GSK0660
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MedKoo CAT#: 407221

CAS#: 1014691-61-2

Description: 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

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GSK0660
CAS# 1014691-61-2
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 407221
Name: GSK0660
CAS#: 1014691-61-2
Chemical Formula: C19H18N2O5S2
Exact Mass: 418.07
Molecular Weight: 418.480
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 Ready to ship
25mg USD 250 Ready to ship
50mg USD 450 Ready to ship
100mg USD 750 Ready to ship
200mg USD 1250 Ready to ship
500mg USD 2650 Ready to ship
1g USD 3850 2 weeks
2g USD 6450 2 weeks
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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/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. 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

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.

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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.