Ogerin 是一种选择性的GPR68正向别构调节剂 (pEC50=6.83)，对A2A具有中度拮抗作用 (Ki=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。
| 生物活性 | Ogerin is a selectiveGPR68positive aliasing modulator (PAM) (pEC50=6.83) with a moderate antagonistic effect onA2A(Ki=220 nM). Ogerin inhibits the fear conditioning reflex in mice and also inhibitsTGF-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]. |
| IC50& Target | pEC50: 6.83 (GPR68)[1]
Ki: 220 nM (A2Areceptoor), 736 nM (5-HT2Breceptor)[1] |
体外研究
(In Vitro) | 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 Gαssignaling 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: | Primary human lung fibroblasts (PHLFs) (TGF-β induced) | | Concentration: | 50, 100 μM | | Incubation Time: | 72 h | | Result: | Inhibited TGF-β stimulated proliferation. |
Cell Viability Assay[2] | Cell Line: | HEK293 cells (stably expressing HA-GPR68) | | Concentration: | 50 μM | | Incubation Time: | 10 min | | Result: | Activated PKA and p42/p44 MAP kinase. |
RT-PCR[1] | Cell Line: | Primary human lung fibroblasts (PHLFs) (TGF-β induced) | | Concentration: | 50-150 μM | | Incubation Time: | 48 h | | Result: | Suppressed TGF-β induced Col1A1 and Col3A1 mRNA levels in a dose-dependent manner.
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Western Blot Analysis[1] | Cell Line: | Primary human lung fibroblasts (PHLFs) (TGF-β induced) | | Concentration: | 150 μM | | Incubation Time: | 40 min (pre-treat) | | Result: | Induced CREB phosphorylation in both non-fibrotic and fibrotic PHLFs. |
Western Blot Analysis[1] | Cell Line: | Primary human lung fibroblasts (PHLFs) (TGF-β induced) | | Concentration: | 50-150 μM | | Incubation Time: | 72 h | | Result: | Inhibited TGF-β induced αSMA expression in a dose-dependent manner. |
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体内研究
(In Vivo) | Ogerin (10 mg/kg; single) shows effects that supports a role for GPR68 in hippocampal-associated memory[2].
| Animal Model: | GPR68 knockout and WT mice[2]. | | Dosage: | 10 mg/kg | | Administration: | Single (30 min before the training) | | Result: | Suppressed recall in fear conditioning in wild-type, but not in GPR68 knockout mice. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 250 mg/mL(813.40 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.2536 mL | 16.2681 mL | 32.5362 mL | | 5 mM | 0.6507 mL | 3.2536 mL | 6.5072 mL | | 10 mM | 0.3254 mL | 1.6268 mL | 3.2536 mL |
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此方案可获得 ≥ 2.08 mg/mL (6.77 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (6.77 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.77 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (6.77 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.77 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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