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YM-254890, a macrocyclohexapeptide isolated from Chromobacterium sp, is a selective and potent inhibitor of Gαq/11 protein, inhibits ADP-induced platelet aggregation and inhibits G protein signaling.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $1,107 | 35 days | 35 days |
| Description | YM-254890, a macrocyclohexapeptide isolated from Chromobacterium sp, is a selective and potent inhibitor of Gαq/11 protein, inhibits ADP-induced platelet aggregation and inhibits G protein signaling. |
| Targets&IC50 | HL-60 cells:> 10 μM, P2Y2-C6-15 cells:0.15 μM |
| In vitro | METHODS: The effects of YM-254890 on P2Y1 and P2Y12 signaling pathways were examined using C6-15 cells stably expressing human P2Y1 or P2Y12 receptors. RESULTS: 2MeSADP stimulation of P2Y1-C6-15 cells resulted in increased intracellular calcium mobilization. In this assay, YM-254890 inhibited the increase in [Ca2+]i (IC50: 0.031 μM). However, 40 μM of YM-254890 did not affect the 2MeSADP-induced inhibition of forskolin-stimulated adenylate cyclase activity in P2Y12-C6-15 cells [1]. |
| Synonyms | YM254890, YM 254890 |
| Molecular Weight | 960.08 |
| Formula | C46H69N7O15 |
| Cas No. | 568580-02-9 |
| Smiles | CO[C@H](C)[C@@H]1N(C)C(=O)[C@@H](NC(=O)[C@H](C)N(C)C(=O)[C@H](C)NC(=O)C(=C)N(C)C(=O)[C@@H](Cc2ccccc2)OC(=O)[C@@H](NC(C)=O)[C@@H](C)OC1=O)[C@H](OC(=O)[C@@H](NC(C)=O)[C@H](O)C(C)C)C(C)C |
| Relative Density. | 1.26 g/cm3 (Predicted) |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 30 mg/mL (31.25 mM), Sonication is recommended. | |||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 1.5 mg/mL (1.56 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
| ||||||||||||||||||||||||||
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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