Ogerin 是一种选择性的 GPR68 正向别构调节剂 (pEC₅₀=6.83)，对 A_2A 具有中度拮抗作用 (K_i=220 nM)。Ogerin 能抑制小鼠的恐惧条件反射，还能抑制 TGF-β. 诱导的来自多个器官系统的成纤维细胞的肌成纤维细胞分化。Ogerin 可用于纤维化疾病和神经性疾病的研究。

Ogerin is a selective GPR68 positive aliasing modulator (PAM) (pEC 50 =6.83) with a moderate antagonistic effect on A 2A (K i =220 nM). Ogerin inhibits the fear conditioning reflex in mice and also inhibits TGF-β-induced myofibroblast differentiation of fibroblasts from multiple organ systems. Ogerin can be used in the studies of fibrotic diseases and neurological disorders.

Solid

pEC50: 6.83 (GPR68)
Ki: 220 nM (A2A receptoor), 736 nM (5-HT2B receptor)

Ogerin (50-150 μM; 72 h) inhibits and partially reverses TGF-β induced pro-fibrotic fibroblast phenotypes in PHLFs.
Ogerin (50-150 μM; 48 h) inhibits basal and TGF-β induced collagen production at the transcriptional level in PHLFs.
Ogerin (50, 100 μM; 72 h) shows anti-proliferative effect on TGF-β stimulated PHLFs.
Ogerin (150 μM; 40 min) activates Gαs signaling in PHLFs.
Ogerin (50 μM; 10 min) activates the PKA and MAP kinase pathways in HEK293 cells (stably expressing HA-GPR68). has not independently confirmed the accuracy of these methods. They are for reference only.

Ogerin (10 mg/kg; single) shows effects that supports a role for GPR68 in hippocampal-associated memory. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: GPR68 knockout and WT mice.

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Powder -20°C 3 years；4°C 2 years

[1]. Bell TJ, et al. Ogerin mediated inhibition of TGF-β(1) induced myofibroblast differentiation is potentiated by acidic pH. PLoS One. 2022 Jul 28;17(7):e0271608.
[2]. Huang XP, et al. Allosteric ligands for the pharmacologically dark receptors GPR68 and GPR65. Nature. 2015 Nov 26;527(7579):477-83.

In Vitro: DMSO : 250 mg/mL (813.40 mM; Need ultrasonic)配制储备液