Dexfadrostat (Synonyms: (R)-Fadrozole; (R)-CGS 16949A free base; FAD286)

Name: Dexfadrostat
Brand: MedChemExpress
SKU: HY-113986
Rating: 4.5 (1 reviews)

Cat. No.: HY-113986 Purity: 98.75%: FAQs
Data Sheet SDS COA Handling Instructions

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Dexfadrostat ((R)-Fadrozole) is a potent nonsteroidal inhibitor. Dexfadrostat also inhibits human placental aromatase (pIC₅₀ = 6.17) and aldosterone biosynthesis. Dexfadrostat reverses cardiac fibrosis in spontaneously hypertensive heart failure rats..

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Dexfadrostat Chemical Structure

CAS No. : 102676-87-9

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 1768	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 1768	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 720	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

Other Forms of Dexfadrostat:

Fadrozole hydrochloride In-stock
Fadrozole In-stock
(S)-Dexfadrostat Get quote
Fadrozole hydrochloride hemihydrate Get quote

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Description

Dexfadrostat ((R)-Fadrozole) is a potent nonsteroidal inhibitor^[1]. Dexfadrostat also inhibits human placental aromatase (pIC₅₀ = 6.17) and aldosterone biosynthesis. Dexfadrostat reverses cardiac fibrosis in spontaneously hypertensive heart failure rats.^[1]^[2].

IC₅₀ & Target

pIC50: 6.17 (human placental aromatase)

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	4 nM Compound: FAD-286	Inhibition of human CYP11B2 expressed in HEK293A cells using deoxycorticosterone as substrate pretreated for 1 hr followed by substrate addition measured after 1 hr by HTRF assay Inhibition of human CYP11B2 expressed in HEK293A cells using deoxycorticosterone as substrate pretreated for 1 hr followed by substrate addition measured after 1 hr by HTRF assay	[PMID: 28359792]
NCI-H295R	IC₅₀	30 nM Compound: FAD286	Inhibition of CYP11B2 in human NCI-H295R cells assessed as inhibition of angiotensin-2-induced aldosterone production after 24 hrs by RIA Inhibition of CYP11B2 in human NCI-H295R cells assessed as inhibition of angiotensin-2-induced aldosterone production after 24 hrs by RIA	[PMID: 24900631]

In Vitro

The (-)-enantiomer with the S-absolute configuration was responsible for the high aromatase inhibitory activity of Dexfadrostat^[1].

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

In Vivo

Dexfadrostat ((R)-fadrozole; 0.24 and 1.2 mg/kg; daily; oral) and (S)-fadrozole similarly decreases plasma aldosterone levels, whereas urinary aldosterone excretion rate was reduced only by S-fadrozole^[2].
Dexfadrostat (0.24 and 1.2 mg/kg; daily; oral) effectively reverses preexistent left ventricular interstitial fibrosis by 50% (vs. 42% for canrenoate), S-fadrozole was devoid of an antifibrotic effect^[2].

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

Animal Model:	SHHF rats^[2]
Dosage:	0.24 and 1.2 mg/kg
Administration:	Daily; oral
Result:	Decreased plasma aldosterone levels and reversed preexistent left ventricular interstitial fibrosis.

Molecular Weight

223.27

Formula

C₁₄H₁₃N₃

CAS No.

102676-87-9

Appearance

Solid

Color

Light yellow to yellow

SMILES

N#CC1=CC=C([C@H]2CCCC3=CN=CN23)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 110 mg/mL (492.68 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	4.4789 mL	22.3944 mL	44.7888 mL
5 mM	0.8958 mL	4.4789 mL	8.9578 mL
10 mM	0.4479 mL	2.2394 mL	4.4789 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, 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.

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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: ≥ 2.75 mg/mL (12.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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: ≥ 2.75 mg/mL (12.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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: ≥ 2.75 mg/mL (12.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 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 (27.5 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: 98.75%

Select Batch:

Data Sheet (272 KB) SDS (393 KB)

COA (248 KB) HNMR (392 KB) LCMS (87 KB)

Handling Instructions (2659 KB)

References

[1]. Furet P, et al. Aromatase inhibitors: synthesis, biological activity, and binding mode of azole-type compounds. J Med Chem. 1993;36(10):1393-1400. [Content Brief]

[2]. Minnaard-Huiban M, et al. Fadrozole reverses cardiac fibrosis in spontaneously hypertensive heart failure rats: discordant enantioselectivity versus reduction of plasma aldosterone. Endocrinology. 2008;149(1):28-31. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	4.4789 mL	22.3944 mL	44.7888 mL	111.9720 mL
	5 mM	0.8958 mL	4.4789 mL	8.9578 mL	22.3944 mL
	10 mM	0.4479 mL	2.2394 mL	4.4789 mL	11.1972 mL
	15 mM	0.2986 mL	1.4930 mL	2.9859 mL	7.4648 mL
	20 mM	0.2239 mL	1.1197 mL	2.2394 mL	5.5986 mL
	25 mM	0.1792 mL	0.8958 mL	1.7916 mL	4.4789 mL
	30 mM	0.1493 mL	0.7465 mL	1.4930 mL	3.7324 mL
	40 mM	0.1120 mL	0.5599 mL	1.1197 mL	2.7993 mL
	50 mM	0.0896 mL	0.4479 mL	0.8958 mL	2.2394 mL
	60 mM	0.0746 mL	0.3732 mL	0.7465 mL	1.8662 mL
	80 mM	0.0560 mL	0.2799 mL	0.5599 mL	1.3997 mL
	100 mM	0.0448 mL	0.2239 mL	0.4479 mL	1.1197 mL

Dexfadrostat Related Classifications

Cardiovascular Disease

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:

Dexfadrostat102676-87-9(R)-Fadrozole(R)-CGS 16949A FAD286FAD286FAD 286FAD-286Othershumanplacentalaromatasealdosteronebiosynthesis,heartfailureInhibitorinhibitorinhibit

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Dexfadrostat (Synonyms: (R)-Fadrozole; (R)-CGS 16949A free base; FAD286)

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