| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Toxicity/Toxicokinetics |
Toxicity Summary
Caulis Calycanthine is a major alkaloid of the Calycanthaceae family and has long been considered a centrally acting convulsant. The convulsive effect of causticine is mediated at least in part by blocking the postsynaptic action of GABA, as evidenced by its inhibitory effect on the binding of the radiolabeled cage-like convulsant [35S]tert-butylbicyclic thiophosphate. This alkaloid inhibited the release of [(3)H]GABA from potassium-stimulated rat hippocampal sections with an ED50 of approximately 21 μM. This effect appears to be moderately selective, as 100 μM callicin had a weak (15%) effect on potassium-stimulated [(3)H]acetylcholine release and no significant effect on the release of [(3)H]D-aspartate from hippocampal and cerebellar sections or [(3)H]glycine from spinal cord sections. Calicane blocked L-type calcium currents with an IC50 value of approximately 42 μM and also showed a weak inhibitory effect on N-type calcium currents in neuroblastoma X glioma cells (IC50 > 100 μM), suggesting that voltage-dependent calcium channel blockade may be its possible mechanism for inhibiting GABA and ACh release. The study found that calicane directly inhibited the GABA-mediated current of human α1β2γ2L GABA(A) receptors expressed in Xenopus laevis oocytes (K(B) approximately 135 μM), but had no effect on human p1 GABA(c) receptors at a concentration of 100 μM. Calicane may exert its spastic effect mainly through interaction with L-type Ca(2+) channels, inhibiting the release of the inhibitory neurotransmitter GABA, and inhibiting GABA-mediated chloride currents of GABA(A) receptors. Furthermore, researchers used giant axons from the American cockroach (Periplaneta americana) to investigate the effects of this alkaloid on the generation, conduction, and transmission of nerve impulses. Calicutine hydrochloride (10⁻⁵ M) does not alter neurotransmission in presynaptic and postsynaptic fibers, but it significantly reduces the efficiency of synaptic transmission. (PMID: 1653964; PMID: 12831783) |
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| References | |
| Additional Infomation |
LSM-6401 is an aminoquinoline compound. (+)-Calicantine is found in herbs and spices. (+)-Calicantine is an alkaloid extracted from Calycanthus floridus (also known as Carolina's allspice) and other plants in the Calycanthus genus. (+)-Calicantine belongs to the naphthidine class of compounds. These compounds contain naphthidine structural units, i.e., structures in which two carbon atoms on a naphthalene ring are replaced by nitrogen atoms. The naphthidine skeleton can also be described as two fused pyridine rings that do not share a nitrogen atom. See also: Calicantine (note moved to).
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| Molecular Formula |
C22H26N4
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|---|---|
| Molecular Weight |
346.4686
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| Exact Mass |
346.216
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| CAS # |
595-05-1
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| PubChem CID |
264115
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.29g/cm3
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| Boiling Point |
531.8ºC at 760mmHg
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| Melting Point |
245° (evac tube)
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| Flash Point |
310.3ºC
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| Index of Refraction |
1.711
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| LogP |
3.188
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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 |
0
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| Heavy Atom Count |
26
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| Complexity |
531
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
XSYCDVWYEVUDKQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H26N4/c1-25-13-11-22-16-8-4-5-9-17(16)23-19(25)21(22)12-14-26(2)20(22)24-18-10-6-3-7-15(18)21/h3-10,19-20,23-24H,11-14H2,1-2H3
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| Chemical Name |
21,24-dimethyl-3,12,21,24-tetrazahexacyclo[9.7.3.32,10.01,10.04,9.013,18]tetracosa-4,6,8,13,15,17-hexaene
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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 (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 (~288.63 mM)
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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 | 2.8863 mL | 14.4313 mL | 28.8625 mL | |
| 5 mM | 0.5773 mL | 2.8863 mL | 5.7725 mL | |
| 10 mM | 0.2886 mL | 1.4431 mL | 2.8863 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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