NCGC00379308 (Synonyms: (D3-βArr;NCGC-00379308;NCGC 00379308)) |
| カタログ番号GC19543 |
NCGC00379308 は、チロトロピン受容体 (TSHR) のポジティブ アロステリック モジュレーターであり、TSHR の直接活性化によって β-Arr 1 の転座を開始し、in vitro で TSH を介した前骨芽細胞の分化を増強します。
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Cas No.: 662164-09-2
Sample solution is provided at 25 µL, 10mM.
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A potent, functionally selective TSH receptor (TSHR) positive allosteric modulator with EC50 of 11.6 uM (β-Arr 1 translocation); does not activate β-Arr 1 translocation to the GLP1R, binds and activates the TSHR and has no agonistic effect on cAMP production nor inhibit TSH-induced cAMP production in DiscoverX1 cells and primary cultures of human thyrocytes; potentiates TSH-induced upregulation of ALPL and OPN mRNA levels, and increases TSH-induced secretion of OPN protein; potentiates the effect of TSH to enhance differentiation of a human preosteoblast in an in vitro model
Reference:
[1]. Neumann S, et al. J Pharmacol Exp Ther. 2018 Jan;364(1):38-45..
Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)
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