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Cat. Number

YM-254890

Chemical Name

YM-254890

CAS Number

568580-02-9

Qty 1

1mg

Application Notes

≥95.0%

References

YM-254890 是一种从 Chromobacterium sp 中分离的选择性 G_αq/11 蛋白抑制剂。YM-254890 对其他 G 蛋白亚型无抑制作用。YM-254890 通过阻断 P2Y₁ 信号转导途径来抑制 ADP 诱导的血小板凝集，其 IC₅₀ 值低于 0.6 μM。

生物活性

YM-254890 is a selective G_αq/11 protein inhibitor isolated from Chromobacterium sp. YM-254890 shows no inhibition of other G protein subtypes. YM-254890 inhibits platelet aggregation induced by ADP by blocking the P2Y₁ signal transduction pathway, with an IC₅₀ value below 0.6 μM^[1]^[2].

IC₅₀ & Target

P2Y1 Receptor

体外研究
(In Vitro)

YM-254890 inhibits platelet aggregation induced by ADP (2, 5 and 20 μM) in human platelet-rich plasma with IC₅₀ values of 0.37, 0.39 and 0.51 μM. ADP mediates platelet aggregation via two G protein-coupled receptors, P2Y₁ and P2Y₁₂. The effect of YM-254890 on the P2Y₁ and P2Y₁₂ signal transduction pathways using C6-15 cells stably expressing the human P2Y₁ or P2Y₁₂ receptors is examined. Stimulation of P2Y₁-C6-15 cells by 2MeSADP leads to increases in intracellular calcium mobilization. In this assay, YM-254890 inhibits the increase in [Ca²⁺]_i with an IC₅₀ value of 0.031 μM. In contrast, 2MeSADP-induced inhibition of forskolin-stimulated adenylyl cyclase activity in P2Y₁₂-C6-15 cells is unaffected by YM-254890 at 40 μM^[1].

They are for reference only.

分子量	960.08
性状	固体
Formula	C₄₆H₆₉N₇O₁₅
CAS 号	568580-02-9
结构分类	Others
初始来源	the culture broth of Chromobacterium sp
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder-20°C3 yearsIn solvent-80°C6 months-20°C1 month

参考文献:

[1]. Taniguchi M, et al. YM-254890, a novel platelet aggregation inhibitor produced by Chromobacterium sp. QS3666. J Antibiot (Tokyo). 2003 Apr;56(4):358-63.
[2]. Zhang H, et al. Structure-activity relationship and conformational studies of the natural product cyclic depsipeptides YM-254890 and FR900359. Eur J Med Chem. 2018 Aug 5;156:847-860.

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