Size | Price | Stock | Qty |
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1mg |
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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 |
Similar to glucagon-like peptide 1 (GLP-1) and its receptor, the endogenous ligand OEA signals through GPR119 by affecting intracellular calcium, cAMP, and insulin production [2].
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References |
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Exact Mass |
285.184
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CAS # |
388575-52-8
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Related CAS # |
PSN 375963 hydrochloride;1781834-82-9
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PubChem CID |
2875918
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Appearance |
White to off-white solid powder
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Density |
1.1±0.1 g/cm3
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Boiling Point |
440.1±47.0 °C at 760 mmHg
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Flash Point |
209.8±23.3 °C
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Vapour Pressure |
0.0±1.0 mmHg at 25°C
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Index of Refraction |
1.521
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LogP |
5.16
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Hydrogen Bond Donor Count |
0
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Hydrogen Bond Acceptor Count |
4
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Rotatable Bond Count |
5
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Heavy Atom Count |
21
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Complexity |
298
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Defined Atom Stereocenter Count |
0
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SMILES |
Cl.O1C(C2CCC(CCCC)CC2)=NC(C2C=CN=CC=2)=N1
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InChi Key |
OAVLEYPTWABFLF-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C17H23N3O/c1-2-3-4-13-5-7-15(8-6-13)17-19-16(20-21-17)14-9-11-18-12-10-14/h9-13,15H,2-8H2,1H3
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Chemical Name |
5-(4-butylcyclohexyl)-3-pyridin-4-yl-1,2,4-oxadiazole
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Synonyms |
PSN375963 PSN-375963 PSN 375963
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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 : ~50 mg/mL (~175.20 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (8.76 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: ≥ 2.5 mg/mL (8.76 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 25.0 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: ≥ 2.5 mg/mL (8.76 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
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.
GPR119 agonists increase insulin secretion in RIN cell lines. (a and b) The RINm5f and RIN-119 cells were stimulated by 16 mm glucose, with or without the presence of 30 nm glucagon-like peptide-1, 10 μm oleoylethanolamide, 10 μm oleoyl-lysophosphatidylcholine, 10 μm PSN375963 and PSN632408 as indicated. The insulin levels from the triplicates were measured for each treatment and data were presented as ng insulin per ml (mean±s.e.mean). *P<0.05; **P<0.01 using ANOVA-Bonferroni, compared with insulin induced by 16 mm glucose alone in the same cell line.[2]. Ning Y, et al. Endogenous and synthetic agonists of GPR119 differ in signalling pathways and their effects on insulin secretion in MIN6c4 insulinoma cells. Br J Pharmacol. 2008;155(7):1056-1065. td> |
PSN375963 and PSN632408 vary in their ability to augment glucose-stimulated insulin secretion in MIN6c4 cells. (a) MIN6c4 cells were stimulated with the indicated concentrations of PSN375963 in the presence of 2.8 mm glucose or 16 mm glucose (b) MIN6c4 cells were stimulated with the indicated concentrations of PSN632408 in the presence of 2.8 mm glucose or 16 mm glucose. For all experiments, the insulin levels were measured after 2 h incubation. Each treatment was performed in triplicate and data were presented as ng insulin per ml of culture supernatant (mean±s.e.mean). *P<0.05; using ANOVA-Bonferroni, compared with insulin induced by glucose alone.[2]. Ning Y, et al. Endogenous and synthetic agonists of GPR119 differ in signalling pathways and their effects on insulin secretion in MIN6c4 insulinoma cells. Br J Pharmacol. 2008;155(7):1056-1065. td> |
PSN375963 and PSN632408 have opposite effects on [Ca2+]i in MIN6c4 cells. MIN6c4 cells were incubated in HEPES–Krebs–Ringer bicarbonate buffer with 2.8 mm glucose for 30 min. Cells were subsequently maintained at 2.8 mm glucose or brought to 16 mm glucose followed by the addition of the indicated concentrations of PSN375963 (a and b) or PSN632408 (c and d). [Ca2+]i was continuously monitored by FLIPR.[2]. Ning Y, et al. Endogenous and synthetic agonists of GPR119 differ in signalling pathways and their effects on insulin secretion in MIN6c4 insulinoma cells. Br J Pharmacol. 2008;155(7):1056-1065. td> |