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GLPG3970 SIK inhibitor

Name: GLPG3970
Brand: Selleck Chemicals
SKU: E1997
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.E1997

GLPG3970 (compound 32) is a dual inhibitor of SIK2 and SIK3, with IC50 of 282.8 nM, 7.8 nM and 3.8 nM for SIK1, SIK2 and SIK3, respectively. It has the potential to treat autoimmune and inflammatory diseases.

Chemical Structure

Molecular Weight: 504.50

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Quality Control

Batch: E199701 DMSO]100 mg/mL]false]Ethanol]100 mg/mL]false]Water]Insoluble]false Purity: 99.57%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS/MSDS
Datasheet

99.57

Related Targets	PD-1/PD-L1 CXCR STING AhR Immunology & Inflammation related CD markers Interleukins Anti-infection Antioxidant COX
Other SIK Inhibitors	HG-9-91-01 ARN-3236 YKL-05-099 GLPG3312 PF-07899895 YKL 06-061

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (198.21 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (9.91mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/ml (0.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

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
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	504.50	Formula	C₂₅H₂₇F₃N₄O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	2403733-82-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Read more about storage stability stock solution CAS number

Mechanism of Action

Targets/IC₅₀/Ki	SIK3 3.8 nM SIK2 7.8 nM SIK1 282.8 nM
References	[1] https://pubmed.ncbi.nlm.nih.gov/38552030/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2023-09-18)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04700280	TERMINATED	Primary Sjögren Syndrome	Lakefront Biotherapeutics NV	2021-01-28	PHASE2
NCT04700267	TERMINATED	Systemic Lupus Erythematosus	Lakefront Biotherapeutics NV	2020-12-28	PHASE1
NCT04907149	COMPLETED	Healthy	Lakefront Biotherapeutics NV	2021-06-07	PHASE1
NCT04577794	COMPLETED	Ulcerative Colitis	Lakefront Biotherapeutics NV	2020-10-05	PHASE2
NCT04720183	COMPLETED	Healthy	Lakefront Biotherapeutics NV	2021-01-11	PHASE1
NCT04577781	COMPLETED	Rheumatoid Arthritis	Lakefront Biotherapeutics NV	2020-10-12	PHASE2

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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