832714-46-2

中文名稱 ISOPROPYL 4-(1-(2-FLUORO-4-(METHYLSULFONYL)PHENYL)-1H-PYRAZOLO[3,4-D]PYRIMIDIN-4-YLOXY)PIPERIDINE-1-CARBOXYLATE

英文名稱 APD668

CAS 832714-46-2

分子式 C21H24FN5O5S

分子量 477.51

MOL 文件 832714-46-2.mol

更新日期 2023/03/20 15:41:25

832714-46-2 結(jié)構(gòu)式

基本信息物理化學(xué)性質(zhì) 圖譜信息 APD668價(jià)格(試劑級(jí)) 常見問題列表

基本信息

中文別名

4-(1-(2-氟-4-(甲磺?；?苯基)-1H-吡唑并[3,4-D]嘧啶-4-氧基)哌啶-1-羧酸異丙酯
異丙基 4-(1-(2-氟-4-(甲基磺酰基)苯基)-1H-吡唑并[3,4-D]嘧啶-4-基氧基)哌啶-1-羧酸

英文別名

APD668
CS-1179
APD 668, >=98%
APD 668
APD-668
4-[[1-(2-Fluoro-4-methylsulfonylphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylic acid isopropyl ester
1-Piperidinecarboxylic acid,4-[[1-[2-fluoro-4-(methylsulfonyl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-4-yl]oxy]-, 1-methylethyl ester
isopropyl 4-((1-(2-fluoro-4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl)oxy)piperidine-1-carboxylate APD668
APD668 ISOPROPYL 4-(1-(2-FLUORO-4-(METHYLSULFONYL)PHENYL)-1H-PYRAZOLO[3,4-D]PYRIMIDIN-4-YLOXY)PIPERIDINE-1-CARBOXYLATE

所屬類別

生物化工：激動(dòng)劑抑制劑

物理化學(xué)性質(zhì)

沸點(diǎn)611.6±55.0 °C(Predicted)

密度1.47±0.1 g/cm3(Predicted)

儲(chǔ)存條件-20°C儲(chǔ)存

溶解度insoluble in H2O; ≥17.4 mg/mL in DMSO; ≥2.61 mg/mL in EtOH with gentle warming and ultrasonic

酸度系數(shù)(pKa)2.13±0.30(Predicted)

形態(tài)固體

顏色White to off-white

圖譜信息

APD668(832714-46-2)核磁圖(¹HNMR)

APD668價(jià)格(試劑級(jí))

報(bào)價(jià)日期	產(chǎn)品編號(hào)	產(chǎn)品名稱	CAS號(hào)	包裝	價(jià)格
2026/03/03	S6746	APD668 APD668	832714-46-2	5mg	1870.82元
2025/12/22	HY-15565	APD668	832714-46-2	1 mg	623元
2025/12/22	HY-15565	APD668 APD668	832714-46-2	5 mg	1300元

常見問題列表

生物活性

APD668是有效的GPR119激動(dòng)劑，對(duì)人源GPR119和大鼠GPR119的EC50值分別為2.7 nM和33 nM。

靶點(diǎn)

Target	Value
human GPR119 ()	2.7 nM(EC50)
rat GPR119 ()	33 nM(EC50)

體外研究

APD668 increases adenylate cyclase activation in HEK293 cells transfected with human GPR119 in a concentration-dependent manner with an EC ₅₀ of 23 nM.
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.

體內(nèi)研究

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.
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.
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.
APD668 (p.o.) exhibits rapid to moderate absorption (t _max ≤2 h) in mice, rats, and monkeys, but slower in dogs (t _max =6 h), and moderate to good absolute oral bioavailability (44-79%) in mice, rats, and monkeys, but lower in dogs (22%).