effects on ion channels and neurotransmitter systems.
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| ln Vitro |
In vitro, Songorine acts as a GABAA receptor antagonist with an IC50 of 7.06 µM in rat brain. It has been shown to have potential for the treatment of epithelial ovarian cancer (EOC). Its effects on GABAergic neurotransmission and cancer cell lines have been studied.
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| ln Vivo |
Songorine's efficacy and safety were investigated in BALB/c nude mice having SKOV3 tumors. In addition to promoting EOC cell apoptosis and suppressing mammalian EOC tumorigenic activity, songorine reduces EOC cell survival, invasion, and migration. Furthermore, the results of Western blot and IHC demonstrated that songorine consistently up-regulated the expression of Ecadherin, cleaved caspase3, cleaved caspase9, and Bax and continuously down-regulated the expression of Ncadherin, vimentin, matrix metalloproteinase (MMP) 2, MMP9, phosphorylated GSK3β, βcatenin, and Bcl2 [1]. In the aconitine-induced rat arrhythmia paradigm, songorine exhibited antiarrhythmic action, with LD50 and ED50 values of 142 mg and 7.3 mg, respectively [2].
In vivo, Songorine is a CNS stimulant. It has antiarrhythmic activities and has been studied for its potential in treating epithelial ovarian cancer. However, detailed in vivo efficacy data for specific disease models are limited. The compound is primarily used as a research tool. |
| Enzyme Assay |
In vitro receptor binding assays for Songorine typically measure its affinity for the GABAA receptor. Radioligand binding studies using membrane preparations from rat brain are performed to determine the IC50 for inhibiting the binding of a GABAA receptor ligand.
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| Cell Assay |
In vitro cellular assays for Songorine involve treating neuronal cell lines with the compound and measuring its effects on GABA-induced chloride currents using patch-clamp electrophysiology. The compound's antiproliferative effects on cancer cell lines can also be assessed.
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| Animal Protocol |
In vivo animal models for Songorine may include models of cardiac arrhythmia to evaluate its antiarrhythmic activity or models of cancer to assess its antitumor effects. However, detailed animal protocol information is limited. The compound is primarily used as a research tool.
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| ADME/Pharmacokinetics |
Songorine has a molecular formula of C22H31NO3 and a molecular weight of 357.49 g/mol. Its chemical name is (1a,15b)-21-Ethyl-1,15-dihydroxy-4-methyl-16-methylene-7,20-cycloveatchan-12-one. It is a C20-diterpenoid alkaloid from Aconitum species. The compound is typically stored as a powder at -20°C.
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| Toxicity/Toxicokinetics |
Songorine is a diterpenoid alkaloid with a well-characterized mechanism of action as a GABAA receptor antagonist. As with any alkaloid, potential toxicity may include effects on the CNS and cardiovascular system. The compound is for research use only and is not approved for human therapeutic use. It should be handled with appropriate safety precautions.
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| References | |
| Additional Infomation |
Bullatine G is a coalkyl diterpenoid compound. It has been reported that Songorine exists in Aconitum monticola, Aconitum kongboense, and other organisms with relevant data.
Songorine (CAS# 509-24-0) is a C20-diterpenoid alkaloid from Aconitum species. It is a GABAA receptor antagonist, a CNS stimulant, and has antiarrhythmic activity. The compound has potential for cancer research and is for research use only. It is not approved for human therapeutic use. |
| Molecular Formula |
C22H31NO3
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|---|---|
| Molecular Weight |
357.494
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| Exact Mass |
357.23
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| CAS # |
509-24-0
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| PubChem CID |
71456946
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| Appearance |
White to off-white solid powder
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| Density |
1.29
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| Boiling Point |
535.8±50.0 °C at 760 mmHg
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| Melting Point |
201-203ºC
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| Flash Point |
277.8±30.1 °C
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| Vapour Pressure |
0.0±3.2 mmHg at 25°C
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| Index of Refraction |
1.630
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| LogP |
0.71
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
26
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| Complexity |
735
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| Defined Atom Stereocenter Count |
10
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| SMILES |
CCN1C[C@@]2(CC[C@@H]([C@@]34[C@@H]2C[C@@H]([C@H]31)[C@]56[C@H]4CC(=O)[C@H](C5)C(=C)[C@H]6O)O)C
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| InChi Key |
CBOSLVQFGANWTL-DVPYZRQCSA-N
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| InChi Code |
InChI=1S/C22H31NO3/c1-4-23-10-20(3)6-5-17(25)22-15(20)7-13(18(22)23)21-9-12(11(2)19(21)26)14(24)8-16(21)22/h12-13,15-19,25-26H,2,4-10H2,1,3H3/t12-,13+,15-,16-,17+,18-,19-,20+,21+,22+/m1/s1
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| Chemical Name |
(1R,2R,5R,7R,8R,9R,10R,13R,16S,17R)-11-ethyl-7,16-dihydroxy-13-methyl-6-methylidene-11-azahexacyclo[7.7.2.15,8.01,10.02,8.013,17]nonadecan-4-one
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| Synonyms |
BRN 0045107; BRN-0045107; Songorine
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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 : ~100 mg/mL (~279.73 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.99 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 (6.99 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 (6.99 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 | 2.7973 mL | 13.9864 mL | 27.9728 mL | |
| 5 mM | 0.5595 mL | 2.7973 mL | 5.5946 mL | |
| 10 mM | 0.2797 mL | 1.3986 mL | 2.7973 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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