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Chemical Structure : SYD5115
Catalog No.: PC-20498Not For Human Use, Lab Use Only.
SYD5115 (SYD-5115) is a potent, selective and orally bioavailable thyrotropin receptor (TSH-R) antagonist with IC50 of 48 and 62 nM for rTSHR and hTSHR, respectively.
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SYD5115 (SYD-5115) is a potent, selective and orally bioavailable thyrotropin receptor (TSH-R) antagonist with IC50 of 48 and 62 nM for rTSHR and hTSHR, respectively.
SYD5115 potently blocks the TSH-induced cAMP production by rat and human TSH-R in HEK293-hTSHR cells with IC50 of 69 nM.
SYD5115 antagonizes TSH-R stimulating autoantibody M22-induced cAMP response in rat FRTL-5 cell with IC50 of 22 nM.
SYD5115 also is a potent TSH-R antagonist when tested on primary orbital fibroblasts of GD and GO patients (GOFs) and is also able to block TSH-R-stimulation by stimulating TSH-R-antibody containing sera of GD patients on TSH-R overexpressing CHO-cells.
SYD5115 alsois a relatively potent antagonist for the hFSH-R (IC50 = 259 nM), but shows very high selectivity over the also closely related hLH-R (IC50 >10 uM).
YD5115 (50 and 100 µmol/kg) inhibits M22-induced FT4 release in vivo.
| M.Wt | 438.52 | |
| Formula | C22H32F2N4O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Karstens WFJ, et al. Bioorg Med Chem. 2023 Apr 15;84:117258.
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