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

APD668 

Cat. No.: HY-15565 Purity: 99.71%
Handling Instructions

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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 158 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 158 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
10 mg USD 250 In-stock
Estimated Time of Arrival: December 31
50 mg USD 750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 950 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE APD668

  • 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].

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

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].

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.
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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (69.80 mM; Need ultrasonic)

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
10 mM 0.2094 mL 1.0471 mL 2.0942 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

  • 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

*All of the co-solvents are available by MCE.
References

Purity: 99.71%

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APD668
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