Chemical Structure : ADGRD1 agonist GL64
货号: PC-24994Not For Human Use, Lab Use Only.
ADGRD1 agonist GL64 is a selective agonist of ADGRD1/GPR133 with EC50 of 3.98 uM in CRE-luciferase assays in ADGRD1-overexpressing HEK293T cells.
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ADGRD1 agonist GL64 is a selective agonist of ADGRD1/GPR133 with EC50 of 3.98 uM in CRE-luciferase assays in ADGRD1-overexpressing HEK293T cells.
GL64 shows no effect in HEK293T cells overexpressing adhesion GPCRs, such as ADGRD2, ADGRG5, ADGRG6, CELSR1, CELSR2, CELSR3, and ADGRG4.
GL64 also does not activate nonadhesion GPCRs, including GPR68, NPFFR1, GPR183, and GPRC5B.
GL64 (10 μM) inhibits the differentiation of male WT BMMs into mature osteoclasts but had no effect on Adgrd1−/− cells, down-regulates the expression levels of osteoclastogenesis-related genes, including Dc-stamp, Acp5, and Nfatc1, during male mouse osteoclast maturation.
GL64 regulates osteoclast maturation through the cAMP-PKA-NFATC1 pathway.
GL64 (30 mg/kg, i.p.) rescues ovariectomy-induced bone loss and osteoclast hyperactivity in OVX-induced osteoporosis mice.
分子量 | 509.81 | |
分子式 | C27H19Cl3N2O2 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. He L, et al. Sci Adv. 2025 Jul 11;11(28):eads3829.
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