Art. -Nr.: HY-150203

GLPG3970

Name: GLPG3970
Brand: MedChemExpress
SKU: HY-150203
Price: 200.00 USD
Availability: InStock
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GLPG3970 (compound 88) is a first-in-class SIK2/SIK3 inhibitor. GLPG3970 can be used for the research of inflammation and autoimmune disease.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 99.70%
CAS. Nr.: 2403733-82-2
Formel: C₂₅H₂₇F₃N₄O₄
Molecular Weight:504.50

Speicherung:

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

GLPG3970 Chemical Structure

CAS. Nr.: 2403733-82-2

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll (1)
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

GLPG3970 (compound 88) is a first-in-class SIK2/SIK3 inhibitor. GLPG3970 can be used for the research of inflammation and autoimmune disease^[1].

Alle Salt-inducible Kinase (SIK) Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Monocyte	EC₅₀	1087 nM Compound: 3	Induction of IL-10 expression in human CD14+ monocytes isolated from PBMC measured incubated for 1 hr followed by LPS addition further incubated for 2 hrs by ELISA assay Induction of IL-10 expression in human CD14+ monocytes isolated from PBMC measured incubated for 1 hr followed by LPS addition further incubated for 2 hrs by ELISA assay	[PMID: 37467565]
Monocyte	IC₅₀	133 nM Compound: 3	Reduction in LPS-stimulated TNFalpha production in human CD14+ monocytes isolated from PBMC measured after 4 hrs Reduction in LPS-stimulated TNFalpha production in human CD14+ monocytes isolated from PBMC measured after 4 hrs	[PMID: 37467565]

In Vivo

GLPG3970 (10 mg/kg; oral administration; twice daily for 5 consecutive days) decreases the ear thickness of murine models of psoriatic-like epidermal hyperplasia induced by intradermal injections of IL-23^[1].
GLPG3970 (60 mg/kg; oral administration; twice daily until mice are sacrificed) shows better clinical manifestations compared to vehicle groups in murine collagen-antibody induced arthritis model (CAIA)^[1].
GLPG3970 (30 mg/kg; oral administration; twice daily for 7 consecutive days) reduces disease activity index ompared to vehicle groups in mice T cell transfer model^[1].

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

Clinical Trial

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

Chemical Information

CAS. Nr. 2403733-82-2
Appearance Solid
Molecular Weight 504.50
Formel C₂₅H₂₇F₃N₄O₄
Color White to off-white
SMILES

O=C1C2=C(CCN1CC(F)(F)F)C=C(C3=CN=C4C=C(C=CN43)OCCN5CCOCC5)C=C2OC
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 (198.22 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

1.9822 mL

9.9108 mL

19.8216 mL

5 mM

0.3964 mL

1.9822 mL

3.9643 mL

10 mM

0.1982 mL

0.9911 mL

1.9822 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: 2.5 mg/mL (4.96 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.

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.

Protocol 2

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

Solubility: 2.5 mg/mL (4.96 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (4.96 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. 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 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

Protokoll

All Signal Pathway Related

Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 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]. DESROY N, et al. NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF DISEASES. WO/2019/238424. 2019.

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	1.9822 mL	9.9108 mL	19.8216 mL	49.5540 mL
	5 mM	0.3964 mL	1.9822 mL	3.9643 mL	9.9108 mL
	10 mM	0.1982 mL	0.9911 mL	1.9822 mL	4.9554 mL
	15 mM	0.1321 mL	0.6607 mL	1.3214 mL	3.3036 mL
	20 mM	0.0991 mL	0.4955 mL	0.9911 mL	2.4777 mL
	25 mM	0.0793 mL	0.3964 mL	0.7929 mL	1.9822 mL
	30 mM	0.0661 mL	0.3304 mL	0.6607 mL	1.6518 mL
	40 mM	0.0496 mL	0.2478 mL	0.4955 mL	1.2389 mL
	50 mM	0.0396 mL	0.1982 mL	0.3964 mL	0.9911 mL
	60 mM	0.0330 mL	0.1652 mL	0.3304 mL	0.8259 mL
	80 mM	0.0248 mL	0.1239 mL	0.2478 mL	0.6194 mL
	100 mM	0.0198 mL	0.0991 mL	0.1982 mL	0.4955 mL

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GLPG3970

Alle Salt-inducible Kinase (SIK) Isoform-spezifische Produkte anzeigen