2. GPCR/G Protein Neuronal Signaling Metabolic Enzyme/Protease Membrane Transporter/Ion Channel
  3. GPR119 Cytochrome P450 Potassium Channel
  4. APD668

APD668 is a potent, selective and orally active agonist of G-protein coupled receptor GPR119, with EC50s of 2.7 nM and 33 nM for hGPR119 and rGPR119, respectively. APD668 shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (Ki=0.1 μM). APD668 can be used for the research of steatohepatitis and diabetes.

For research use only. We do not sell to patients.

APD668 Chemical Structure

APD668 Chemical Structure

CAS No. : 832714-46-2

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10 mM * 1 mL in DMSO
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Customer Review

Based on 2 publication(s) in Google Scholar

APD668 Related Antibodies

Top Publications Citing Use of Products

View All Cytochrome P450 Isoform Specific Products:

View All Isoforms
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

APD668 is a potent, selective and orally active agonist of G-protein coupled receptor GPR119, with EC50s of 2.7 nM and 33 nM for hGPR119 and rGPR119, respectively. APD668 shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (Ki=0.1 μM). APD668 can be used for the research of steatohepatitis and diabetes[1][2].

IC50 & Target[1]

hGPR119

2.7 nM (IC50)

rGPR119

33 nM (IC50)

CYP2C9

0.1 μM (Ki)

hERG channel

3 μM (IC50)

In Vitro

APD668 increases adenylate cyclase activation in HEK293 cells transfected with human GPR119 in a concentration-dependent manner with an EC50 of 23 nM[1].
APD668 is highly bound to plasma proteins of male and female cynomolgus monkeys and humans (⩾99%), but is less extensively bound to male (93.0%) and female (96.6%) rats[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

APD668 Related Antibodies
In Vivo

APD668 (10-30 mg/kg; p.o. once daily for 8 weeks) significantly reduces blood glucose and glycated hemoglobin (HbA1c) levels, with no desensitization of the acute drug response[1].
APD668 (1-10 mg/kg; a single p.o.) markedly reduces blood glucose levels during oral glucose tolerance test in a dose-dependent manner in mice[1].
APD668 (0.08 mg/kg/min; i.v.) shows no effect during euglycemic condition, but significantly stimulates insulin release when blood glucose levels are raised to approximately 300 mg/dl in a hyperglycemic clamp model in the Sprague-Dawley rat[1].
APD668 (p.o.) exhibits rapid to moderate absorption (tmax≤2 h) in mice, rats, and monkeys, but slower in dogs (tmax=6 h), and moderate to good absolute oral bioavailability (44-79%) in mice, rats, and monkeys, but lower in dogs (22%)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Zucker Diabetic Fatty (ZDF) rats (6 weeks old, 200-250 g)[1]
Dosage: 10, 30 mg/kg
Administration: P.o. once daily for 8 weeks
Result: Decreased the blood glucose and HbA1c levels at 30 mg/kg/day.
Did not develop diabetes, whereas the vehicle treated rats did.
Molecular Weight

477.51

Formula

C21H24FN5O5S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(OC(C)C)N(CC1)CCC1OC2=C3C(N(C4=CC=C(S(=O)(C)=O)C=C4F)N=C3)=NC=N2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (69.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0942 mL 10.4710 mL 20.9420 mL
5 mM 0.4188 mL 2.0942 mL 4.1884 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (4.36 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.10%

SDS (393 KB)

COA (249 KB) LCMS (269 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0942 mL 10.4710 mL 20.9420 mL 52.3549 mL
5 mM 0.4188 mL 2.0942 mL 4.1884 mL 10.4710 mL
10 mM 0.2094 mL 1.0471 mL 2.0942 mL 5.2355 mL
15 mM 0.1396 mL 0.6981 mL 1.3961 mL 3.4903 mL
20 mM 0.1047 mL 0.5235 mL 1.0471 mL 2.6177 mL
25 mM 0.0838 mL 0.4188 mL 0.8377 mL 2.0942 mL
30 mM 0.0698 mL 0.3490 mL 0.6981 mL 1.7452 mL
40 mM 0.0524 mL 0.2618 mL 0.5235 mL 1.3089 mL
50 mM 0.0419 mL 0.2094 mL 0.4188 mL 1.0471 mL
60 mM 0.0349 mL 0.1745 mL 0.3490 mL 0.8726 mL
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APD668 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

APD668832714-46-2APD 668APD-668GPR119Cytochrome P450Potassium ChannelG Protein-Coupled Receptor 119CYPsKcsAG-proteincoupledCYP2C9steatohepatitisdiabetesInhibitorinhibitorinhibit

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