Art. -Nr.: HY-167874

ASP-8731

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ASP-8731 is an orally active BACH1 inhibitor. ASP-8731 activates antioxidant, anti-inflammatory and globin gene pathways by relieving the inhibitory effect of BACH1 on NRF2-mediated gene transcription. ASP-8731 significantly upregulates the expression of HMOX1, FTH1 and various globins (such as HGB, HBG, HBA), increases fetal hemoglobin (HbF) levels, and effectively induces F-cell production in hydroxyurea-unresponsive cells. Meanwhile, ASP-8731 reduces inflammatory responses and white blood cell counts by downregulating VCAM1, ICAM-1 and the phosphorylation level of NF-κB(p65), and blocks heme-induced glutathione depletion and microcirculatory stasis. ASP-8731 holds potential for inhibiting sickle cell disease and related hematological disorders.

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Reinheit: 98.42%
CAS. Nr.: 2488255-42-9
Formel: C₂₀H₂₁N₅O₄
Molecular Weight:395.41

Speicherung:

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

ASP-8731 Chemical Structure

CAS. Nr.: 2488255-42-9

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

p65

Alle Heme Oxygenase (HO) Isoform-spezifische Produkte anzeigen :

HO-1
HO-2

Alle NF-κB Isoform-spezifische Produkte anzeigen :

In Vitro

ASP-8731 (0.1-50 μM; 24 h) potently upregulates the mRNA levels of HMOX1 and FTH1 in human hepatocellular carcinoma HepG2 cells^[1].
ASP-8731 (1-10 μM; pre-incubated for 24 h prior to 4 h of TNF-α treatment) reduces TNF-α-induced VCAM1 mRNA levels in primary human pulmonary artery endothelial cells^[1].
ASP-8731 (1-3 μM; pre-incubated for 24 h followed by 30 min hemin treatment) inhibits hemin-induced reduction of glutathione levels in primary human pulmonary endothelial cells^[1].
ASP-8731 (0.3-1 μM; 7 days of erythroid differentiation) increases HBG mRNA levels and the proportion of HbF-containing F cells during erythroid differentiation of human bone marrow-derived CD34⁺ cells, and ASP-8731 (1-3 μM) induces the generation of F cells in HU non-responder donor cells^[1].
ASP-8731 (0.3-10 μM; 10 days of erythroid differentiation) upregulates the mRNA levels of HBG, HBA and multiple antioxidant genes in erythroid-differentiated CD34⁺ cells derived from patients with sickle cell disease, but exerts no effect on the mRNA level of HBB^[1].
Erythroid differentiation:
This is the process by which hematopoietic stem cells in the bone marrow undergo stepwise directional development and maturation into functional red blood cells under the regulation of specific signals.
The process involves continuous stages from erythroid progenitor cells (BFU-E, CFU-E) to proerythroblasts, erythroblasts (early, intermediate and late stages), and finally enucleation to form reticulocytes that mature into red blood cells, with the entire process taking approximately 7 days.
During this process, cells undergo significant morphological and biochemical changes, including massive synthesis of hemoglobin, gradual reduction in cell volume, and eventual extrusion of the nucleus, to maximize their oxygen-carrying capacity.
Reference for erythroid differentiation medium^[1]:
X-Vivo-15, rhIL-3 (10 ng/mL), rhSCF (100 ng/mL), Epo (3 U/mL)

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

Real Time qPCR^[1]

Cell Line:

HepG2
Concentration:

0.1, 10, 50 μM
Incubation Time:

24 h
Result:

Effectively increased the mRNA levels of HMOX1 and FTH1, even more potently than DMF (HY-Y0345) (1-250 μM).

In Vivo

ASP-8731 (1-25 mg/kg; p.o.; once daily, 6 days per week; for 4 weeks) dose-dependently inhibits heme-induced microvascular stasis in Townes HbSS mice (the stasis rate can be reduced to as low as 7% at the 25 mg/kg dose) and decreases their white blood cell count^[1].
ASP-8731 (3-25 mg/kg; p.o.; once daily; 14 days) upregulates the expression of HO-1 and heme oxygenase activity in the liver of Townes HbSS mice, while it reduces the expression of NF-κB phosphorylated p65 and ICAM-1, upregulates the expression of γ-globin, and increases HbF-containing F cells^[1].

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

Animal Model:

Townes-sickle (HbSS) (male and female, 12-16 weeks of age, 129/B6 mixed genetic background, knock-in model)^[1]
Dosage:

1, 3, 25 mg/kg
Administration:

p.o.; once daily, 6 days per week; 4 weeks
Result:

Reduced hemin-induced microvascular stasis to 26% (1 mg/kg), 21% (3 mg/kg), and 7% (25 mg/kg) (vs 33% in vehicle controls).\n
Reduced white blood cell counts to 22 × 103/μL (1 mg/kg), 18 × 103/μL (3 mg/kg), and 13 × 103/μL (25 mg/kg) (vs 28 × 103/μL in vehicle controls).

Animal Model:

Townes-sickle (HbSS) (male and female, 12-16 weeks of age, 129/B6 mixed genetic background, knock-in model)^[1]
Dosage:

3, 10, 25 mg/kg
Administration:

p.o.; once daily; 14 consecutive days
Result:

Increased microsomal heme oxygenase-1 (HO-1) protein expression in the liver at 25 mg/kg.\n
Decreased nuclear NF-ĸB phospho-p65 and microsomal ICAM-1 protein expression in the liver at all tested doses.\n
Increased hepatic heme oxygenase activity in a dose-dependent manner.
Increased the ratio of gamma globin to gamma globin + beta-S globin to 7.8% (3 mg/kg) and 8.3% (25 mg/kg) (vs 5.8% in vehicle controls).
Increased the percentage of HbF-containing F-cells to 1.8% (3 mg/kg) and 2.1% (25 mg/kg) (vs 1.0% in vehicle controls).

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2488255-42-9
Appearance Solid
Molecular Weight 395.41
Formel C₂₀H₂₁N₅O₄
Color Off-white to light yellow
SMILES

O=C(C1=CC(N=C(N2C)NC3=NC4=C(O3)C=CC=C4)=C2C=C1)NCCOCCO
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 (252.90 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

2.5290 mL

12.6451 mL

25.2902 mL

5 mM

0.5058 mL

2.5290 mL

5.0580 mL

10 mM

0.2529 mL

1.2645 mL

2.5290 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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 5 mg/mL (12.65 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 5 mg/mL (12.65 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (12.65 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 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 (278 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Belcher JD, et al. The BACH1 inhibitor ASP8731 inhibits inflammation and vaso-occlusion and induces fetal hemoglobin in sickle cell disease. Front Med (Lausanne). 2023;10:1101501. Published 2023 Apr 18. [Content Brief]

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	2.5290 mL	12.6451 mL	25.2902 mL	63.2255 mL
	5 mM	0.5058 mL	2.5290 mL	5.0580 mL	12.6451 mL
	10 mM	0.2529 mL	1.2645 mL	2.5290 mL	6.3226 mL
	15 mM	0.1686 mL	0.8430 mL	1.6860 mL	4.2150 mL
	20 mM	0.1265 mL	0.6323 mL	1.2645 mL	3.1613 mL
	25 mM	0.1012 mL	0.5058 mL	1.0116 mL	2.5290 mL
	30 mM	0.0843 mL	0.4215 mL	0.8430 mL	2.1075 mL
	40 mM	0.0632 mL	0.3161 mL	0.6323 mL	1.5806 mL
	50 mM	0.0506 mL	0.2529 mL	0.5058 mL	1.2645 mL
	60 mM	0.0422 mL	0.2108 mL	0.4215 mL	1.0538 mL
	80 mM	0.0316 mL	0.1581 mL	0.3161 mL	0.7903 mL
	100 mM	0.0253 mL	0.1265 mL	0.2529 mL	0.6323 mL

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ASP-8731

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Alle Heme Oxygenase (HO) Isoform-spezifische Produkte anzeigen

Alle NF-κB Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ASP-8731 Related Classifications

HY-167874 Related Classifications