2. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel Metabolic Enzyme/Protease Autophagy
  3. Cannabinoid Receptor TRP Channel Endogenous Metabolite Autophagy
  4. Pregnenolone

Pregnenolone  (Synonyms: 3β-Hydroxy-5-pregnen-20-one)

Cat. No.: HY-B0151 Purity: 99.87%
SDS COA Handling Instructions

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Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.

For research use only. We do not sell to patients.

Pregnenolone Chemical Structure

Pregnenolone Chemical Structure

CAS No. : 145-13-1

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10 mM * 1 mL in DMSO
ready for reconstitution
 USD 61 In-stock
Solution
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Based on 3 publication(s) in Google Scholar

Other Forms of Pregnenolone:

Pregnenolone Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication[1][2]. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].

IC50 & Target[1]

CB1

 

Human Endogenous Metabolite

 

Cellular Effect
Cell Line Type Value Description References
A549 ED50
8.6 μg/mL
Compound: 3
Cytotoxicity against human A549 cells by modified MTT assay
Cytotoxicity against human A549 cells by modified MTT assay
[PMID: 10650100]
HT-29 ED50
0.7 μg/mL
Compound: 3
Cytotoxicity against human HT29 cells by modified MTT assay
Cytotoxicity against human HT29 cells by modified MTT assay
[PMID: 10650100]
KB ED50
> 50 μg/mL
Compound: 3
Cytotoxicity against human KB cells by modified MTT assay
Cytotoxicity against human KB cells by modified MTT assay
[PMID: 10650100]
P388 ED50
7.8 μg/mL
Compound: 3
Cytotoxicity against mouse P388 cells by modified MTT assay
Cytotoxicity against mouse P388 cells by modified MTT assay
[PMID: 10650100]
In Vitro

CB1 receptor stimulation increases brain Pregnenolone levels, which in turn exerts a negative feedback on the activity of the CB1 receptor antagonizing most of the known behavioral and somatic effects of THC. Pregnenolone likely acts as a signaling-specific negative allosteric modulator binding to a site distinct from that occupied by orthosteric ligands. Pregnenolone does not modify agonist binding but only agonist efficacy[1].
The effect of THC is significantly attenuated when slices are pre-treated with Pregnenolone 100 nM (15.1±1.8 % of inhibition). These effects are likely due to a pre-synaptic action of Pregnenolone. Thus, Pregnenolone blocks the increase in paired-pulse ratio (PPR) induced by THC but does not modify either the amplitude or the decay time of miniature EPSC (mEPSC)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pregnenolone Related Antibodies
In Vivo

Pregnenolone administration (2-6 mg/kg) blocks THC-induced food-intake in Wistar rats and in C57BL/6N mice, and blunts the memory impairment induced by THC in mice, but it does not modify these behaviors per se. Injections of Pregnenolone (2 and 4mg/kg) before each self-administration session reduce the intake of WIN 55,212-2 and reduce the break-point in a progressive ratio schedule[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

316.48

Formula

C21H32O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@@](C1=CC2)(CC[C@H](O)C1)[C@]3([H])[C@]2([H])[C@@](CC[C@@H]4C(C)=O)([H])[C@]4(C)CC3
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (78.99 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1598 mL 15.7988 mL 31.5976 mL
5 mM 0.6320 mL 3.1598 mL 6.3195 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.90 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.90 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  50% PEG300    50% Saline

    Solubility: 10 mg/mL (31.60 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.87%

SDS (393 KB)

COA (251 KB) HNMR (283 KB) RP-HPLC (142 KB)

Handling Instructions (2659 KB)
References
Animal Administration
[1]

Mice and Rats[1]
Adult male Wistar rats (weighing 320-340g), Sprague Dawley male rats (weighing 330-350g), C57BL/6N mice (2-3 months) and CD1 mice (weighing 25-30 g at the beginning of the experiments) are used. Pregnenolone is injected subcutaneously (sc). The injection volumes are 1 mL/kg of body weight for rats and 10 mL/kg for mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1598 mL 15.7988 mL 31.5976 mL 78.9939 mL
5 mM 0.6320 mL 3.1598 mL 6.3195 mL 15.7988 mL
10 mM 0.3160 mL 1.5799 mL 3.1598 mL 7.8994 mL
15 mM 0.2107 mL 1.0533 mL 2.1065 mL 5.2663 mL
20 mM 0.1580 mL 0.7899 mL 1.5799 mL 3.9497 mL
25 mM 0.1264 mL 0.6320 mL 1.2639 mL 3.1598 mL
30 mM 0.1053 mL 0.5266 mL 1.0533 mL 2.6331 mL
40 mM 0.0790 mL 0.3950 mL 0.7899 mL 1.9748 mL
50 mM 0.0632 mL 0.3160 mL 0.6320 mL 1.5799 mL
60 mM 0.0527 mL 0.2633 mL 0.5266 mL 1.3166 mL
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Pregnenolone Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pregnenolone145-13-13β-Hydroxy-5-pregnen-20-oneCannabinoid ReceptorTRP ChannelEndogenous MetaboliteAutophagyTransient receptor potential channelsInhibitorinhibitorinhibit

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