Ogerin

SKU: orb1218944

Description

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.

Key Properties

• CAS Number: 1309198-71-7
• MW: 307.35
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₇N₅O
• SMILES: OCC1=C(C2=NC(N)=NC(NCC3=CC=CC=C3)=N2)C=CC=C1
• Target: 5-HT Receptor
• Solubility: DMSO:250 mg/mL (813.40 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  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.
• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

5-HT Receptor