Pregnenolone Estrogen/progestogen Receptor modulator

Cat.No.S1914

Pregnenolone(3β-Hydroxy-5-pregnen-20-one) is an endogenous steroid hormone, used in the treatment of fatigue, Alzheimer’s disease, trauma and injuries.
Pregnenolone Estrogen/progestogen Receptor modulator Chemical Structure

Chemical Structure

Molecular Weight: 316.48

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 316.48 Formula

C21H32O2

Storage (From the date of receipt)
CAS No. 145-13-1 Download SDF Storage of Stock Solutions

Synonyms 3β-Hydroxy-5-pregnen-20-one Smiles CC(=O)C1CCC2C1(CCC3C2CC=C4C3(CCC(C4)O)C)C

Solubility

In vitro
Batch:

DMSO : 22 mg/mL (69.51 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 22 mg/mL

Water : Insoluble

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Mass Concentration Volume Molecular Weight

In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
progestogen Receptor [1]
In vitro

Pregnenolone induces a large, dose-related increase of both the rate and extent of MAP2-induced tubulin assembly, whereas progesterone, inactive per se, counteracted the stimulatory effect of this compound. This compound-increased assembly of microtubules produces a completely normal structure. [1] It preserves microtubule abundance and promotes cell movement during epiboly. [2] This chemical results in dramatic reduction in GR nuclear localization in mouse hippocampal cell line (HT-22). It has neuroprotective effects against both glutamate and amyloid beta protein neuropathology. [3]

In vivo

Pregnenolone sustains its proliferative activity in vivo and stimulates the growth of LNCaP-tumor xenografts in intact male SCID mice as well as in castrated animals. This compound is shown to activate transcription through the LNCaP androgen receptor (AR), but not the wild-type AR. [4] It results in a significant decrease in the accumulation of astrocytes in the proximity of the wound and in a decreased bromodeoxyuridine incorporation in reactive astrocytes of rats. [5] Administration of this chemical results in elevations in downstream neurosteroids such as allopregnanolone, a molecule with neuroprotective effects that also increases neurogenesis, decreases apoptosis and inflammation, modulates the hypothalamic-pituitary-adrenal axis, and markedly increases GABA(A) receptor responses. It elevates pregnenolone sulfate, a neurosteroid that positively modulates NMDA receptors. [6]

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/11179903/
  • [5] https://pubmed.ncbi.nlm.nih.gov/10221674/
  • [6] https://pubmed.ncbi.nlm.nih.gov/21756978/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05781009 Recruiting
Alcohol Use Disorder
Yale University|National Institute on Alcohol Abuse and Alcoholism (NIAAA)
January 8 2024 Phase 2
NCT05903716 Recruiting
Acne Vulgaris
Marmara University
September 15 2022 --
NCT04791124 Unknown status
Down Syndrome
Parc de Salut Mar|Aelis Farma|Starlab
January 11 2021 --
NCT03801629 Completed
Drug Effect
Yale University
September 12 2019 Phase 1
NCT03953612 Completed
Cocaine-Related Disorders
Yale University|National Institute on Drug Abuse (NIDA)
March 12 2019 Early Phase 1

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