Home Metabolism Dehydrogenase inhibitor - NADPH-oxidase inhibitor ASP-9521

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ASP-9521 Dehydrogenase inhibitor

Cat.No.S6749

ASP-9521 is a selective, orally bioavailable inhibitor of 17beta-hydroxysteroid dehydrogenase type 5 (17β-HSD5), also known as aldo-keto reductase family 1 member C3 (AKR1C3).
ASP-9521 Dehydrogenase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 330.42

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S674901 DMSO]66 mg/mL]false]Ethanol]66 mg/mL]false]Water]Insoluble]false Purity: 98.2%
98.2

Chemical Information, Storage & Stability

Molecular Weight 330.42 Formula

C19H26N2O3

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1126084-37-4 -- Storage of Stock Solutions

Synonyms N/A Smiles CC(C)(CC1CCN(CC1)C(=O)C2=CC3=C(N2)C=CC(=C3)OC)O

Solubility

In vitro
Batch:

DMSO : 66 mg/mL (199.74 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 66 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Mechanism of Action

Targets/IC50/Ki
17β-HSD5 [1]
In vitro

In vitro, ASP9521 inhibited the conversion of androstenedione into testosterone by recombinant human and cynomolgus monkey AKR1C3 in a concentration-dependent manner, with IC50 values of 11 and 49 nmol/L, respectively. In contrast, ASP9521 did not inhibit the conversion by rat and mouse homologues (AKR1C1 and AKR1C6, respectively) up to a concentration of 10 μmol/L. ASP9521 showed moderately high selectivity (>100-fold) for human AKR1C3 (IC50: 120 nmol/L) over the human isoform AKR1C2 (IC50: >20,000 nmol/L)[1].
In vivo

In murine models harbouring CWR22R xenograft tumours, single oral administration of ASP9521 suppressed AD-induced intratumoural testosterone production in a dose-dependent manner. This inhibitory effect was maintained for 24 h after single oral administration of ASP9521. Over this 24 h period, ASP9521 concentration rapidly decreased in plasma from 771.8 ng/mL (mean) to undetectable levels, while its intratumoural concentration reached its maximal level within 15 min after administration of ASP9521 and remained stable for 24 h. In nude mice bearing HEK293 tumours with or without AKR1C3 expression, after single oral administration of ASP9521, plasma concentrations of ASP9521 reached maximum values within 0.25 h (mean: 767.3 ng/mL and 648.2 ng/mL for HEK293 and HEK293-AKR1C3 cells, respectively), but decreased rapidly thereafter. Accumulation of ASP9521 in tumour tissue may depend on AKR1C3 expression. After single oral administration of 1 mg/kg ASP9521 to rats, dogs and monkeys, the drug was rapidly absorbed. The bioavailability values were 35 %, 78 %, and 58 %, respectively. After iv administration of ASP9521 to rats, dogs and monkeys, plasma concentrations of the drug declined with t1/2 values of 0.2, 1.7 and 5.8 h, respectively[1].
References

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