[CAS NO. 1309198-71-7] Ogerin
PRODUCTS SPECIFICATIONS [1309198-71-7]
DESCRIPTION [1309198-71-7]
Overview
| MDL | MFCD19037230 |
|---|---|
| Molecular Weight | 307.35 |
| Molecular Formula | C17H17N5O |
| SMILES | OCC1=C(C2=NC(N)=NC(NCC3=CC=CC=C3)=N2)C=CC=C1 |
Summary
Ogerin is a selective GPR68 positive aliasing modulator (PAM) ( pEC 50 =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 [1] [2] .
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 Gα
s
signaling in PHLFs
[1]
.
Ogerin (50 μM; 10 min) activates the PKA and MAP kinase pathways in HEK293 cells (stably expressing HA-GPR68)
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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.
|
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. |
In Vivo
Ogerin (10 mg/kg; single) shows effects that supports a role for GPR68 in hippocampal-associated memory [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 250 mg/mL ( 813.40 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
References