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

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.

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Ogerin Chemical Structure

Ogerin Chemical Structure

CAS No. : 1309198-71-7

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Customer Review

Based on 1 publication(s) in Google Scholar

Ogerin Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Ogerin

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Ogerin Related Antibodies

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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (813.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
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%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2536 mL 16.2681 mL 32.5362 mL 81.3405 mL
5 mM 0.6507 mL 3.2536 mL 6.5072 mL 16.2681 mL
10 mM 0.3254 mL 1.6268 mL 3.2536 mL 8.1340 mL
15 mM 0.2169 mL 1.0845 mL 2.1691 mL 5.4227 mL
20 mM 0.1627 mL 0.8134 mL 1.6268 mL 4.0670 mL
25 mM 0.1301 mL 0.6507 mL 1.3014 mL 3.2536 mL
30 mM 0.1085 mL 0.5423 mL 1.0845 mL 2.7113 mL
40 mM 0.0813 mL 0.4067 mL 0.8134 mL 2.0335 mL
50 mM 0.0651 mL 0.3254 mL 0.6507 mL 1.6268 mL
60 mM 0.0542 mL 0.2711 mL 0.5423 mL 1.3557 mL
80 mM 0.0407 mL 0.2034 mL 0.4067 mL 1.0168 mL
100 mM 0.0325 mL 0.1627 mL 0.3254 mL 0.8134 mL
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Ogerin Related Classifications

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.

Keywords:

Ogerin1309198-71-7GPR68G Protein-Coupled Receptor 68fibrotic diseasesfibroblastsTGF-βHEK293A2AInhibitorinhibitorinhibit

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