1. Metabolic Enzyme/Protease
  2. ROR
  3. GSK805

GSK805 

Cat. No.: HY-12776 Purity: 97.14%
Handling Instructions

GSK805 is a potent, orally bioavailable, and CNS penetrant RORγt inhibitor with pIC50 of 8.4 and >8.2 for RORγ FRET assay and Th17 assay.

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

GSK805 Chemical Structure

GSK805 Chemical Structure

CAS No. : 1426802-50-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 187 In-stock
Estimated Time of Arrival: December 31
1 mg USD 55 In-stock
Estimated Time of Arrival: December 31
5 mg USD 160 In-stock
Estimated Time of Arrival: December 31
10 mg USD 280 In-stock
Estimated Time of Arrival: December 31
25 mg USD 560 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1750 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

Publications Citing Use of MCE GSK805

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  • Protocol

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  • References

  • Customer Review

Description

GSK805 is a potent, orally bioavailable, and CNS penetrant RORγt inhibitor with pIC50 of 8.4 and >8.2 for RORγ FRET assay and Th17 assay[1].

IC50 & Target

IC50: 8.4 (RORγt)[1]

Molecular Weight

532.36

Formula

C₂₃H₁₈Cl₂F₃NO₄S

CAS No.

1426802-50-7

SMILES

O=C(NC1=CC(Cl)=C(C2=CC=CC=C2OC(F)(F)F)C(Cl)=C1)CC3=CC=C(S(=O)(CC)=O)C=C3

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 (187.84 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8784 mL 9.3921 mL 18.7843 mL
5 mM 0.3757 mL 1.8784 mL 3.7569 mL
10 mM 0.1878 mL 0.9392 mL 1.8784 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.70 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.70 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

Animal administration[1]
GSK805 are orally administered once daily at 3 doses (1, 3, and 10 mg/kg) to EAE mice from the day of immunization. Compared to the control, the treatment with 9a or 9g resulted in a delay and significant reduction in clinical severity of EAE in a dose-dependent manner. Compared to thiazole ketone amide 2, which only showed EAE efficacy up to day 20 at 100 mg/kg twice daily dosing,32 the biaryl amides 9a and 9g are much more efficacious. This could be attributed to their good in vitro activities as well as much improved oral exposure and CNS penetration. However, it should be noted that although 9g had more brain exposure than 9a, it exhibited less efficacy than 9a in EAE experiments, indicating that there might be additional factors such as "free" brain concentration affecting in vivo efficacy[1].

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

References
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Product name:
GSK805
Cat. No.:
HY-12776
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