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PSN375963

Alias: PSN375963 PSN-375963 PSN 375963
Cat No.:V6451 Purity: ≥98%
PSN 375963 is a potent GPR119 agonist with EC50 of 8.4 and 7.9 μM in humans and mice, respectively.
PSN375963
PSN375963 Chemical Structure CAS No.: 388575-52-8
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
50mg
100mg
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Other Forms of PSN375963:

  • PSN 375963 hydrochloride
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
PSN 375963 is a potent GPR119 agonist with EC50 of 8.4 and 7.9 μM in humans and mice, respectively. PSN 375963 displays similar potency to endogenous oleoylethanolamide (OEA).
Biological Activity I Assay Protocols (From Reference)
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Exact Mass
285.184
CAS #
388575-52-8
Related CAS #
PSN 375963 hydrochloride;1781834-82-9
PubChem CID
2875918
Appearance
White to off-white solid powder
Density
1.1±0.1 g/cm3
Boiling Point
440.1±47.0 °C at 760 mmHg
Flash Point
209.8±23.3 °C
Vapour Pressure
0.0±1.0 mmHg at 25°C
Index of Refraction
1.521
LogP
5.16
Hydrogen Bond Donor Count
0
Hydrogen Bond Acceptor Count
4
Rotatable Bond Count
5
Heavy Atom Count
21
Complexity
298
Defined Atom Stereocenter Count
0
SMILES
Cl.O1C(C2CCC(CCCC)CC2)=NC(C2C=CN=CC=2)=N1
InChi Key
OAVLEYPTWABFLF-UHFFFAOYSA-N
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
Chemical Name
5-(4-butylcyclohexyl)-3-pyridin-4-yl-1,2,4-oxadiazole
Synonyms
PSN375963 PSN-375963 PSN 375963
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO : ~50 mg/mL (~175.20 mM)
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.

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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.
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 corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

Biological Data
  • 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.
  • 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.
  • 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.
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