APD668

Name: APD668
Brand: TargetMol
SKU: T2088
Price: 498 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.97%

货号 T2088Cas号 832714-46-2

别名 APD 668

APD668 是选择性的，口服有效的GPR119激动剂，对hGPR119和rGPR119的EC50分别为 2.7 nM 和 33 nM。它对除CYP2C9(Ki=0.1 μM) 以外的五种主要 CYP 亚型均无明显抑制作用。它可用于脂肪性肝炎和糖尿病的研究。

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APD668

一键复制产品信息

很棒

纯度: 99.97%

货号 T2088 别名 APD 668Cas号 832714-46-2

规格	价格	库存
1 mg	¥ 498	现货
5 mg	¥ 1,070	现货
10 mg	¥ 1,650	现货
25 mg	¥ 3,150	现货
50 mg	¥ 4,890	现货
100 mg	¥ 6,780	现货
1 mL x 10 mM (in DMSO)	¥ 1,130	现货

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产品介绍

APD668 AI Summary

APD668 exhibits a range of bioactivities including notable pharmacological and biochemical properties. It demonstrates potent inhibition of CYP2C9 with a Ki value of 100.0 nM and exhibits agonist activity at human and rat GPR119, with EC50 values of 2.7 nM and 33.0 nM, respectively. In ZDF rat models, it shows antidiabetic activity by reducing glycated hemoglobin and blood glucose levels. The compound has favorable oral bioavailability and a selectivity ratio of EC50, indicating selective activity on GPR119. Pharmacokinetic studies reveal varying clearance rates across animal models: 3.833 mL.min-1.kg-1 in Swiss albino mice, 20.0 mL.min-1.kg-1 in Sprague-Dawley rats, 7.333 mL.min-1.kg-1 in Zucker fa/fa rats, 2.0 mL.min-1.kg-1 in Beagle dogs, and 1.833 mL.min-1.kg-1 in Cynomolgus monkeys, which suggests species-specific metabolic behaviors. The LogD7.4 value of 3.0 indicates high lipophilicity and potential for membrane permeability, and the moderate solubility in pH 7.4 buffer (2100.0 nM) may influence its formulation and bioavailability. APD668 has demonstrated antiviral properties, inhibiting the cytotoxicity induced by SARS-CoV-2 in Caco-2 cells at 10 µM with a 24.13% inhibition rate and showing SARS-CoV-2 3CL-Pro protease inhibition at 20 µM concentrations (8.79% and 22.19% inhibition). It also inhibits SARS-CoV-2-induced cytotoxicity in VERO-6 cells at the same concentration. Additionally, APD668 exhibits inhibitory activity in human HDAC6 enzymatic assays, stronger with commercial peptide substrates (22.09%) than with custom ones (2.8%). It affects cell growth variably, inhibiting U2OS cell growth while promoting viability in human fibroblast and HEK293T cells. Thermal Shift Assays indicate it impacts thermal stability across different protein domains, suggesting interactions with protein stability. In GPCR beta-arrestin recruitment assays, APD668 displays both agonistic and inhibitory effects on various receptors, indicating multifunctional GPCR activity. This versatility highlights its potential as a compound with diverse therapeutic applications..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	APD668 is a potent GPR119 agonist with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119, respectively.
靶点活性	CYP2C9:0.1 μM (Ki), GPR119 (rat):33 nM (EC50), GPR119 (human):2.7 nM (EC50), ERG channel (human):3 μM
别名	APD 668

化学信息

分子量	477.51
分子式	C₂₁H₂₄FN₅O₅S
CAS No.	832714-46-2
Smiles	CC(C)OC(=O)N1CCC(CC1)Oc1ncnc2n(ncc12)-c1ccc(cc1F)S(C)(=O)=O
密度	1.47 g/cm3 (Predicted)
颜色	White
物理性状	Solid

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 45 mg/mL (94.24 mM), Sonication is recommended.

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0942 mL	10.4710 mL	20.9420 mL	104.7098 mL
5 mM	0.4188 mL	2.0942 mL	4.1884 mL	20.9420 mL
10 mM	0.2094 mL	1.0471 mL	2.0942 mL	10.4710 mL
20 mM	0.1047 mL	0.5235 mL	1.0471 mL	5.2355 mL
50 mM	0.0419 mL	0.2094 mL	0.4188 mL	2.0942 mL