| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Targets |
Pregnenolone sulfate sodium targets multiple receptors and channels. It is a specific inhibitor of cannabinoid CB1 receptor signaling, inhibiting the effects of THC mediated by CB1 receptors. It acts as a GABAA receptor antagonist, a TRPM3 channel activator, and can weakly activate TRPM1 channels. It is also an NMDAR modulator. By interacting with these targets, pregnenolone sulfate sodium modulates neurotransmission, neuroinflammation, and neuroprotection.
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| ln Vitro |
Stimulation of CB1 receptors raises brain pregnenolone levels, which counteracts most of the known physical and behavioral effects of THC by producing negative feedback on CB1 receptor activity. Pregnenolone binds to a different location than the orthosteric ligand, potentially acting as a distinct negative allosteric modulator of signaling. Pregnenolone solely affects agonist efficacy; it has no effect on agonist binding [1]. Slices that had a 100 nM pregnenolone pretreatment showed a considerable reduction in THC's impact (inhibition rate of 15.1±1.8%). Pregnenolone's presynaptic actions could be the cause of these results. Pregnenolone, therefore, does not change the amplitude or decay duration of micro-EPSCs (mEPSCs), but it does suppress the THC-induced rise in paired pulse ratio (PPR) [1].
In vitro, pregnenolone sulfate sodium does not alter agonist binding, but only agonist efficacy. It acts as a specific inhibitor of CB1 receptor signaling, reducing the psychoactive effects of THC. Its activity is characterized by its ability to modulate multiple receptor systems, including CB1, GABAA, NMDA, and TRPM channels. The compound's neurosteroid properties make it a valuable tool for studying neurosteroid signaling and its role in brain function. |
| ln Vivo |
Pregnenolone treatment (2-6 mg/kg) reduces THC-induced food intake in Wistar rats and C57BL/6N mice and attenuates THC-induced memory impairment in mice, but does not change itself these behaviors. Injection of pregnenolone (2 and 4 mg/kg) before each self-administration reduces WIN 55,212-2 consumption and reduces breakpoints in a graduated-ratio regimen [1].
In vivo, pregnenolone sulfate sodium protects the brain from marijuana toxicity. It is a TRPM3 channel activator and can weakly activate TRPM1 channels. As a neurosteroid, it modulates various neurological processes, including stress responses, memory, and pain perception. Its ability to inhibit CB1 receptor signaling suggests potential therapeutic applications for reducing the psychoactive effects of cannabinoids. Specific in vivo efficacy data is not detailed in the provided search results. |
| Enzyme Assay |
The in vitro activity of pregnenolone sulfate sodium is assessed using radioligand binding assays and functional assays. For CB1 receptor studies, cells expressing CB1 receptors are treated with pregnenolone sulfate sodium, and the inhibition of CB1 receptor-mediated signaling (e.g., inhibition of cAMP accumulation) is measured. For GABAA receptor studies, the compound's ability to antagonize GABA-induced chloride influx is measured using electrophysiological techniques or fluorescence-based chloride-sensitive dyes. For TRPM3 channel studies, the compound's ability to activate the channel is assessed by measuring calcium influx using fluorescent dyes.
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| Cell Assay |
For cellular assays, cell lines expressing CB1 receptors, GABAA receptors, or TRPM3 channels are cultured in appropriate media. Cells are treated with various concentrations of pregnenolone sulfate sodium (typically 0.1-100 µM) for defined periods. Receptor activation or inhibition is assessed by measuring changes in intracellular signaling pathways (e.g., cAMP levels, calcium influx). Cell viability is assessed using standard assays.
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| Animal Protocol |
In vivo, pregnenolone sulfate sodium is typically administered via intraperitoneal or intravenous injection in animal models. In studies of cannabinoid toxicity, the compound is administered before or after THC exposure, and the effects on THC-induced behaviors (e.g., hypothermia, catalepsy, analgesia) are assessed. In neurological studies, the compound's effects on stress responses, memory, and pain perception are assessed using behavioral tests.
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| ADME/Pharmacokinetics |
Pregnenolone sulfate sodium has a molecular weight of 418.52 g/mol and a molecular formula of C21H31NaO5S. It is a sodium salt that is soluble in water and DMSO. The compound should be stored as a powder at -20°C under desiccated conditions. Specific pharmacokinetic parameters such as bioavailability, half-life, and volume of distribution are not detailed in the provided search results.
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| Toxicity/Toxicokinetics |
Specific toxicity data for pregnenolone sulfate sodium is not available in the provided search results. As an endogenous neurosteroid, it is generally well-tolerated at physiological levels. The compound is intended for research purposes only and is not approved for human or veterinary use. Standard laboratory safety precautions should be followed when handling the compound. Comprehensive toxicological studies are required to establish its full safety profile.
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| References |
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| Additional Infomation |
Pregnenolone sulfate sodium is an endogenous neurosteroid that plays a role in various neurological processes, including stress responses, memory, and neuroprotection. It is a precursor of all steroid hormones and is found in the brain and other tissues. The compound has been studied for its potential therapeutic applications in neuroprotection, addiction, and neurological disorders. Pregnenolone sulfate sodium is not approved as a pharmaceutical drug but is available as a research compound.
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| Molecular Formula |
C21H31NAO5S
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| Molecular Weight |
418.52
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| Exact Mass |
418.179
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| CAS # |
1852-38-6
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| Related CAS # |
Pregnenolone;145-13-1;Pregnenolone monosulfate;1247-64-9;Pregnenolone monosulfate sodium-13C2,d2;2483824-22-0;Pregnenolone monosulfate-d4 sodium;1485492-21-4
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| PubChem CID |
23676306
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| Appearance |
White to off-white solid powder
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| Melting Point |
192ºC(lit.)
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| LogP |
5.08
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
28
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| Complexity |
772
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| Defined Atom Stereocenter Count |
7
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| SMILES |
CC(=O)[C@H]1CC[C@@H]2[C@@]1(CC[C@H]3[C@H]2CC=C4[C@@]3(CC[C@@H](C4)OS(=O)(=O)[O-])C)C.[Na+]
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| InChi Key |
QQVJEIZJHDPTSH-UTNKIXDHSA-M
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| InChi Code |
InChI=1S/C21H32O5S.Na/c1-13(22)17-6-7-18-16-5-4-14-12-15(26-27(23,24)25)8-10-20(14,2)19(16)9-11-21(17,18)3;/h4,15-19H,5-12H2,1-3H3,(H,23,24,25);/q;+1/p-1/t15-,16-,17+,18-,19-,20-,21+;/m0./s1
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| Chemical Name |
sodium;[(3S,8S,9S,10R,13S,14S,17S)-17-acetyl-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-yl] sulfate
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| Synonyms |
Pregnenolone sulfate sodium salt; Pregnenolone sulfate sodium
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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, avoid exposure to moisture. |
| 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 (~238.94 mM)
H2O : ~5 mg/mL (~11.95 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.97 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 (5.97 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 (5.97 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 | 2.3894 mL | 11.9469 mL | 23.8937 mL | |
| 5 mM | 0.4779 mL | 2.3894 mL | 4.7787 mL | |
| 10 mM | 0.2389 mL | 1.1947 mL | 2.3894 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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