THIQ 是一种选择性黑皮质素 4 受体 (MC4R) 激动剂,对 hMC4R 和 rMC4R 的 IC50 分别为 1.2 和 0.6 nM。
产品描述
THIQ is a selective melanocortin-4 receptor (MC4R) agonist (hMC4R and rMC4R with IC50 of 1.2 nM and 0.6 nM , respectively).
体外活性
THIQ,?a small molecule agonist of the MC4R, on the cell surface expression and signaling of ten intracellularly retained MC4R mutants using different cell lines.?THIQ increased the cell surface expression of three mutants (N62S, C84R, and C271Y) and two of them (N62S and C84R) had increased signaling in HEK293 cells.THIQ increased the signaling of two other mutants (P78L and P260Q) without increasing their cell surface expression in HEK293 cells.?In neuronal cells, THIQ exhibited a more potent effect, correcting the cell surface expression and signaling of seven mutants (N62S, I69R, P78L, C84R, W174C, P260Q, and C271Y).
Cas No.
312637-48-2
分子式
C33H41ClN6O2
分子量
589.18
储存和溶解度
DMSO:245 mg/ml(415.84 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years