Art. -Nr.: HY-105191

Azalanstat

Name: Azalanstat
Brand: MedChemExpress
SKU: HY-105191
Price: 355.00 USD
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Rating: 5 (1 reviews)

(Synonyms: RS-21607)

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Azalanstat (RS-21607) is an orally active lanosterol 14α-demethylase inhibitor. Azalanstat exerts a cholesterol-lowering effect by inhibiting cholesterol synthesis and regulating HMG-CoA Reductase (HMGCR), and shows an additive effect when used in combination with Cholestyramine (HY-104081). Azalanstat is used in the study of hypercholesterolemia.

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Reinheit : 99.52%
CAS. Nr.: 143393-27-5
Formel: C₂₂H₂₄ClN₃O₂S
Molecular Weight:429.96

Speicherung:

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

Azalanstat Chemical Structure

CAS. Nr.: 143393-27-5

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vitro

Azalanstat (RS-21607) (0.1 nM-10 μM; 1 h pre-incubation, 2 h pulse) mesylate potently inhibits cholesterol synthesis in human fibroblasts (IC₅₀ = 0.2 nM), HepG2 cells (IC₅₀ = 6.5 nM), and hamster hepatocytes (IC₅₀ = 10 nM) by inhibiting lanosterol 14α-demethylase, which leads to the accumulation of methyl sterols without the accumulation of oxidosqualene^[1].
Azalanstat (0.01-100 μM; 20 h) mesylate exerts a biphasic regulatory effect on HMG-CoA reductase activity in HepG2 cells: it inhibits approximately 40% of the enzyme activity at concentrations of 0.01-1 μM, and stimulates enzyme activity up to 600% at concentrations of 30-100 μM^[1].
Azalanstat (0.1-5 μM; 18 h) mesylate increases HMG-CoA reductase mRNA levels by 300% at 0.1 μM and by 100% at 5 μM in HepG2 cells, and elevates LDL receptor mRNA levels by 70% at both 0.1 μM and 5 μM, suggesting post-transcriptional regulation of HMG-CoA reductase activity^[1].
Azalanstat (0.1-10 μM; 24 h pre-incubation, 3 h LDL uptake) mesylate increases specific ¹²⁵I-LDL uptake by approximately 25% in HepG2 cells^[1].
Azalanstat (0.1-100 μM; 10 min pre-incubation, 15 min total incubation at 37 °C) mesylate moderately inhibits rat spleen HO-1 (IC₅₀ = 5.3 μM) and rat brain HO-2 (IC₅₀ = 24.5 μM), with a 4.6-fold selectivity for HO-1 over HO-2^[3].

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

Cell Viability Assay^[1]

View Protocol

Cell Line:

human fibroblasts, HepG2 cells, hamster hepatocytes
Concentration:

0.1, 1.0, 10, 100, 1000, 10000 nM
Incubation Time:

1 hr pre-incubation, 2 hr pulse
Result:

Inhibited cholesterol synthesis in human fibroblasts (IC₅₀ = 0.2 nM), HepG2 cells (IC₅₀ = 6.5 nM), and hamster hepatocytes (IC₅₀ = 10 nM) by blocking lanosterol 14α-demethylase.

In Vivo

Azalanstat (RS-21607) (25-100 mg/kg; oral; once daily; for 14 consecutive days) mesylate reduces serum cholesterol in hamsters fed a normal diet in a dose-dependent manner, with an ED₅₀ of 62 mg/kg^[1].
Azalanstat (50 mg/kg; oral; once daily; for 28 days) mesylate reduces plasma cholesterol by 37% in hamsters fed a high-fat/high-cholesterol diet, and its effect is transiently maintained after drug withdrawal^[1].
Azalanstat (50 mg/kg; oral; once daily; for 14 consecutive days) mesylate inhibits cholesterol synthesis in hamster tissues by up to 98%. It exhibits no selectivity in tissue distribution and also elevates methyl sterol levels, particularly dihydrolanosterol levels in the liver^[1].
Azalanstat (25-100 mg/kg; oral; daily; 14 days) mesylate inhibits hepatic microsomal HMG-CoA reductase activity in a dose-dependent manner in hamsters, with an ED₅₀ of 31 mg/kg, and this activity is highly correlated with serum cholesterol reduction^[1].
Azalanstat (50-75 mg/kg; oral; daily; for 1-2 weeks) mesylate increases hepatic cholesterol 7α-hydroxylase activity in hamsters by 1.5- to 5-fold, and this effect emerges after 1-2 weeks of oral administration at a dose of 50-75 mg/kg^[1].
Azalanstat (30 mg/kg; p.o.; once daily; for 7 consecutive days) mesylate reduces serum cholesterol in hamsters by 44% and inhibits hepatic HMG-CoA reductase activity; its cholesterol-lowering effect exerts a synergistic effect with Cholestyramine (HY-104081), and it also attenuates Cholestyramine-induced activation of HMG-CoA reductase^[1].
Azalanstat (50 mg/kg; oral; daily; 7-10 days) mesylate reduces liver-specific LDL binding capacity and LDL receptor protein expression levels in hamsters, while lowering serum cholesterol by up to 53%^[1].

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

Animal Model:

Golden Syrian hamsters (male, 90-110 g, fed regular Purina Rodent Chow 5001 containing 0.027% cholesterol)^[1]
Dosage:

25 mg/kg; 50 mg/kg; 75 mg/kg; 100 mg/kg
Administration:

p.o.; daily; 14 days
Result:

Lowered serum cholesterol in a dose-dependent manner with an ED₅₀ of 62 mg/kg.
Reduced total cholesterol to 91.2 mg/dL, LDL cholesterol to 13.2 mg/dL, apo B to 17.3 mg/dL, and increased the HDL/total cholesterol ratio to 63.4%, while increasing the apo A-1/apo B ratio to 6.5 at 25 mg/kg.
Reduced total cholesterol to 71.8 mg/dL, LDL cholesterol to 9.9 mg/dL, apo B to 15.4 mg/dL, triglycerides to 185.8 mg/dL, increased the HDL/total cholesterol ratio to 66.3%, and increased the apo A-1/apo B ratio to 6.8 at 50 mg/kg.
Reduced total cholesterol to 66.5 mg/dL, LDL cholesterol to 3.5 mg/dL, apo B to 9.1 mg/dL, increased the HDL/total cholesterol ratio to 71.4%, and increased the apo A-1/apo B ratio to 10.0 at 75 mg/kg.
Reduced total cholesterol to 60.7 mg/dL, LDL cholesterol to 6.1 mg/dL, apo B to 11.7 mg/dL, triglycerides to 177.4 mg/dL, increased the HDL/total cholesterol ratio to 68.2%, and increased the apo A-1/apo B ratio to 8.2 at 100 mg/kg.

Animal Model:

Golden Syrian hamsters (male, 90-110 g, fed high fat diet containing 0.1% cholesterol, 5.9% butter fat, and 6% peanut oil for 4 weeks)^[1]
Dosage:

50 mg/kg
Administration:

p.o.; daily; 28 days
Result:

Reduced plasma cholesterol by 37% within 2 weeks.
Maintained plasma cholesterol levels significantly lower than controls for 2 weeks after treatment termination.

Animal Model:

Golden Syrian hamsters (male, 90-110 g, fed regular Purina Rodent Chow 5001)^[1]
Dosage:

50 mg/kg
Administration:

p.o.; daily; 14 days
Result:

Inhibited cholesterol (demethyl-sterol) synthesis by 98% in liver, 95% in kidney, 87% in spleen, 38% in adrenals, 93% in testes, and 95% in small intestine.
Increased methyl-sterol synthesis in all tested tissues.
Elevated hepatic dihydrolanosterol levels ~100-fold.
Raised serum dihydrolanosterol to 0.78 mg/dL.

Animal Model:

Golden Syrian hamsters (male, 90-110 g, fed regular Purina Rodent Chow 5001)^[1]
Dosage:

25 mg/kg; 50 mg/kg; 75 mg/kg; 100 mg/kg
Administration:

p.o.; daily; 14 days
Result:

Suppressed hepatic microsomal HMG-CoA reductase activity in a dose-dependent manner with an ED₅₀ of 31 mg/kg.
Showed a strong correlation between serum cholesterol levels and hepatic HMG-CoA reductase activity.

Animal Model:

Golden Syrian hamsters (male, 90-110 g, fed regular Purina Rodent Chow 5001)^[1]
Dosage:

50 mg/kg; 75 mg/kg
Administration:

p.o.; daily; 7-14 days
Result:

Induced hepatic cholesterol 7α-hydroxylase activity by 149% at 50 mg/kg for 1 week.
Induced hepatic cholesterol 7α-hydroxylase activity by 235% at 50 mg/kg for 2 weeks.
Induced hepatic cholesterol 7α-hydroxylase activity by 501% at 75 mg/kg for 2 weeks.

Animal Model:

Golden Syrian hamsters (male, 90-110 g, fed regular Purina Rodent Chow 5001)^[1]
Dosage:

30 mg/kg; 30 mg/kg plus cholestyramine 500 mg/kg
Administration:

p.o.; daily; 7 days; p.o.; twice daily; 7 days (cholestyramine)
Result:

Reduced serum cholesterol by 44% and suppressed hepatic HMG-CoA reductase activity to 44% of control levels when administered alone.
Reduced serum cholesterol by 58% and attenuated cholestyramine-induced increase in HMG-CoA reductase activity to 171% of control levels when coadministered with cholestyramine.

Animal Model:

Golden Syrian hamsters (male, 90-110 g, fed regular Purina Rodent Chow 5001)^[1]
Dosage:

50 mg/kg
Administration:

p.o.; daily; 7-10 days
Result:

Reduced specific ¹²⁵I-LDL binding to hepatic membranes to 38% of control levels and reduced serum cholesterol by 41% after 7 days.
Reduced LDL receptor protein expression to 51% of control levels and reduced serum cholesterol by 53% after 10 days.

Chemical Information

CAS. Nr. 143393-27-5
Appearance Solid
Molecular Weight 429.96
Formel C₂₂H₂₄ClN₃O₂S
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
Synonyms

RS-21607
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

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)

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

2.3258 mL

11.6290 mL

23.2580 mL

5 mM

0.4652 mL

2.3258 mL

4.6516 mL

10 mM

0.2326 mL

1.1629 mL

2.3258 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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 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 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (293 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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)
Handling Instructions (2659 KB)

Verweise

[1]. Burton PM, et al. Azalanstat (RS-21607), a lanosterol 14 alpha-demethylase inhibitor with cholesterol-lowering activity. Biochemical pharmacology. 1995 Aug 08;50(4):529-44.

[2]. Alfredson et al. Enantioselectivity of Azalanstat and Its Ketal Tosylate Intermediate in Chiral High Performance Liquid Chromatography Separations. Journal of Liquid Chromatography & Related Technologies, 19(10), 1653–1668.

[3]. Roman G, et al. Heme oxygenase inhibition by 2-oxy-substituted 1-(1H-imidazol-1-yl)-4-phenylbutanes: effect of halogen substitution in the phenyl ring. Bioorg Med Chem. 2007 May 1;15(9):3225-34. [Content Brief]

[4]. Vlahakis JZ, et al. Synthesis and evaluation of azalanstat analogues as heme oxygenase inhibitors. Bioorganic & medicinal chemistry letters. 2005 Mar 01;15(5):1457-61.

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	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