MedKoo Cat#: 407221 | Name: GSK0660
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

GSK0660 is a selective PPARδ antagonist. GSK0660 differentially regulated 273 transcripts in TNFα-treated cells compared to TNFα alone. A pathway analysis revealed the enrichment of cytokine-cytokine receptor signaling. In particular, GSK0660 blocks the TNFα-induced upregulation of CCL8, a chemokine involved in leukocyte recruitment. GSK0660 blocks the effect of TNFα on the expressions of cytokines involved in leukocyte recruitment, including CCL8, CCL17, and CXCL10 and it may therefore block TNFα-induced retinal leukostasis.

Chemical Structure

GSK0660
GSK0660
CAS#1014691-61-2

Theoretical Analysis

MedKoo Cat#: 407221

Name: GSK0660

CAS#: 1014691-61-2

Chemical Formula: C19H18N2O5S2

Exact Mass: 418.0657

Molecular Weight: 418.48

Elemental Analysis: C, 54.53; H, 4.34; N, 6.69; O, 19.12; S, 15.32

Price and Availability

Size Price Availability Quantity
10mg USD 150.00 Ready to ship
25mg USD 250.00 Ready to ship
50mg USD 450.00 Ready to ship
100mg USD 750.00 Ready to ship
200mg USD 1,250.00 Ready to ship
500mg USD 2,650.00 Ready to ship
1g USD 3,850.00 2 weeks
2g USD 6,450.00 2 weeks
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Related CAS #
No Data
Synonym
GSK0660; GSK-0660; GSK 0660
IUPAC/Chemical Name
methyl 3-(N-(2-methoxy-4-(phenylamino)phenyl)sulfamoyl)thiophene-2-carboxylate
InChi Key
NDFKBGWLUHKMFY-UHFFFAOYSA-N
InChi Code
InChI=1S/C19H18N2O5S2/c1-25-16-12-14(20-13-6-4-3-5-7-13)8-9-15(16)21-28(23,24)17-10-11-27-18(17)19(22)26-2/h3-12,20-21H,1-2H3
SMILES Code
O=C(C1=C(S(=O)(NC2=CC=C(NC3=CC=CC=C3)C=C2OC)=O)C=CS1)OC
Appearance
Solid powder
Purity
>96% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Biological target:
GSK0660 is an antagonist of PPARβ and PPARδ, with IC50s of 155 nM for both isoforms.
In vitro activity:
To determine the effects of PPARβ/δ manipulation, PPARβ/δ inhibition in leukocyte behavior was assessed. As shown in Fig. 4A, treatment of HRMEC (human retinal microvascular endothelial cells) with both 1μM and 10μM GSK0660 significantly inhibited TNFα- (tumor necrosis factor α-) induced cell adhesion by 49.7% (p=0.0291) and 36.8% (p=0.0083), respectively. Reference: Exp Eye Res. 2020 Jan;190:107885. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7426872/
In vivo activity:
PPARβ/δ is involved in TNFα-induced retinal leukostasis in vivo. Intravitreal injections of TNFα increased the number of adherent leukocytes in retinal vessels by 2.3-fold (p=0.0072; Fig. 6A). Co-treatment of TNFα and GSK0660 reduced TNFα-induced leukostasis by 47.1% (p=0.0486). Reference: Exp Eye Res. 2020 Jan;190:107885. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7426872/
Solvent mg/mL mM
Solubility
DMSO 58.3 139.27
DMF 20.0 47.79
DMF:PBS (pH 7.2) (1:3) 0.3 0.60
Ethanol 3.1 7.38
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 418.48 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Capozzi ME, Savage SR, McCollum GW, Hammer SS, Ramos CJ, Yang R, Bretz CA, Penn JS. The peroxisome proliferator-activated receptor-β/δ antagonist GSK0660 mitigates retinal cell inflammation and leukostasis. Exp Eye Res. 2020 Jan;190:107885. doi: 10.1016/j.exer.2019.107885. Epub 2019 Nov 20. PMID: 31758977; PMCID: PMC7426872.
In vitro protocol:
1. Capozzi ME, Savage SR, McCollum GW, Hammer SS, Ramos CJ, Yang R, Bretz CA, Penn JS. The peroxisome proliferator-activated receptor-β/δ antagonist GSK0660 mitigates retinal cell inflammation and leukostasis. Exp Eye Res. 2020 Jan;190:107885. doi: 10.1016/j.exer.2019.107885. Epub 2019 Nov 20. PMID: 31758977; PMCID: PMC7426872.
In vivo protocol:
1. Capozzi ME, Savage SR, McCollum GW, Hammer SS, Ramos CJ, Yang R, Bretz CA, Penn JS. The peroxisome proliferator-activated receptor-β/δ antagonist GSK0660 mitigates retinal cell inflammation and leukostasis. Exp Eye Res. 2020 Jan;190:107885. doi: 10.1016/j.exer.2019.107885. Epub 2019 Nov 20. PMID: 31758977; PMCID: PMC7426872.
1: Savage SR, McCollum GW, Yang R, Penn JS. RNA-seq identifies a role for the PPARβ/δ inverse agonist GSK0660 in the regulation of TNFα-induced cytokine signaling in retinal endothelial cells. Mol Vis. 2015 May 20;21:568-76. eCollection 2015. PubMed PMID: 26015769; PubMed Central PMCID: PMC4443583.