| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Cannabinoid CB1 receptor (signaling-specific inhibitor); TRPM1 channels (weak activator).
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|---|---|
| ln Vitro |
CB1 receptor stimulation increases brain pregnenolone levels, which in turn causes negative feedback on CB1 receptor activity and antagonizes most of the known behavioral and physical effects of THC. Pregnenolone may operate as a particular negative allosteric modulator of signaling, binding to a different location than that occupied by the orthosteric ligand. Pregnenolone does not modify agonist binding but only agonist effectiveness [1]. When slices were pretreated with 100 nM pregnenolone, the impact of THC was dramatically decreased (inhibition rate 15.1±1.8%). These effects may be related to presynaptic actions of pregnenolone. Therefore, pregnenolone prevents the THC-induced increase in paired pulse ratio (PPR) but does not alter the amplitude or decay duration of micro-EPSCs (mEPSCs) [1].
Pregnenolone monosulfate acts as a signaling-specific inhibitor of CB1 receptor signaling, inhibiting the effects of tetrahydrocannabinol (THC) that are mediated by CB1 receptors. It weakly activates TRPM1 channels. |
| ln Vivo |
Administration of pregnenolone (2–6 mg/kg) attenuates THC-induced memory impairment in mice and inhibits THC-induced food intake in Wistar rats and C57BL/6N mice, but does not alter these behaviors in and of itself. Pregnenolone injections (2 and 4 mg/kg) prior to each self-administration lower breakpoints in a graduated-ratio regimen and decrease WIN 55,212-2 intake [1].
In vivo, pregnenolone monosulfate reduces several effects of THC, including those mediated by CB1 receptors. It protects the brain from cannabis intoxication. |
| Enzyme Assay |
CB1 receptor binding assays are performed using membrane preparations from cells expressing human CB1 receptors. Radiolabeled ligand (e.g., [3H]CP-55,940) displacement assays determine the compound's affinity. THC-induced CB1 receptor signaling (e.g., cAMP inhibition) is measured in the presence of the compound to assess its signaling-specific inhibitory effects.
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| Cell Assay |
Neuronal cell lines (e.g., SH-SY5Y) or primary neurons are treated with pregnenolone monosulfate and stimulated with THC. CB1 receptor-mediated signaling (cAMP levels, ERK phosphorylation) is measured. The compound's ability to block THC-induced effects without affecting basal CB1 signaling is assessed.
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| Animal Protocol |
Rodent models of THC intoxication are used. Animals are pretreated with pregnenolone monosulfate (i.p. or s.c.) followed by THC administration. Behavioral endpoints (locomotor activity, hypothermia, analgesia) and biochemical markers (cAMP levels in brain regions) are measured to assess the compound's protective effects.
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| ADME/Pharmacokinetics |
Predicted to have good brain penetration due to its steroid structure. Oral bioavailability is expected to be low due to first-pass metabolism. Plasma half-life in rodents is estimated at 1-2 hours. Metabolized via sulfatase enzymes to pregnenolone.
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| Toxicity/Toxicokinetics |
Low toxicity profile; no significant acute toxicity reported at therapeutic doses. In animal studies, it is well-tolerated with no major adverse effects. No genotoxicity or cardiotoxicity concerns have been identified.
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| References |
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| Additional Infomation |
Pregnenolone sulfate is a steroidal sulfate. It is an EC 2.7.1.33 (pantothenic acid kinase) inhibitor and a human metabolite. Its function is related to pregnenolone. It is the conjugate acid of pregnenolone sulfate (1-). There are reports and relevant data on pregnenolone sulfate in the human body.
Pregnenolone monosulfate is a naturally occurring neurosteroid and an endogenous metabolite. It is being investigated for its potential in treating cannabis use disorder and neuropsychiatric conditions. The compound has not been approved for clinical use; it remains a research tool for studying CB1 receptor biology and neurosteroid functions. |
| Molecular Formula |
C21H32O5S
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|---|---|
| Molecular Weight |
396.54078
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| Exact Mass |
396.197
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| CAS # |
1247-64-9
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| Related CAS # |
Pregnenolone monosulfate sodium;1852-38-6;Pregnenolone;145-13-1
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| PubChem CID |
105074
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| Appearance |
White to off-white solid powder
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| LogP |
5.423
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
27
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| Complexity |
766
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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
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| InChi Key |
DIJBBUIOWGGQOP-QGVNFLHTSA-N
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| InChi Code |
InChI=1S/C21H32O5S/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)/t15-,16-,17+,18-,19-,20-,21+/m0/s1
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| Chemical Name |
[(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] hydrogen sulfate
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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 |
| 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 : ~62.5 mg/mL (~157.61 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.25 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 20.8 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: ≥ 2.08 mg/mL (5.25 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 20.8 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: ≥ 2.08 mg/mL (5.25 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 | 2.5218 mL | 12.6091 mL | 25.2181 mL | |
| 5 mM | 0.5044 mL | 2.5218 mL | 5.0436 mL | |
| 10 mM | 0.2522 mL | 1.2609 mL | 2.5218 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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