1. GPCR/G Protein
  2. GPR68
  3. Ogerin

Ogerin 

Cat. No.: HY-110279 Purity: 98.98%
COA Handling Instructions

Ogerin is a selective GPR68 positive aliasing modulator (PAM) (pEC50=6.83) with a moderate antagonistic effect on A2A (Ki=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.

For research use only. We do not sell to patients.

Ogerin Chemical Structure

Ogerin Chemical Structure

CAS No. : 1309198-71-7

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Solution
10 mM * 1 mL in DMSO USD 97 In-stock
Estimated Time of Arrival: December 31
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ready for reconstitution
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5 mg USD 88 In-stock
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10 mg USD 154 In-stock
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25 mg USD 319 In-stock
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50 mg USD 539 In-stock
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100 mg USD 935 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Ogerin is a selective GPR68 positive aliasing modulator (PAM) (pEC50=6.83) with a moderate antagonistic effect on A2A (Ki=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].

IC50 & Target

pEC50: 6.83 (GPR68)[1]
Ki: 220 nM (A2A receptoor), 736 nM (5-HT2B receptor)[1]

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 Gαs 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.
Molecular Weight

307.35

Formula

C17H17N5O

CAS No.
SMILES

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

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
In Vitro: 

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

Preparing
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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (6.77 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (6.77 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (6.77 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Ogerin
Cat. No.:
HY-110279
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