化学性质
| Storage | Store at -20°C |
| M.Wt | 386.4 |
| Cas No. | 917910-45-3 |
| Formula | C19H22N4O5 |
| Synonyms | MK 6892;MK6892 |
| Solubility | ≥34.9 mg/mL in DMSO; ≥3.41 mg/mL in EtOH with ultrasonic; insoluble in H2O |
| Chemical Name | 2-[[2,2-dimethyl-3-[(3E)-3-(5-oxopyridin-2-ylidene)-1,2,4-oxadiazol-5-yl]propanoyl]amino]cyclohexene-1-carboxylic acid |
| Canonical SMILES | CC(C)(CC1=NC(=C2C=CC(=O)C=N2)NO1)C(=O)NC3=C(CCCC3)C(=O)O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
资料参考
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
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