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MK-6892

 
Catalog No.
A3623
GPR109A激动剂
组合的产品项目
规格价格库存 数量
5mg
¥ 2,536.00
现货
10mg
¥ 3,855.00
现货
50mg
¥ 9,130.00
现货
100mg
¥ 14,203.00
Ship with 10-15 days

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A

背景

Description: IC50 Value: 4.0 nM (Ki for Human GPR109A) [1] MK-6892 is a highly potential GPR109A agonists. in vitro: . Despite the increased serum shift of these compounds, the representative 1e was highly potent. Furthermore, these compounds had no activity on GPR109B and GPR81, the two most closely related GPCRs with ?96% and 50% sequence identity to GPR109A,respectively [1]. in vivo: NA or MK-6892 was orally administered to WT or NA receptor null mice on the same C57Bl/6 genetic background. After 15 min of 100 mpk dosing of NA or MK-6892 to fed WT or NA receptor null mice, the blood levels of MK-6892 at 15 min were 229 μM (?950-fold greater than the in vitro EC50 determined in mouse NA receptor GTPγS assay, which is 240 nM) in WT mice and 148 μM (?620-fold greater than the in vitro EC50) in NA receptor null mice [1]. Clinical trial: N/A

化学属性

StorageStore at -20°C
M.Wt386.4
Cas No.917910-45-3
FormulaC19H22N4O5
SynonymsMK 6892;MK6892
Solubility≥34.9 mg/mL in DMSO; ≥3.41 mg/mL in EtOH with ultrasonic; insoluble in H2O
Chemical Name2-[[2,2-dimethyl-3-[(3E)-3-(5-oxopyridin-2-ylidene)-1,2,4-oxadiazol-5-yl]propanoyl]amino]cyclohexene-1-carboxylic acid
SDFDownload SDF
Canonical SMILESCC(C)(CC1=NC(=C2C=CC(=O)C=N2)NO1)C(=O)NC3=C(CCCC3)C(=O)O
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