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首页-小分子抑制剂&激动剂-GPCR-Thyrotropin Receptor-SYD5115
SYD5115

Chemical Structure : SYD5115

CAS No.: 3043770-26-6

SYD5115 (SYD-5115, SYD 5115)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 438.52
分子式 C22H32F2N4O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-3,3-dimethylbutan-2-yl (5'-acetyl-4,4-difluoro-6',6'-dimethyl-5',6'-dihydrospiro[cyclohexane-1,7'-pyrrolo[3,2-d]pyrimidin]-2'-yl)carbamate

参考文献

1. Karstens WFJ, et al. Bioorg Med Chem. 2023 Apr 15;84:117258.

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