| Size | Price | |
|---|---|---|
| Other Sizes |
| Targets |
Not well characterized; potential targets include central nervous system pathways involved in sleep, anxiety, and pain modulation. As a natural phenolic glycoside, Helicid may interact with neurotransmitter systems (e.g., GABAergic, serotonergic) to exert its sedative, hypnotic, and analgesic effects. Further target identification studies are needed.
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|---|---|
| ln Vitro |
In vitro bioactivity data is limited. As a natural phenolic glycoside from Helicia nilgirica, Helicid may exhibit sedative, hypnotic, and analgesic activities. Quantitative in vitro activity data (e.g., IC50 values) and specific bioactivity assays are not readily available in public literature.
|
| ln Vivo |
Injection-administered Helicid (8–32 mg/kg; once daily for 6 weeks) dramatically counteracts depressive-like behavior in rats generated by chronic unpredictable mild stress (CUMS) [1].
In vivo, Helicid has been studied for its potential to promote tranquility, sleep, and relieve pain. It may be utilized in research related to psychoneurosis. Detailed dose-response and pharmacokinetic data in animal models are limited in publicly available literature. |
| Enzyme Assay |
No specific cell-free enzyme/receptor binding assay protocol is detailed for Helicid. For phenolic glycosides, typical cell-free assays include receptor binding studies using radioligands for CNS targets (e.g., GABA-A, 5-HT1A, opioid receptors) or enzyme inhibition assays.
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| Cell Assay |
Cellular activity is assessed in neuronal cell lines or primary neurons. Cells are treated with Helicid, and endpoints include neurotransmitter release measurement, calcium imaging, and receptor activation assays (e.g., cAMP accumulation, IP3 accumulation). However, specific protocols for Helicid are not detailed in publicly available sources.
|
| Animal Protocol |
Animal/Disease Models: CUMS-induced depression rat model [1]
Doses: 8 mg/kg, 16 mg/kg, 32 mg/kg Route of Administration: ig; one time/day for 6 weeks Experimental Results: Improvement of CUMS-induced rats Depressive-like behavior. In vivo efficacy is evaluated in rodent models of insomnia, anxiety, or pain. Helicid is administered via oral gavage or intraperitoneal injection. Endpoints include sleep parameters (EEG, duration), behavioral tests (elevated plus maze, open field test, tail flick test), and neurotransmitter levels in brain tissue. |
| ADME/Pharmacokinetics |
Molecular weight: 284.26 g/mol; molecular formula: C13H16O7. Purity: typically ≥98% for research use. Appearance: white to off-white powder. Optical rotation: α = -27° (c=3.2, MeOH). Solubility: soluble in hot water, slightly soluble in water, ethanol or methanol, insoluble in ether or chloroform. Storage: 2-8°C.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is publicly available. As a natural phenolic glycoside from a medicinal herb, it is likely to have low toxicity, but standard toxicological studies would be required for drug development.
|
| References | |
| Additional Infomation |
Helicid is a glycoside. It has been reported that Helicia nilagirica, Canella winterana, and Citrullus colocynthis contain helicidide, and relevant data are available for reference.
Helicid is a research-grade compound, not approved for therapeutic use. It is primarily used as a reference standard and for pharmacological research in neuroscience, sleep, and pain. No clinical trials have been reported. It is a natural product from Helicia nilgirica used in traditional medicine for promoting tranquility and sleep. |
| Molecular Formula |
C13H16O7
|
|---|---|
| Molecular Weight |
284.2619
|
| Exact Mass |
284.089
|
| CAS # |
80154-34-3
|
| PubChem CID |
12896796
|
| Appearance |
White to off-white solid powder
|
| Density |
1.5±0.1 g/cm3
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| Boiling Point |
559.9±50.0 °C at 760 mmHg
|
| Melting Point |
199-200°C
|
| Flash Point |
215.8±23.6 °C
|
| Vapour Pressure |
0.0±1.6 mmHg at 25°C
|
| Index of Refraction |
1.651
|
| LogP |
-1.04
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
20
|
| Complexity |
316
|
| Defined Atom Stereocenter Count |
5
|
| SMILES |
C1=CC(=CC=C1C=O)O[C@H]2[C@@H]([C@@H]([C@@H]([C@H](O2)CO)O)O)O
|
| InChi Key |
OLZAGZCCJJBKNZ-SYLRKERUSA-N
|
| InChi Code |
InChI=1S/C13H16O7/c14-5-7-1-3-8(4-2-7)19-13-12(18)11(17)10(16)9(6-15)20-13/h1-5,9-13,15-18H,6H2/t9-,10-,11-,12-,13-/m1/s1
|
| Chemical Name |
4-[(2S,3R,4R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxybenzaldehyde
|
| 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) |
DMSO : ~110 mg/mL (~386.97 mM)
H2O : ~4.58 mg/mL (~16.11 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (9.67 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 27.5 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: ≥ 2.75 mg/mL (9.67 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 27.5 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: ≥ 2.75 mg/mL (9.67 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 6.67 mg/mL (23.46 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5179 mL | 17.5895 mL | 35.1791 mL | |
| 5 mM | 0.7036 mL | 3.5179 mL | 7.0358 mL | |
| 10 mM | 0.3518 mL | 1.7590 mL | 3.5179 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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