2. Metabolic Enzyme/Protease NF-κB Immunology/Inflammation
  3. Cytochrome P450 Reactive Oxygen Species (ROS)
  4. Azalanstat

Azalanstat (RS-21607) is an inhibitor of heme oxygenase and lanosterol 14α-demethylase, with inhibitory activity against HO-1 (IC50 = 5.5 µM) and HO-2 (IC50 = 24.5 µM). Azalanstat reduces the maturation rate of rat oocytes, increases rat oocyte degeneration, and partially inhibits progesterone production in preovulatory follicles of rats.

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Azalanstat

Azalanstat Chemical Structure

CAS No. : 143393-27-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

Other Forms of Azalanstat:

Azalanstat Related Antibodies

Top Publications Citing Use of Products

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

Azalanstat (RS-21607) is an inhibitor of heme oxygenase and lanosterol 14α-demethylase, with inhibitory activity against HO-1 (IC50 = 5.5 µM) and HO-2 (IC50 = 24.5 µM). Azalanstat reduces the maturation rate of rat oocytes, increases rat oocyte degeneration, and partially inhibits progesterone production in preovulatory follicles of rats[1][2][3].

In Vitro

Azalanstat (Compound I) inhibits rat spleen microsomal HO-1 (IC50 = 5.8 μM) and rat brain microsomal HO-2 (IC50 = 28.0 μM) in vitro, with a selectivity index of 5 for HO-1 over HO-2[1].
Azalanstat (0-100 μM) inhibits the activity of rat liver microsomal CYP3A1/3A2 in vitro, with an IC50 of 48.1 μM[1].
Azalanstat (0-200 μM; 3-24 h, or 6 h + 24 h inhibitor-free culture) reduces GVBD in a dose- and time-dependent manner at high concentrations (≥50 μM for 6 h treatment, ≥10 μM for 24 h treatment), while increasing the degree of oocyte degeneration; notably, oocyte degeneration becomes irreversible after 6 h of treatment at 100 μM[2].
Azalanstat (1-100 μM; 6-24 h with 5 μg/mL LH) reduces LH-induced GVBD in a dose-dependent manner, accompanied by increased degeneration of oocytes and follicles at 1-100 μM with a 24 h treatment[2].
Azalanstat (1-100 μM; 6-24 h with 5 μg/mL LH) partially inhibits LH-induced progesterone synthesis in preovulatory rat follicles in vitro in a dose-dependent manner when applied at concentrations of 1, 50, and 100 μM for 6 or 24 h[2].

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

Azalanstat Related Antibodies
In Vivo

zalanstat (2.15-215 μg/bursa; intracapsular injection; single administration) significantly inhibits ovulation in immature female Wistar rats at the highest tested intracapsular dose[2].

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

Animal Model: Wistar-derived rats (female, 23-24 days of age, injected with 10 IU eCG then 4 IU hCG to induce ovulatory dysfunction model)[2]
Dosage: 2.15-215 μg/bursa
Administration: intrabursal injection; single dose
Result: Caused statistically significant inhibition of ovulation.
Molecular Weight

429.96

Formula

C22H24ClN3O2S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC(C=C1)=CC=C1CC[C@]2(O[C@@H](CO2)CSC3=CC=C(C=C3)N)CN4C=CN=C4
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 : 100 mg/mL (232.58 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 2.3258 mL 11.6290 mL 23.2580 mL
5 mM 0.4652 mL 2.3258 mL 4.6516 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.81 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)

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: 99.52%

SDS (254 KB)

COA (248 KB) HNMR (183 KB) LCMS (133 KB)

Handling Instructions (2659 KB)
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, 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 2.3258 mL 11.6290 mL 23.2580 mL 58.1449 mL
5 mM 0.4652 mL 2.3258 mL 4.6516 mL 11.6290 mL
10 mM 0.2326 mL 1.1629 mL 2.3258 mL 5.8145 mL
15 mM 0.1551 mL 0.7753 mL 1.5505 mL 3.8763 mL
20 mM 0.1163 mL 0.5814 mL 1.1629 mL 2.9072 mL
25 mM 0.0930 mL 0.4652 mL 0.9303 mL 2.3258 mL
30 mM 0.0775 mL 0.3876 mL 0.7753 mL 1.9382 mL
40 mM 0.0581 mL 0.2907 mL 0.5814 mL 1.4536 mL
50 mM 0.0465 mL 0.2326 mL 0.4652 mL 1.1629 mL
60 mM 0.0388 mL 0.1938 mL 0.3876 mL 0.9691 mL
80 mM 0.0291 mL 0.1454 mL 0.2907 mL 0.7268 mL
100 mM 0.0233 mL 0.1163 mL 0.2326 mL 0.5814 mL
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Azalanstat 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:

Azalanstat143393-27-5RS-21607RS21607RS 21607Cytochrome P450Reactive Oxygen Species (ROS)CYPsHeme Oxygenase/Lanosterol 14α-Demethylase InhibitorWistar-derived ratsInhibitorinhibitorinhibit

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