Selonsertib (Synonyms: GS-4997)

Name: Selonsertib
Brand: MedChemExpress
SKU: HY-18938
Rating: 5.0 (16 reviews)

Cat. No.: HY-18938 Purity: 99.05%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Selonsertib (GS-4997), an orally bioavailable, selective apoptosis signal-regulating kinase 1 (ASK1) inhibitor with a pIC₅₀ of 8.3, has been evaluated as an experimental treatment for diabetic nephropathy and kidney fibrosis.

For research use only. We do not sell to patients.

Selonsertib Chemical Structure

CAS No. : 1448428-04-3

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 101	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 101	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 92	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 121	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 270	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 490	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 704	In-stock	Estimated Time of Arrival: December 31
500 mg		Get quote
1 g		Get quote

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Customer Review

Based on 16 publication(s) in Google Scholar

Other Forms of Selonsertib:

Selonsertib hydrochloride Get quote

15 Publications Citing Use of MCE Selonsertib

Cell Viability Assay

: Selonsertib purchased from MedChemExpress. Usage Cited in: Phytother Res. 2022 Nov 24. [Abstract]; Selonsertib (5 µM) alleviates TMAO-induced morphological changes and improve cellular viability in RTEC cells.

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MAP3K7/TAK1 MAP3K8 ASK2 MAP3K5/ASK1

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

ASK1

8.3 (pIC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HEK-293T	IC₅₀	20 nM Compound: 3	Inhibition of V5 tagged human ASK1 expressed in HEK293T cells assessed as reduction in T848 autophosphorylation incubated for 1 hr by MSD assay Inhibition of V5 tagged human ASK1 expressed in HEK293T cells assessed as reduction in T848 autophosphorylation incubated for 1 hr by MSD assay	[PMID: 32292554]
HEK-293T	IC₅₀	20 nM Compound: 4; GS-4997	Inhibition of V5 tagged human ASK1 expressed in HEK-293T cells assessed as reduction in T838 autophosphorylation incubated for 1 hr Inhibition of V5 tagged human ASK1 expressed in HEK-293T cells assessed as reduction in T838 autophosphorylation incubated for 1 hr	[PMID: 31710475]

In Vitro

Selonsertib (GS-4997) is a clinical stage ASK1 inhibitor, which has been evaluated as an experimental treatment for diabetic nephropathy and kidney fibrosis^[1]. Selonsertib (GS-4997) is a highly selective and potent once-daily oral ASK1 inhibitor that competes with ATP in the ASK1 catalytic kinase domain^[2].

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

Clinical Trial

Molecular Weight

445.49

Formula

C₂₄H₂₄FN₇O

CAS No.

1448428-04-3

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(NC1=NC(C2=NN=CN2C(C)C)=CC=C1)C3=CC(N4C=C(C5CC5)N=C4)=C(C)C=C3F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : ≥ 31 mg/mL (69.59 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2447 mL	11.2236 mL	22.4472 mL
5 mM	0.4489 mL	2.2447 mL	4.4894 mL
10 mM	0.2245 mL	1.1224 mL	2.2447 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.62 mg/mL (5.88 mM); Clear solution
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.67 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.67 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.67 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

mg/kg

Animal weight
(per animal)

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: 99.05%

Select Batch:

Data Sheet (281 KB) SDS (393 KB)

COA (248 KB) LCMS (98 KB)

Handling Instructions (2659 KB)

References

[1]. Lanier M, et al. Structure-Based Design of ASK1 Inhibitors as Potential Agents for Heart Failure. ACS Med Chem Lett. 2017 Feb 8;8(3):316-320. [Content Brief]

[2]. Lin JH, et al. Design of a phase 2 clinical trial of an ASK1 inhibitor, GS-4997, in patients with diabetic kidney disease. Nephron. 2015;129(1):29-33. [Content Brief]

[3]. Loomba R, et al. The ASK1 inhibitor selonsertib in patients with nonalcoholic steatohepatitis: A randomized, phase 2trial. Hepatology. 2018 Feb;67(2):549-559. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2447 mL	11.2236 mL	22.4472 mL	56.1180 mL
	5 mM	0.4489 mL	2.2447 mL	4.4894 mL	11.2236 mL
	10 mM	0.2245 mL	1.1224 mL	2.2447 mL	5.6118 mL
	15 mM	0.1496 mL	0.7482 mL	1.4965 mL	3.7412 mL
	20 mM	0.1122 mL	0.5612 mL	1.1224 mL	2.8059 mL
	25 mM	0.0898 mL	0.4489 mL	0.8979 mL	2.2447 mL
	30 mM	0.0748 mL	0.3741 mL	0.7482 mL	1.8706 mL
	40 mM	0.0561 mL	0.2806 mL	0.5612 mL	1.4029 mL
	50 mM	0.0449 mL	0.2245 mL	0.4489 mL	1.1224 mL
	60 mM	0.0374 mL	0.1871 mL	0.3741 mL	0.9353 mL

Selonsertib 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:

Selonsertib1448428-04-3GS-4997GS4997GS 4997MAP3KApoptosisMAP kinase kinase kinase, MEKK, MAPKKKInhibitorinhibitorinhibit

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Selonsertib (Synonyms: GS-4997)

Customer Review

Other Forms of Selonsertib:

Selonsertib Related Antibodies

15 Publications Citing Use of MCE Selonsertib

Featured Recommendations

•Related Screening Libraries:

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View All MAP3K Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Selonsertib Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

Selonsertib Related Classifications

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