Cat. No.: HY-113320

Etiocholanolone

(Synonyms: 5β-Androsterone)

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Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABA_A receptor than its enantiomer form.

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Pureté: 99.49%
CAS No.: 53-42-9
Formule: C₁₉H₃₀O₂
Masse moléculaire:290.44

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Etiocholanolone Chemical Structure

CAS No.: 53-42-9

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity^[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABA_A receptor than its enantiomer form^[2].

IC₅₀ & Target

Human Endogenous Metabolite

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Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	3.76 μM Compound: 45	Agonist activity at human TGR5 expressed in CHO cells by luciferase assay Agonist activity at human TGR5 expressed in CHO cells by luciferase assay	[PMID: 18307294]
HEK293	IC₅₀	182 nM Compound: ADT	The ability to inhibit the Type-3 17-beta- hydroxysteroid dehydrogenase activity in transfected human embryonic kidney (HEK)-293 cells experiment 3 The ability to inhibit the Type-3 17-beta- hydroxysteroid dehydrogenase activity in transfected human embryonic kidney (HEK)-293 cells experiment 3	[PMID: 11806715]
HEK293	IC₅₀	330 nM Compound: ADT	Inhibitory concentration against type-3 17-beta-HSD expressed in HEK293 cells Inhibitory concentration against type-3 17-beta-HSD expressed in HEK293 cells	[PMID: 11086723]
HEK293	IC₅₀	330 nM Compound: ADT	The ability to inhibit the Type-3 17-beta- hydroxysteroid dehydrogenase activity in transfected human embryonic kidney (HEK)-293 cells experiment 1 The ability to inhibit the Type-3 17-beta- hydroxysteroid dehydrogenase activity in transfected human embryonic kidney (HEK)-293 cells experiment 1	[PMID: 11806715]
HEK293	IC₅₀	330 nM Compound: ADT	Inhibition of type-3 17 beta-hydroxysteroid dehydrogenase expressed in HEK293 cells at 37 degree C pH7.4 Inhibition of type-3 17 beta-hydroxysteroid dehydrogenase expressed in HEK293 cells at 37 degree C pH7.4	[PMID: 16078844]

In Vitro

Etiocholanolone (10 μM) coapplication with GABA leads to an increase in the relative frequency of long openings (fraction of OT3, site A2 effect), but it is ineffective at increasing the duration of long openings (site B effect) or at decreasing the relative frequency of the activation-related closed time component (site A1 effect)^[2].

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

In Vivo

Etiocholanolone (intraperitoneal injection; 0-109.1 mg/kg; single dose) exhibits ED50 values of 57.6 and 109.1 mg/kg in the 6-Hz and PTZ tests, respectively. Protective activity in the 6-Hz test of 5β,3α-A persists for 2 h and is shorter than ent-5β,3α-A treatment (3 hours) in mice^[1].

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

Chemical Information

CAS No. 53-42-9
Appearance Solid
Masse moléculaire 290.44
Formule C₁₉H₃₀O₂
Color White to off-white
SMILES

C[C@@]1(CC2)[C@](CC3)([H])[C@](CC[C@]1([H])C[C@@H]2O)([H])[C@@](CCC4=O)([H])[C@]34C
Synonyms

5β-Androsterone
Structure Classification
- Steroids
Initial Source
- Endogenous metabolite
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

In Vitro:

DMSO : 50 mg/mL (172.15 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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.4431 mL

17.2153 mL

34.4305 mL

5 mM

0.6886 mL

3.4431 mL

6.8861 mL

10 mM

0.3443 mL

1.7215 mL

3.4431 mL

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (8.61 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 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (8.61 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.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (8.61 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (277 KB)
SDS (761 KB)
- English - EN (761 KB)
- Français - FR (761 KB)
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- Español - ES (761 KB)
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- Portuguese - PT (761 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Ping Li,et al. Natural and Enantiomeric Etiocholanolone Interact With Distinct Sites on the Rat alpha1beta2gamma2L GABAA Receptor. Mol Pharmacol. 2007 Jun;71(6):1582-90. [Content Brief]

[2]. Dorota Zolkowska, et al. Anticonvulsant Potencies of the Enantiomers of the Neurosteroids Androsterone and Etiocholanolone Exceed Those of the Natural Forms. Psychopharmacology (Berl). 2014 Sep;231(17):3325-32. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.4431 mL	17.2153 mL	34.4305 mL	86.0763 mL
	5 mM	0.6886 mL	3.4431 mL	6.8861 mL	17.2153 mL
	10 mM	0.3443 mL	1.7215 mL	3.4431 mL	8.6076 mL
	15 mM	0.2295 mL	1.1477 mL	2.2954 mL	5.7384 mL
	20 mM	0.1722 mL	0.8608 mL	1.7215 mL	4.3038 mL
	25 mM	0.1377 mL	0.6886 mL	1.3772 mL	3.4431 mL
	30 mM	0.1148 mL	0.5738 mL	1.1477 mL	2.8692 mL
	40 mM	0.0861 mL	0.4304 mL	0.8608 mL	2.1519 mL
	50 mM	0.0689 mL	0.3443 mL	0.6886 mL	1.7215 mL
	60 mM	0.0574 mL	0.2869 mL	0.5738 mL	1.4346 mL
	80 mM	0.0430 mL	0.2152 mL	0.4304 mL	1.0760 mL
	100 mM	0.0344 mL	0.1722 mL	0.3443 mL	0.8608 mL

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Etiocholanolone

Membrane Transporter/Ion Channel Compound Library

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Voir tous les produits spécifiques à Isoform Endogenous Metabolite

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Etiocholanolone Related Classifications

HY-113320 Related Classifications