Home Endocrinology & Hormones GPR agonist APD668 For research use only.

APD668

Synonyms: JNJ28630368

APD668 (JNJ28630368) is a potent GPR119 agonist with EC50s of 2.7 and 33 nM for human and rat forms, respectively.

APD668 Chemical Structure

APD668 Chemical Structure

CAS: 832714-46-2

Purity & Quality Control

Batch: S674601 DMSO] 96 mg/mL] false] Ethanol] 2 mg/mL] false] Water] Insoluble] false Purity: 99.39%
99.39

Other GPR Products

Related compound libraries

Choose Selective GPR Inhibitors

Biological Activity

Description APD668 (JNJ28630368) is a potent GPR119 agonist with EC50s of 2.7 and 33 nM for human and rat forms, respectively.
Targets
human GPR119 [1] rat GPR119 [1]
2.7 nM(EC50) 33 nM(EC50)
In vitro
In vitro

APD668 is shown to increase adenylate cyclase activation in HEK293 cells transfected with human GPR119 (but not in non-transfected cells) in a concentration-dependent manner with an EC50 of 23 nM. APD668 also enhanced insulin release from both rat and human isolated pancreatic islets in a glucose-dependent manner. In a standard panel of around 80 known receptors and ion channels, APD668 did not show any binding in excess of 50% of control to any other proteins at concentrations up to 10 μM[1].
In Vivo
In vivo

Chronic treatment with APD668 showed that blood glucose and glycated hemoglobin (HbA1c) levels could be significantly reduced in Zucker Diabetic Fatty (ZDF) rats over several weeks of dosing. APD668 is highly bound to plasma proteins of male and female cynomolgus monkeys and humans (P99%), but was less extensively bound to male (93.0%) and female (96.6%) rats. In pharmacokinetic assessments across multiple species using single oral doses of APD668, absorption was rapid to moderate (Tmax 62 h) in mice, Sprague-Dawley (SD) rats, and monkeys, but slower in dogs (Tmax = 6 h) and showed a dose-dependent increase in rats and monkeys. In general, exposure was dose-dependent at lower doses and appeared to plateau at doses greater than 300 mg/kg. Exposure was greater in female rats compared with males. Absolute oral bioavailability was moderate to good in mice, rats, and monkeys (44–79%), but was lower in dogs (22%). The volume of distribution (Vdss) values were somewhat variable ranging from 0.1 L/kg in monkey to 2.6 L/kg in rats. Elimination, based on mean T1/2 after intravenous (iv) dosing, was rapid to moderate in mice, rats, dogs, and monkeys (0.8-3.9 h). The pharmacokinetic profile of APD668 in Zucker fa/fa rats was somewhat different from that in SD rats. After oral administration, the tmax and T1/2 were longer, and the AUC and the oral bioavailability were greater in the Zucker compared with the SD rats. Following iv administration, the Zucker rats also had larger AUC values, longer T1/2 values and greater Vdss values[1].

Chemical lnformation & Solubility

Molecular Weight 477.51 Formula

C21H24FN5O5S
CAS No. 832714-46-2 SDF --
Smiles CC(C)OC(=O)N1CCC(CC1)OC2=NC=NC3=C2C=NN3C4=C(C=C(C=C4)S(=O)(=O)C)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 96 mg/mL ( (201.04 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy APD668 | APD668 supplier | purchase APD668 | APD668 cost | APD668 manufacturer | order APD668 | APD668 distributor