[CAS NO. 832714-46-2] APD668

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PRODUCTS SPECIFICATIONS [832714-46-2]

Catalog

SLK-S6746

Brand

Selleck

CAS

832714-46-2

DESCRIPTION [832714-46-2]

Overview

MDL	MFCD12032117
Molecular Weight	477.51
Molecular Formula	C21H24FN5O5S
SMILES	O=C(N1CCC(OC2=C3C(N(C4=CC=C(S(=O)(C)=O)C=C4F)N=C3)=NC=N2)CC1)OC(C)C

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Description

APD668 (JNJ28630368) is a potent 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

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.

References

[1] Semple G, et al. Bioorg Med Chem Lett. 2011, 21(10):3134-41.