APD668

Catalog No.S6746 Batch:S674601

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Technical Data

Formula

C21H24FN5O5S
Molecular Weight 477.51 CAS No. 832714-46-2
Solubility (25°C)* In vitro DMSO 96 mg/mL (201.04 mM)
Ethanol 2 mg/mL (4.18 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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

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

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].

Protocol (from reference)

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.