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DC260126

Alias: DC 260126; DC-260126; DC260126
Cat No.:V30807 Purity: ≥98%
DC260126 is a potent GPR40 (FFAR1) antagonist.
DC260126
DC260126 Chemical Structure CAS No.: 346692-04-4
Product category: GPR
This product is for research use only, not for human use. We do not sell to patients.
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Product Description
DC260126 is a potent GPR40 (FFAR1) antagonist. DC260126 concentration-dependently inhibits GPR40-mediated Ca2+ elevation stimulated by linoleic acid, oleic acid, palmitoleic acid and lauric acid (IC50 6.28, 5.96, 7.07, 4.58 μM, respectively). DC260126 has a protective effect against palmitate-induced endoplasmic reticulum stress and apoptosis.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
DC260126 suppresses palmitic acid potentiated glucose-stimulated insulin secretion, decreases GTP-loading and ERK1/2 phosphorylation stimulated by linoleic acid in GPR40-CHO cells, and negatively regulates GPR40 mRNA expression induced by oleic acid in Min6 cells[1].
Animal Protocol
Mice: Male C57BL/KsJ-Lepdb (db/db) animals are kept in a 12-hour light-dark cycle at 23°C with free access to water and a regular diet of chow. Nine-week-old male db/db mice are split into four groups (n=6) to examine the dose-dependent effect of DC260126. Using a tail vein injection, mice are given either DC260126 (3, 10, 30 mg/kg) or vehicle (5% DMSO in PBS) once a day for five days. On day five, all mouse groups undergo a 6-hour fast, after which blood samples are taken from the orbital venous plexus and separated by centrifugation to extract serum. Next, an ELISA kit is used to measure the serum insulin concentration. In these long-term studies, eighteen six-week-old male, obese db/db mice are placed into two groups and given either DC260126 (10 mg/kg) or vehicle (5% DMSO in PBS) once a day by tail vein injection for 24 days.
Rats: Zucker rats that are obese and female (fa/fa) are kept in a 12:12 light-dark cycle, given free access to water, and fed a high-fat diet consisting of 15% fat, 1% cholesterol, 0.5% sodium cholate, and 15% sucrose, with the exception of times when they are fasted prior to certain experiments. Based on body weight, two groups of six rats each are created at eight weeks of age. During eight weeks, rats receive intraperitoneal injections of DC260126 (6 mg/kg) or vehicle (propylene glycol) once a day. Periodically, food consumption and body weight are assessed. Following a 12-hour fast at the conclusion of the experiment, blood is drawn from the mice. Adipose, renal, and liver tissues are quickly removed and weighed. For western blotting analysis, liver samples are kept at -80°C after being snap frozen in liquid nitrogen.
References

[1]. A novel class of antagonists for the FFAs receptor GPR40. Biochem Biophys Res Commun. 2009;390(3):557-563.

[2]. Inhibition of GPR40 protects MIN6 β cells from palmitate-induced ER stress and apoptosis [published correction appears in J Cell Biochem. 2013 May;114(5):1216]. J Cell Biochem. 2012;113(4):1152-1158.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C₁₆H₁₈FNO₂S
Molecular Weight
307.3834
Exact Mass
307.104
Elemental Analysis
C, 62.52 H, 5.90 F, 6.18 N, 4.56 O, 10.41 S, 10.43
CAS #
346692-04-4
PubChem CID
2843133
Appearance
White to off-white solid powder
Density
1.2±0.1 g/cm3
Boiling Point
423.6±55.0 °C at 760 mmHg
Flash Point
210.0±31.5 °C
Vapour Pressure
0.0±1.0 mmHg at 25°C
Index of Refraction
1.579
LogP
4.95
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
4
Rotatable Bond Count
6
Heavy Atom Count
21
Complexity
391
Defined Atom Stereocenter Count
0
SMILES
O=S(C1=CC=C(F)C=C1)(NC2=CC=C(CCCC)C=C2)=O
InChi Key
CNGHPXKWPGIDSK-UHFFFAOYSA-N
InChi Code
InChI=1S/C16H18FNO2S/c1-2-3-4-13-5-9-15(10-6-13)18-21(19,20)16-11-7-14(17)8-12-16/h5-12,18H,2-4H2,1H3
Chemical Name
N-(4-butylphenyl)-4-fluorobenzenesulfonamide
Synonyms
DC 260126; DC-260126; DC260126
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: ~61 mg/mL (~198.5 mM)
Ethanol: ~61 mg/mL
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.13 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 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 (8.13 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 (8.13 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.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.2533 mL 16.2665 mL 32.5330 mL
5 mM 0.6507 mL 3.2533 mL 6.5066 mL
10 mM 0.3253 mL 1.6267 mL 3.2533 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.

Calculator

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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?
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  • 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:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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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.

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