| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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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].
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|---|---|
| ln Vivo |
It has been demonstrated that agerin (10 mg/kg; single dose) supports GPR68's involvement in hippocampal-related memory [2].
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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 |
| 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. |
| References |
| Molecular Formula |
C17H17N5O
|
|---|---|
| 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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