Cat. No.: HY-131969

ASK1-IN-2

고객리뷰

Based on 1 Customer Validation

ASK1-IN-2 is a potent and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC₅₀ of 32.8 nM. ASK1-IN-2 can be used for the research of ulcerative colitis.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity: 99.37%
CAS No.: 2541792-70-3
화학식: C₁₉H₁₇FN₆O
분자량:364.38

보관:

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

ASK1-IN-2 Chemical Structure

CAS No.: 2541792-70-3

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
용액&용해도
- In Vitro
- In Vivo
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

ASK1-IN-2 is a potent and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC₅₀ of 32.8 nM. ASK1-IN-2 can be used for the research of ulcerative colitis^[1].

IC₅₀ & Target^[1]

ASK1

32.8 nM (IC₅₀)

All MAP3K Isoforms :

In Vitro

ASK1-IN-2 (compound 19) (10 mM; 1 h) inhibits the luciferase reporter activity in AP1-HEK293 cells, with inhibition rate of 95.59%^[1].

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

In Vivo

ASK1-IN-2 (25 mg/kg; p.o. daily for 7 d) improves dextran sulphate sodium (DSS)-induced ulcerative colitis (UC) in mice^[1].
ASK1-IN-2 (25 mg/kg; p.o. daily for 7 d) blocks ASK1-p38/JNK signaling pathways and reduces inflammatory cytokine levels in DSS-induced mouse colon tissues^[1].
ASK1-IN-2 (1 mg/kg; i.v.) shows low clearance (CL=1.38 L/h/kg) and moderate half-life (T_1/2=1.45 h) in rats^[1].
ASK1-IN-2 (10 mg/kg; p.o.) shows high oral exposure (AUC_last=4517 h ng/mL), 62.2% oral bioavailability and acceptable terminal half-life (T_1/2=2.31 h) in rats^[1].

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

Animal Model:

Male ICR mice (18-22 g, 6-8 weeks) were given 3% DSS (w/v) orally in drinking water^[1]
Dosage:

25 mg/kg
Administration:

P.o. daily for 7 days
Result:

Induced a significant recovery of body weight loss, with an increase of +11.2%.
Decreased the disease activity index (DAI) score about a 2 unit.
Significantly prevented colon shortening.
Attenuated a severe colonic tissue damage and infiltration of inflammatory cells.

Animal Model:

Male SD rats ^[1]
Dosage:

1 mg/kg for i.v.; 10 mg/kg for p.o. (Pharmacokinetic Analysis)
Administration:

I.v. and p.o. administration
Result:

I.v.: CL=1.38 L/h/kg; T_1/2=1.45 h.
P.o.: AUC_last=4517 h•ng/mL; F=62.2%; T_1/2=2.31 h.

Chemical Information

CAS No. 2541792-70-3
Appearance Solid
분자량 364.38
화학식 C₁₉H₁₇FN₆O
Color White to off-white
SMILES

O=C(C(N1)=CC2=C1C=C(F)C=C2)NC3=NC(C4=NN=CN4C(C)C)=CC=C3
선적

Room temperature in continental US; may vary elsewhere.

보관

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

용액&용해도

In Vitro:

DMSO : 250 mg/mL (686.10 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

2.7444 mL

13.7219 mL

27.4439 mL

5 mM

0.5489 mL

2.7444 mL

5.4888 mL

10 mM

0.2744 mL

1.3722 mL

2.7444 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.

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: ≥ 2.08 mg/mL (5.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% Corn Oil

Solubility: ≥ 2.08 mg/mL (5.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 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)

References

[1]. Hou S, et, al. Structure-based discovery of 1H-indole-2-carboxamide derivatives as potent ASK1 inhibitors for potential treatment of ulcerative colitis. Eur J Med Chem. 2020 Dec 24;211:113114. [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	2.7444 mL	13.7219 mL	27.4439 mL	68.6097 mL
	5 mM	0.5489 mL	2.7444 mL	5.4888 mL	13.7219 mL
	10 mM	0.2744 mL	1.3722 mL	2.7444 mL	6.8610 mL
	15 mM	0.1830 mL	0.9148 mL	1.8296 mL	4.5740 mL
	20 mM	0.1372 mL	0.6861 mL	1.3722 mL	3.4305 mL
	25 mM	0.1098 mL	0.5489 mL	1.0978 mL	2.7444 mL
	30 mM	0.0915 mL	0.4574 mL	0.9148 mL	2.2870 mL
	40 mM	0.0686 mL	0.3430 mL	0.6861 mL	1.7152 mL
	50 mM	0.0549 mL	0.2744 mL	0.5489 mL	1.3722 mL
	60 mM	0.0457 mL	0.2287 mL	0.4574 mL	1.1435 mL
	80 mM	0.0343 mL	0.1715 mL	0.3430 mL	0.8576 mL
	100 mM	0.0274 mL	0.1372 mL	0.2744 mL	0.6861 mL

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ASK1-IN-2

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Oxygen Sensing Compound Library

Orally Active Compound Library

Anti-Obesity Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

All MAP3K Isoforms

Biological Activity

Chemical Information

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

ASK1-IN-2

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Oxygen Sensing Compound Library

Orally Active Compound Library

Anti-Obesity Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

All MAP3K Isoforms

Biological Activity

Chemical Information

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

ASK1-IN-2 Related Classifications

HY-131969 Related Classifications