Selgantolimod (Synonyms: GS-9688)

Name: Selgantolimod
Brand: MedChemExpress
SKU: HY-109137
Rating: 4.5 (1 reviews)

Cat. No.: HY-109137 Purity: 98.23%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Selgantolimod (GS-9688) is an orally active, potent and selective toll-like receptor 8 (TLR8) agonist for the treatment of hepatitis B virus (HBV) and human immunodeficiency virus (HIV) infection.

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

Selgantolimod Chemical Structure

CAS No. : 2004677-13-6

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 605	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 605	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 220	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 550	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 950	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 2800	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 4100	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]^[2]

TLR8

HBV

Cellular Effect

Cell Line	Type	Value	Description	References
MT4	CC₅₀	17 μM Compound: (R)-7, GS-9688	Cytotoxicity against human MT4 cells assessed as reduction in cell viability measured after 4 to 5 days by celltiter-glo assay Cytotoxicity against human MT4 cells assessed as reduction in cell viability measured after 4 to 5 days by celltiter-glo assay	[PMID: 32407112]

In Vitro

Selgantolimod induces the cellular immune mediators interleukin (IL)-12 and IL-8, as well as the antiviral cytokines tumor necrosis factor-α and IFN-γ in vitro in human perpheral blood mononuclear cells^[1].
Selgantolimod activates natural killer (NK) and mucosal associated invariant T cells, stimulates cluster of differentiation (CD)-8⁺ T-cell proliferation, and increas IFNγ production, while lowering programmed cell death protein 1 expression by HBV-specific CD8⁺-T cells in vitro in peripheral blood mononuclear cells^[1].
Selgantolimod-induced cytokines reduce HBV DNA, RNA, and antigen levels in HBV-infected primary human hepatocytes^[1].

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

In Vivo

Once-weekly dosing of oral Selgantolimod induces dose-dependent increases in serum IL-12 and IL-1 receptor antagonist (IL-1RA) in cynomolgus monkeys, and leads to functional cure in the woodchuck model of chronic HBV^[1].

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

Clinical Trial

Molecular Weight

293.34

Formula

C₁₄H₂₀FN₅O

CAS No.

2004677-13-6

Appearance

Solid

Color

Light yellow to yellow

SMILES

C[C@@](CCCC)(CO)NC1=NC(N)=NC2=C1N=CC(F)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 62.5 mg/mL (213.06 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.4090 mL	17.0451 mL	34.0901 mL
5 mM	0.6818 mL	3.4090 mL	6.8180 mL
10 mM	0.3409 mL	1.7045 mL	3.4090 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.52 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (8.52 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

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: 98.23%

Select Batch:

Data Sheet (275 KB) SDS (252 KB)

COA (249 KB) LCMS (257 KB)

Handling Instructions (2659 KB)

References

[1]. Jules Levin. Efficacy and Safety of Oral TLR8 Agonist Selgantolimod in Virally Suppressed Adult Patients With Chronic Hepatitis B: a Phase 2, Randomized, Double-Blind, Placebo-Controlled, Multicenter Study. 2019 Nov 8-12.

[2]. Benjamin Ryan. Selgantolimod Shows Promise as Treatment for Hepatitis B. November 18, 2019.

[3]. Romas Geleziunas, et al. Modulators of toll-like receptors for the treatment of hiv. US20170071944A1.

Complete Stock Solution Preparation Table

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

DMSO	1 mM	3.4090 mL	17.0451 mL	34.0901 mL	85.2253 mL
	5 mM	0.6818 mL	3.4090 mL	6.8180 mL	17.0451 mL
	10 mM	0.3409 mL	1.7045 mL	3.4090 mL	8.5225 mL
	15 mM	0.2273 mL	1.1363 mL	2.2727 mL	5.6817 mL
	20 mM	0.1705 mL	0.8523 mL	1.7045 mL	4.2613 mL
	25 mM	0.1364 mL	0.6818 mL	1.3636 mL	3.4090 mL
	30 mM	0.1136 mL	0.5682 mL	1.1363 mL	2.8408 mL
	40 mM	0.0852 mL	0.4261 mL	0.8523 mL	2.1306 mL
	50 mM	0.0682 mL	0.3409 mL	0.6818 mL	1.7045 mL
	60 mM	0.0568 mL	0.2841 mL	0.5682 mL	1.4204 mL
	80 mM	0.0426 mL	0.2131 mL	0.4261 mL	1.0653 mL
	100 mM	0.0341 mL	0.1705 mL	0.3409 mL	0.8523 mL

Selgantolimod Related Classifications

Infection

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.

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Selgantolimod (Synonyms: GS-9688)

Customer Review

Selgantolimod Related Antibodies

Featured Recommendations

•Related Screening Libraries:

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View All Toll-like Receptor (TLR) Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Selgantolimod Related Antibodies

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Complete Stock Solution Preparation Table

Selgantolimod Related Classifications

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