2. Immunology/Inflammation Apoptosis
  3. Toll-like Receptor (TLR) IFNAR TNF Receptor
  4. GSK2245035

GSK2245035 is a highly potent and selective intranasal Toll-Like receptor 7 (TLR7) agonist with preferential Type-1 interferon (IFN)-stimulating properties. GSK2245035 has pEC50s of 9.3 and 6.5 for IFNα and TFNα. GSK2245035 effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood cell cultures. GSK2245035 is used for asthma.

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GSK2245035 Chemical Structure

GSK2245035 Chemical Structure

CAS No. : 1207629-49-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 363 In-stock
Solution
10 mM * 1 mL in DMSO USD 363 In-stock
Solid
5 mg USD 330 In-stock
10 mg USD 528 In-stock
50 mg USD 1485 In-stock
100 mg USD 1980 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of GSK2245035:

GSK2245035 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE GSK2245035

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

View All Isoforms
TLR3 TLR8 TLR9 TLR2 TLR4 TLR7 TLR1 TLR6

View All TNF Receptor Isoform Specific Products:

View All Isoforms
TNFRSF1A/CD120a TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GSK2245035 is a highly potent and selective intranasal Toll-Like receptor 7 (TLR7) agonist with preferential Type-1 interferon (IFN)-stimulating properties. GSK2245035 has pEC50s of 9.3 and 6.5 for IFNα and TFNα. GSK2245035 effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood cell cultures. GSK2245035 is used for asthma[1].

IC50 & Target[1]

TLR7

 

IFNα

9.3 (pEC50)

CD40

6.5 (pEC50)

In Vitro

GSK2245035 (0.01, 0.1, 1, 10, 100, 1000, 10000 nM; 6 days) reduces levels of the Th2 cytokines IL-5 and IL-13 released in response to Timothy grass or house dust mite in human PBMC cultures derived from individuals allergic to these allergens, in a dose-dependent manner[1].

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

GSK2245035 Related Antibodies
In Vivo

GSK2245035 (i.n.; 0.03-1 mg/kg; 6 hours) makes dose-related increasing in IFNα levels in serum at doses of 0.3 mg/kg and above at the 2 h time point which had subsided at 6 h[1].
GSK2245035 (3, 30, 300, 3000 ng/kg; 6 hours) treatment can make plasma IP-10 provided the most sensitive biomarker of target engagement with raised levels of this chemokine detected at doses of 30 ng/kg and above in the cynomolgus monkey[1].

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

Animal Model: Female BALB/c mice[1]
Dosage: 0.03, 0.1, 0.3, 1 mg/kg
Administration: Intranasally (i.n.); 6 hours
Result: Dose-related increases in IFNα levels in serum were detected at doses of 0.3 mg/kg and above at the 2 h time point which had subsided at 6 h.
Clinical Trial
Molecular Weight

390.52

Formula

C20H34N6O2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1NC2=C(N=C(N=C2N1CCCCCN3CCCCC3)O[C@H](CCC)C)N
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 : 125 mg/mL (320.09 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 2.5607 mL 12.8034 mL 25.6069 mL
5 mM 0.5121 mL 2.5607 mL 5.1214 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
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Concentration
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Volume
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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (5.33 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 2

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

    Solubility: ≥ 2.08 mg/mL (5.33 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.
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 2.5607 mL 12.8034 mL 25.6069 mL 64.0172 mL
5 mM 0.5121 mL 2.5607 mL 5.1214 mL 12.8034 mL
10 mM 0.2561 mL 1.2803 mL 2.5607 mL 6.4017 mL
15 mM 0.1707 mL 0.8536 mL 1.7071 mL 4.2678 mL
20 mM 0.1280 mL 0.6402 mL 1.2803 mL 3.2009 mL
25 mM 0.1024 mL 0.5121 mL 1.0243 mL 2.5607 mL
30 mM 0.0854 mL 0.4268 mL 0.8536 mL 2.1339 mL
40 mM 0.0640 mL 0.3201 mL 0.6402 mL 1.6004 mL
50 mM 0.0512 mL 0.2561 mL 0.5121 mL 1.2803 mL
60 mM 0.0427 mL 0.2134 mL 0.4268 mL 1.0670 mL
80 mM 0.0320 mL 0.1600 mL 0.3201 mL 0.8002 mL
100 mM 0.0256 mL 0.1280 mL 0.2561 mL 0.6402 mL
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GSK2245035 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:

GSK22450351207629-49-9GSK 2245035GSK-2245035Toll-like Receptor (TLR)IFNARTNF ReceptorInterferon-α/β receptorInterferon-alpha/beta receptor Tumor Necrosis Factor ReceptorTNFRintranasalpreferentialType-1interferonallergen-inducedTh2cytokineperipheralbloodasthmaInhibitorinhibitorinhibit

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