Ogerin|cas:1309198-71-7|西域试剂

Ogerin,98.98%

产品编号：Bellancom-110279| CAS NO：1309198-71-7| 分子式：C₁₇H₁₇N₅O| 分子量：307.35

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货号	价格	库存与货期
Bellancom-110279	￥900.00	杭州北京（现货）
Bellancom-110279	￥1600.00	杭州北京（现货）
Bellancom-110279	￥3300.00	杭州北京（现货）
Bellancom-110279	￥5600.00	杭州北京（现货）
Bellancom-110279	￥9500.00	杭州北京（现货）

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Ogerin

产品介绍

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。

生物活性

Ogerin is a selective GPR68 positive aliasing modulator (PAM) (pEC₅₀=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.

体外研究

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 Gα_s signaling in PHLFs.
Ogerin (50 μM; 10 min) activates the PKA and MAP kinase pathways in HEK293 cells (stably expressing HA-GPR68).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

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

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

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.

Western Blot Analysis

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

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.

体内研究
(In Vivo)

Ogerin (10 mg/kg; single) shows effects that supports a role for GPR68 in hippocampal-associated memory.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	GPR68 knockout and WT mice.
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.

体内研究

Ogerin (10 mg/kg; single) shows effects that supports a role for GPR68 in hippocampal-associated memory.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	GPR68 knockout and WT mice.
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.

体内研究

Ogerin (10 mg/kg; single) shows effects that supports a role for GPR68 in hippocampal-associated memory.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	GPR68 knockout and WT mice.
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (813.40 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% 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 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
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。