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OXGR1 agonist A-1

Chemical Structure : OXGR1 agonist A-1

CAS No.: 84703-35-5

OXGR1 agonist A-1

货号: PC-26371Not For Human Use, Lab Use Only.

OXGR1 agonist A-1 is a potent and selective OXGR1 (Oxoglutarate Receptor 1, GPR99) agonist, activates Gq signaling of OXGR1 with EC50 of 626.5 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

OXGR1 agonist A-1 is a potent and selective OXGR1 (Oxoglutarate Receptor 1, GPR99) agonist, activates Gq signaling of OXGR1 with EC50 of 626.5 nM.
A-1 activates OXGR1 with a potency approximately 60 times stronger compared with α-KG.
A-1 shows no detectable activity for GPR91.
OXGR1-F113L mutant reduced the potency of A-1 by more than 10,000-fold.
A-1 promoted phosphorylation of MYL9 and MLCK expression in VSMCs comparable to α-KG.
A-1 (80 uM) obviously improved rosacea-related phenotypes when applied topically to the back skins of mice.
A-1 mitigates erythema and inflammation with efficacy comparable to first-line therapy while offering enhanced safety in rosacea-like models.

物理化学性质&存储条件

分子量 191.20
分子式 C6H9NO4S
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

methyl (1,1-dioxido-2,3-dihydrothiophen-3-yl)carbamate

参考文献

1. Xiao W, et al. Cell. 2026 Mar 5:S0092-8674(26)00164-9. doi: 10.1016/j.cell.2026.01.036.

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