| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
The primary target of Ogerin is GPR68, a proton-sensing GPCR. It acts as a selective positive allosteric modulator of GPR68 with a pEC50 of 6.83. It also displays inverse agonist and antagonist activity at the A2A receptor (Ki = 220 nM) and weak antagonist activity at the 5-HT2B receptor (Ki = 736 nM). By modulating GPR68, it affects fibrotic and neurological processes.
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| ln Vitro |
In PHLFs, agerin (50-150 μM; 72 h) partially reverses and alters the profibrotic fibroblast phenotype generated by TGF-β [1]. Ogerin (50-150 μM; 48 h) partially reverses and alters the profibrotic fibroblast phenotype that TGF-β induces in PHLFs [1]. PHLFs' enhanced TGF-β-induced collagen synthesis is impacted by agerin (50, 100 μM; 72 hours)[1]. In PHLFs, agerin (150 μM; 40 min) stimulates TGF-β-induced collagen synthesis [1]. Ogerin (50 μM; 10 min) causes HEK293 cells that are stably expressing HA-GPR68 to activate PKA and MAP [2].
In vitro, Ogerin is a selective GPR68 PAM with a pEC50 of 6.83. It displays inverse agonist and antagonist activity at the A2A receptor (Ki = 220 nM) and weak antagonist activity at the 5-HT2B receptor (Ki = 736 nM). Its activity at GPR68 is measured using calcium mobilization assays or other functional readouts. |
| ln Vivo |
It has been demonstrated that agerin (10 mg/kg; single dose) supports GPR68's involvement in hippocampal-related memory [2].
In vivo, Ogerin inhibits fear conditioning in mice. It inhibits TGF-β-induced myofibroblast differentiation of fibroblasts from multiple organ systems. These effects suggest potential for treating fibrotic diseases and neurological disorders. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for Ogerin involve radioligand binding studies using cell membranes expressing GPR68, A2A, or 5-HT2B receptors. Competitive binding assays are performed using selective radiolabeled ligands to determine the compound's affinity (Ki) for these receptors. Functional assays (e.g., calcium mobilization, cAMP accumulation) are used to assess its PAM or antagonist activity.
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| Cell Assay |
Cell proliferation analysis [1]
Cell Types: primary human lung fibroblasts (PHLFs). ) (TGF-β induction) Tested Concentrations: 50, 100 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibition of TGF-β stimulated proliferation. Cell viability assay [2] Cell Types: HEK293 cells (stably expressing HA-GPR68) Tested Concentrations: 50 μM Incubation Duration: 10 minutes Experimental Results: Activation of PKA and p42/p44 MAP kinase. RT-PCR[1] Cell Types: Primary human lung fibroblasts (PHLF) (TGF-β induced) Tested Concentrations: 50-150 μM Incubation Duration: 48 hrs (hours) Experimental Results: Inhibited TGF-β-induced Col1A1 in a dose-dependent manner and Col3A1 mRNA levels. Western Blot Analysis[1] Cell Types: Primary human lung fibroblasts (PHLF) (TGF-β induced) Tested Concentrations: 150 μM Incubation Duration: 40 minutes (pre-treatment) Experimental Results: Induced in non-fibrotic and fibrotic PHLF CREB phosphorylation. Western Blot Analysis[1] Cell Types: Primary human lung fibroblasts (PHLF) (TGF-β induced) Tested Concentrations: 50-150 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibition of TG In vitro cellular assays for Ogerin are conducted in fibroblasts from multiple organ systems. Cells are treated with the compound, and TGF-β-induced myofibroblast differentiation is assessed by measuring α-SMA expression or collagen production. Its effects on cellular signaling pathways downstream of GPR68, A2A, or 5-HT2B are measured. |
| Animal Protocol |
Animal/Disease Models: GPR68 knockout and WT mice [2].
Doses: 10 mg/kg Route of Administration: Single (30 minutes before training) Experimental Results: Recall of fear conditioning was inhibited in wild-type mice, but not in GPR68 knockout mice. In vivo animal studies for Ogerin are conducted in mouse models of fear conditioning to assess its effects on memory and learning. Its effects on fibrotic diseases are studied in models of pulmonary or hepatic fibrosis. Animals are administered the compound orally or intraperitoneally, and behavioral or histological endpoints are measured. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Ogerin indicate it has a molecular weight of 307.35 and a molecular formula of C17H17N5O. It is soluble in DMSO at 25 mg/mL. The compound is typically stored as a powder at -20°C for up to 3 years. Its bioavailability and other PK parameters would be determined in preclinical studies.
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| Toxicity/Toxicokinetics |
Toxicological information for Ogerin is limited to its use as a research chemical. As a GPCR modulator, it may have effects on various physiological processes. Comprehensive toxicology studies would be required for its use in vivo, including assessments of its effects on cardiovascular, neurological, and fibrotic pathways.
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| References | |
| Additional Infomation |
GPR68 modulator; structure in the first source
Ogerin is a research compound used as a selective GPR68 positive allosteric modulator. It is also a chemical probe for studying GPR68 biology. It inhibits fear conditioning in mice and inhibits TGF-β-induced myofibroblast differentiation. It is available from research chemical suppliers for preclinical studies. It is not approved for clinical use. |
| Molecular Formula |
C17H17N5O
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|---|---|
| Molecular Weight |
307.349782705307
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| Exact Mass |
307.143
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| CAS # |
1309198-71-7
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| PubChem CID |
56707820
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| Appearance |
White to off-white solid powder
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| LogP |
2.2
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
23
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| Complexity |
350
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1(CO)=CC=CC=C1C1=NC(N)=NC(NCC2=CC=CC=C2)=N1
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| InChi Key |
MDGIEDNDSFMSLP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H17N5O/c18-16-20-15(14-9-5-4-8-13(14)11-23)21-17(22-16)19-10-12-6-2-1-3-7-12/h1-9,23H,10-11H2,(H3,18,19,20,21,22)
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| Chemical Name |
[2-[4-amino-6-(benzylamino)-1,3,5-triazin-2-yl]phenyl]methanol
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| Synonyms |
ZINC-67740571; ZINC67740571; Ogerin
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~813.40 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.77 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.77 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.77 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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