2. Immunology/Inflammation Apoptosis
  3. Salt-inducible Kinase (SIK) TNF Receptor Interleukin Related
  4. GLPG4970

GLPG4970 is a potent, selective and orally active salt-inducible kinase 2/3 (SIK2/SIK3) dual inhibitor with IC50 values of 0.3 nM and 0.7 nM. GLPG4970 has weak inhibition of hERG channel with an IC50 of 29 μM. GLPG4970 can decrease TNFα release and increase IL-10 release GLPG4970 can be used for the researches of inflammation and immunology, such as colitis.

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GLPG4970

GLPG4970 Chemical Structure

CAS No. : 3114869-49-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

GLPG4970 Related Antibodies

Top Publications Citing Use of Products

View All Salt-inducible Kinase (SIK) Isoform Specific Products:

View All Isoforms
SIK1 SIK2 SIK3

View All TNF Receptor Isoform Specific Products:

View All Isoforms
TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

View All Interleukin Related Isoform Specific Products:

View All Isoforms
IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GLPG4970 is a potent, selective and orally active salt-inducible kinase 2/3 (SIK2/SIK3) dual inhibitor with IC50 values of 0.3 nM and 0.7 nM. GLPG4970 has weak inhibition of hERG channel with an IC50 of 29 μM. GLPG4970 can decrease TNFα release and increase IL-10 release GLPG4970 can be used for the researches of inflammation and immunology, such as colitis[1].

IC50 & Target[1]

SIK2

0.3 nM (IC50)

SIK3

0.7 nM (IC50)

SIK1

171 nM (IC50)

IL-10

 

In Vitro

GLPG4970 (Compound 8) shows inhibition effect to many off-target Kinases with IC50 range from 4 nM to 292 nM[1].
GLPG4970 induces nuclear translocation of CRTC3 in U2OS cells with an EC50 of 16 nM in U2OS cells[1].
GLPG4970 dose-dependently inhibits TNFα release in monocytes and macrophages stimulated with LPS (HY-D1056), with an IC50 of 3.6 nM and 8.1 nM, respectively[1].
GLPG4970 increases IL-10 release in monocytes and macrophages stimulated with LPS (HY-D1056) [1].

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

GLPG4970 Related Antibodies
Parmacokinetics
Species Dose Route Cmax AUC0-24
Mice[1] 10 mg/kg p.o. 832 ng/mL 9136 ng·h/mL
Mice[1] 3 mg/kg p.o. 249 ng/mL 2156 ng·h/mL
Mice[1] 30 mg/kg p.o. 3797 ng/mL 32943 ng·h/mL
In Vivo

GLPG4970 (Compound 8) (0.5-30 mg/kg, p.o., 15 mins before LPS) decreases TNFα release and increases IL-10 release in LPS (HY-D1056)-treated mice[1].
GLPG4970 (3-30 mg/kg, p.o., twice a day) decreases disease progression in dextran sulfatesodium (DSS)-induced colitis mice models[1].

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

Animal Model: Dextran sulfatesodium (DSS)-induced colitis mice models[1]
Dosage: 3, 10 and 30 mg/kg
Administration: Orally administration, twice a day
Result: Decreased disease progression.
Reduced the AUC of the DAI score by 31, 74 and 72%, respectively.
Molecular Weight

524.58

Formula

C29H31F3N4O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1N(CC(F)(F)F)CCC2=C1C(OC)=CC(C3=CC(C4=CC5=C(C=C4)CC(C)(C)N(C)C5)=CN=C3N)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (190.63 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 1.9063 mL 9.5314 mL 19.0629 mL
5 mM 0.3813 mL 1.9063 mL 3.8126 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, 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5 mg/mL (9.53 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 5 mg/mL (9.53 mM); Clear solution

    This protocol yields a clear solution of ≥ 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 (50.0 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)

g

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
References

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, 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 1.9063 mL 9.5314 mL 19.0629 mL 47.6572 mL
5 mM 0.3813 mL 1.9063 mL 3.8126 mL 9.5314 mL
10 mM 0.1906 mL 0.9531 mL 1.9063 mL 4.7657 mL
15 mM 0.1271 mL 0.6354 mL 1.2709 mL 3.1771 mL
20 mM 0.0953 mL 0.4766 mL 0.9531 mL 2.3829 mL
25 mM 0.0763 mL 0.3813 mL 0.7625 mL 1.9063 mL
30 mM 0.0635 mL 0.3177 mL 0.6354 mL 1.5886 mL
40 mM 0.0477 mL 0.2383 mL 0.4766 mL 1.1914 mL
50 mM 0.0381 mL 0.1906 mL 0.3813 mL 0.9531 mL
60 mM 0.0318 mL 0.1589 mL 0.3177 mL 0.7943 mL
80 mM 0.0238 mL 0.1191 mL 0.2383 mL 0.5957 mL
100 mM 0.0191 mL 0.0953 mL 0.1906 mL 0.4766 mL
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GLPG4970 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:

GLPG49703114869-49-4GLPG 4970GLPG-4970Salt-inducible Kinase (SIK)TNF ReceptorInterleukin RelatedTumor Necrosis Factor ReceptorTNFRILSalt-inducible kinaseSIK2SIK3TNFαIL-10U2OSColitisInhibitorinhibitorinhibit

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