Aminoglutethimide (Synonyms: DL-Aminoglutethimide)

Name: Aminoglutethimide
Brand: MedChemExpress
SKU: HY-B0237
Rating: 4.5 (0 reviews)

Cat. No.: HY-B0237 Purity: 98.87%: Data Sheet
COA

SDS
Handling Instructions
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Aminoglutethimide (DL-Aminoglutethimide) is an orally active anticonvulsant with various endocrine-related side effects. Aminoglutethimide blocks multiple steroid hormone synthesis pathways by inhibiting several cytochrome P-450-dependent hydroxylases, such as aromatase, cholesterol side-chain cleavage enzyme, 11-hydroxylase, and 18-hydroxylase, with IC₅₀ values of 0.3, 3.5, 120, and 20 μM, respectively. Aminoglutethimide reduces cortisol levels. Aminoglutethimide can be used in research on Cushing's syndrome, breast cancer, and other conditions.

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

Aminoglutethimide Chemical Structure

CAS No. : 125-84-8

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
1 g	Get quote
5 g	Get quote

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View All Cytochrome P450 Isoform Specific Products:

View All Isoforms

CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Aromatase

Cellular Effect

Cell Line	Type	Value	Description	References
MCF7	IC₅₀	10 μM Compound: Cytadren	Inhibition of human aromatase transfected in human MCF7 cells Inhibition of human aromatase transfected in human MCF7 cells	[PMID: 26689671]

In Vitro

Aminoglutethimide inhibits human placental microsomal aromatase by targeting cytochrome P-450, preventing the oxygen-dependent conversion of androgens to estrogens^[1].
Aminoglutethimide (0.05 mM; duration sufficient to produce complete steroidogenesis inhibition) completely inhibits steroidogenesis in monolayer cultures of functional adrenal tumour cells by directly targeting steroidogenic enzymes, without altering ACTH-induced cell morphology or glucose consumption^[4].

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

In Vivo

Aminoglutethimide was assessed for in vivo pharmacodynamic effects on steroidogenesis in normal/healthy rats, with no quantitative results provided^[2].
Aminoglutethimide (125-500 mg/kg/day; p.o.; once daily; 5 days) induces dose-dependent adrenal zona fasciculata cell damage including cytoplasmic vacuolation, single cell necrosis, excessive lipid accumulation, mitochondrial injury, and accelerated lysosomal degradation (mitophagy and lipophagy) in male Crlj:CD1(ICR) mice^[3].
Aminoglutethimide (8 days) exhibits goitrogenic activity and interferes with thyroid metabolism in intact rats on a low iodine diet, as evidenced by increased thyroid weight and reduced radio-iodine uptake^[4].
Aminoglutethimide induces thyromegaly, reduces thyroxine and di-iodotyrosine production, and increases thyroidal inorganic iodide levels in Rattus norvegicus^[4].
Aminoglutethimide inhibits adrenal steroid biosynthesis in rats and puppies, inducing adrenal hypertrophy, decreased corticosterone production, increased plasma ACTH, and characteristic cortical histological changes^[4].
Aminoglutethimide induces ovarian enlargement in intact rats and potential uterine enlargement in hypophysectomized rats^[4].
Aminoglutethimide (large doses) disrupts ovarian function, halts oestrous cycles, induces sterility, and reduces oestrogen-related uterine weight in intact female rats^[4].
Aminoglutethimide (10 mg/kg; i.v.) is active at 10 mg/kg intravenously to inhibit cortisol secretion and block the steroidogenic response to ACTH in dogs^[4].

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

Animal Model:	Crlj:CD1(ICR) (male, 7 weeks old)^[3]
Dosage:	125 mg/kg/day; 250 mg/kg/day; 500 mg/kg/day
Administration:	p.o.; once daily; 5 days
Result:	Induced cytoplasmic vacuolation in adrenal zona fasciculata cells at 125-500 mg/kg/day, with vacuole membranes staining positive for adipophilin and LAMP-2, increased LAMP-2-positive granules, and Sudan black-positive vacuole contents. Observed single cell necrosis in zona fasciculata cells at 250-500 mg/kg/day. Caused 3 of 4 mice to become moribund and require euthanasia on Day 3 at 500 mg/kg/day. Revealed enlarged lipid droplets, increased primary lysosomes, mitochondrial vacuolation, and enlarged lysosomes containing damaged mitochondria and lamellar bodies in zona fasciculata cells across all doses via electron microscopy.

Clinical Trial

Molecular Weight

232.28

Formula

C₁₃H₁₆N₂O₂

CAS No.

125-84-8

Appearance

Solid

Color

White to off-white

SMILES

O=C(C(CC)(C1=CC=C(N)C=C1)CC2)NC2=O

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 : 50 mg/mL (215.26 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	4.3051 mL	21.5257 mL	43.0515 mL
5 mM	0.8610 mL	4.3051 mL	8.6103 mL
10 mM	0.4305 mL	2.1526 mL	4.3051 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (10.76 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (10.76 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 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (10.76 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

mg/kg

Animal weight
(per animal)

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: 98.87%

Select Batch:

Data Sheet (281 KB) SDS (396 KB)

COA (253 KB) HNMR (138 KB) LCMS (97 KB)

Handling Instructions (2659 KB)

References

[1]. Santen RJ, et al. Aminoglutethimide: review of pharmacology and clinical use. Pharmacotherapy. 1981;1(2):95-120. [Content Brief]

[2]. Cocconi G, et al. First generation aromatase inhibitors--aminoglutethimide and testololactone. Breast Cancer Res Treat. 1994;30(1):57-80. [Content Brief]

[3]. Mutsuga M, et al. Aminoglutethimide-induced lysosomal changes in adrenal gland in mice. Exp Toxicol Pathol. 2017;69(7):424-429. [Content Brief]

[4]. Hughss SW, et al. Aminoglutethimide: a "side-effect" turned to therapeutic advantage. Postgrad Med J. 1970;46(537):409-416. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	4.3051 mL	21.5257 mL	43.0515 mL	107.6287 mL
	5 mM	0.8610 mL	4.3051 mL	8.6103 mL	21.5257 mL
	10 mM	0.4305 mL	2.1526 mL	4.3051 mL	10.7629 mL
	15 mM	0.2870 mL	1.4350 mL	2.8701 mL	7.1752 mL
	20 mM	0.2153 mL	1.0763 mL	2.1526 mL	5.3814 mL
	25 mM	0.1722 mL	0.8610 mL	1.7221 mL	4.3051 mL
	30 mM	0.1435 mL	0.7175 mL	1.4350 mL	3.5876 mL
	40 mM	0.1076 mL	0.5381 mL	1.0763 mL	2.6907 mL
	50 mM	0.0861 mL	0.4305 mL	0.8610 mL	2.1526 mL
	60 mM	0.0718 mL	0.3588 mL	0.7175 mL	1.7938 mL
	80 mM	0.0538 mL	0.2691 mL	0.5381 mL	1.3454 mL
	100 mM	0.0431 mL	0.2153 mL	0.4305 mL	1.0763 mL

Aminoglutethimide 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:

Aminoglutethimide125-84-8DL-AminoglutethimideCytochrome P450CYPsprimary aldosteronism18-hydroxylaseCushing's syndromecytochrome P-450aromatasemetastatic breast carcinomaadrenal tumour cellscholesterol side-chain cleavage enzyme11-hydroxylaseprostate cancerInhibitorinhibitorinhibit

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Aminoglutethimide (Synonyms: DL-Aminoglutethimide)

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Aminoglutethimide Related Antibodies

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Aminoglutethimide Related Antibodies

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Complete Stock Solution Preparation Table

Aminoglutethimide Related Classifications

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