Ogerin
Based on 3 publication(s) in Google Scholar
Ogerin, a chemical probe, 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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- Reinheit: 99.94%
- CAS. Nr.: 1309198-71-7
- Formel: C17H17N5O
- Molecular Weight:307.35
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Ogerin
More
Biologische Aktivität
pEC50: 6.83 (GPR68)[1]
Ki: 220 nM (A2A receptoor), 736 nM (5-HT2B receptor)[1]
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.
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Cell Line:Primary human lung fibroblasts (PHLFs) (TGF-β induced)
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Concentration:50, 100 μM
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Incubation Time:72 h
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Result:Inhibited TGF-β stimulated proliferation.
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Cell Line:HEK293 cells (stably expressing HA-GPR68)
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Concentration:50 μM
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Incubation Time:10 min
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Result:Activated PKA and p42/p44 MAP kinase.
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Cell Line:Primary human lung fibroblasts (PHLFs) (TGF-β induced)
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Concentration:50-150 μM
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Incubation Time:48 h
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Result:Suppressed TGF-β induced Col1A1 and Col3A1 mRNA levels in a dose-dependent manner.
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Cell Line:Primary human lung fibroblasts (PHLFs) (TGF-β induced)
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Concentration:150 μM
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Incubation Time:40 min (pre-treat)
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Result:Induced CREB phosphorylation in both non-fibrotic and fibrotic PHLFs.
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Cell Line:Primary human lung fibroblasts (PHLFs) (TGF-β induced)
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Concentration:50-150 μM
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Incubation Time:72 h
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Result:Inhibited TGF-β induced αSMA expression in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:GPR68 knockout and WT mice[2].
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Dosage:10 mg/kg
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Administration:Single (30 min before the training)
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Result:Suppressed recall in fear conditioning in wild-type, but not in GPR68 knockout mice.
Chemical Information
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CAS. Nr. 1309198-71-7
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Appearance Solid
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Molecular Weight 307.35
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Formel C17H17N5O
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Color White to off-white
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SMILES
OCC1=C(C2=NC(N)=NC(NCC3=CC=CC=C3)=N2)C=CC=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Brain Res Bull
Neuroprotective effects of GPR68 against cerebral ischemia-reperfusion injury via the NF-κB/Hif-1α pathway. [Abstract]2024 Oct 1:216:111050. PMID: 39147243 -
Lösungsmittel & Löslichkeit
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)
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Reinheit & Dokumentation
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Data Sheet (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Bell TJ, et al. Ogerin mediated inhibition of TGF-β(1) induced myofibroblast differentiation is potentiated by acidic pH. PLoS One. 2022 Jul 28;17(7):e0271608. [Content Brief]
[2]. Huang XP, et al. Allosteric ligands for the pharmacologically dark receptors GPR68 and GPR65. Nature. 2015 Nov 26;527(7579):477-83. [Content Brief]
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 |
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| 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 |
Ogerin Related Classifications
HY-110279 Related Classifications
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