| Bioactivity | Ogerin is a selective GPR68 positive aliasing modulator (PAM) (pEC50=6.83) with a moderate antagonistic effect on A2A (Ki=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[1][2]. | ||||||||||||
| Target | pEC50: 6.83 (GPR68)Ki: 220 nM (A2A receptoor), 736 nM (5-HT2B receptor) | ||||||||||||
| Invitro | Ogerin (50-150 μM; 72 h) inhibits and partially reverses TGF-β induced pro-fibrotic fibroblast phenotypes in PHLFs[1].Ogerin (50-150 μM; 48 h) inhibits basal and TGF-β induced collagen production at the transcriptional level in PHLFs[1].Ogerin (50, 100 μM; 72 h) shows anti-proliferative effect on TGF-β stimulated PHLFs[1].Ogerin (150 μM; 40 min) activates Gαs signaling in PHLFs[1].Ogerin (50 μM; 10 min) activates the PKA and MAP kinase pathways in HEK293 cells (stably expressing HA-GPR68)[2]. Cell Proliferation Assay[1] Cell Line: | ||||||||||||
| In Vivo | Ogerin (10 mg/kg; single) shows effects that supports a role for GPR68 in hippocampal-associated memory[2]. Animal Model: | ||||||||||||
| Name | Ogerin | ||||||||||||
| CAS | 1309198-71-7 | ||||||||||||
| Formula | C17H17N5O | ||||||||||||
| Molar Mass | 307.35 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |