[CAS NO. 897732-93-3] APD597
PRODUCTS SPECIFICATIONS [897732-93-3]
DESCRIPTION [897732-93-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 479.55 |
| Molecular Formula | C21H29N5O6S |
| SMILES | O=C(OC(C)C)N(CC1)CCC1OC2=C(OC)C(NC3=CC=C(S(=O)(C)=O)N=C3C)=NC=N2 |
1 Publications Citing Use of MCE
Summary
APD597 is a GPR119 agonist intended for the treatment of type 2 diabetes, with EC50 of 46 nM for hGPR119. IC50 value: 46 nM (EC50) [1] Target: hGPR119 The design and synthesis of a second generation GPR119-agonist clinical candidate for the treatment of diabetes is described. APD597 was selected for preclinical development based on a good balance between agonist potency, intrinsic activity and in particular on its good solubility and reduced drug-drug interaction potential. [1]
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00910923 | Johnson & Johnson Pharmaceutical Research & Development, L.L.C. |
Diabetes Mellitus, Type 2
|
November 2008 | Phase 1 |
| NCT01054118 | Johnson & Johnson Pharmaceutical Research & Development, L.L.C. |
Diabetes Mellitus, Type 2
|
December 2009 | Phase 1 |
| NCT00871507 | Johnson & Johnson Pharmaceutical Research & Development, L.L.C. |
Diabetes Mellitus, Type 2
|
April 2009 | Phase 1 |
Appearance
Solid
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
DMSO : 100 mg/mL ( 208.53 mM ; Need ultrasonic)
H 2 O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.0853 mL | 10.4264 mL | 20.8529 mL |
| 5 mM | 0.4171 mL | 2.0853 mL | 4.1706 mL |
| 10 mM | 0.2085 mL | 1.0426 mL | 2.0853 mL |
References
- [1] Buzard DJ, et al. Discovery and optimization of 5-fluoro-4,6-dialkoxypyrimidine GPR119 agonists. Bioorg Med Chem Lett. 2014 Sep 1;24(17):4332-4335.
- [2] Huan Y, et al. The dual DPP4 inhibitor and GPR119 agonist HBK001 regulates glycemic control and beta cell function ex and in vivo. Sci Rep. 2017 Jun 28;7(1):4351.
- [3] Semple G, et al. Discovery of a second generation agonist of the orphan G-protein coupled receptor GPR119 with an improvedprofile. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1750-1755.