Ogerin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Ogerin 是一种选择性 GPR68 正变构调节剂 (pEC50: 6.83)。奥杰林阻断小鼠恐惧条件反射的回忆。

Ogerin is a selective GPR68 positive allosteric modulator (pEC50: 6.83). Ogerin blocks recall in fear conditioning in mice. Ogerin displays inverse agonist and antagonist activity (Ki, 220 nM) at A2A receptor and weak antagonist activity (Ki, 736 nM) at 5-HT2B receptor.

Cell Proliferation Assay Cell Line:Primary human lung fibroblasts (PHLFs) (TGF-β induced)Concentration:50, 100 μMIncubation Time:72 hResult: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 hResult:Inhibited TGF-β induced αSMA expression in a dose-dependent manner.

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.

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Endocrinology/Hormones

5-HT Receptor

5-HT2B|A2A|GPR68

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1309198-71-7

307.35

C17H17N5O

>98% (HPLC)

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

OCC1=C(C2=NC(N)=NC(NCC3=CC=CC=C3)=N2)C=CC=C1

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(-20℃)

With Ice Pack

≥ 2 years