LY83583
| 规格 | 价格 | 货期 | 数量 |
|---|---|---|---|
| 5mg | ¥1383.00 | 10-15工作日发货 | |
| 10mg | ¥2045.00 | 10-15工作日发货 | |
| 50mg | ¥5235.00 | 10-15工作日发货 |
特色产品
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
产品描述
LY83583 is an inhibitor of soluble guanylate cyclase and of cGMP production [1].
Soluble Guanylate cyclase (sGC) is a heterodimeric enzyme involved in converting guanosine triphosphate to cyclic guanosine monophosphate. Soluble Guanylate cyclase is a critical component of the NO/cGMP signaling pathway, which has been involved in a number of important physiological processes, including smooth muscle relaxation and neurotransmission [2].
In human platelets, LY 83583 significantly antagonized the inhibitory effect of sodium nitroprusside and EDRF. LY 83583 attenuated the increases in intracellular cyclic GMP by sodium nitroprusside and EDRF [1]. Low concentrations of LY 83583 (≤ 0.1 μM) inhibited endothelium-dependent relaxations of rabbit aortic strips induced by acetylcholine or by the calcium ionophore A23187. Higher concentrations (≥ 0.3 μM) produced partial inhibition of relaxation to sodium nitroprusside and glyceryl trinitrate. LY 83583 (10 μM) showed no effect on cyclic AMP-mediated relaxations induced by isoprenaline or forskolin [3]. In cultured endothelial cells, treatment with LY 83583 (1 μM) rapidly and reversibly inhibited EDRF release. In the rat gastric fundus, LY 83583 (10 μM) inhibited the relaxation induced by nitric oxide (NO) [4]. In activated human neutrophils, LY-83583 (100 μM) inhibited the release of both LF and MPO after stimulation with FMLP or A-23187. LY-83583 reduced the cGMP-dependent protein kinase (G-kinase) activity [5].
References:
[1] Mülsch A, Lückhoff A, Pohl U, et al. LY 83583 (6-anilino-5, 8-quinolinedione) blocks nitrovasodilator-induced cyclic GMP increases and inhibition of platelet activation[J]. Naunyn-Schmiedeberg's archives of pharmacology, 1989, 340(1): 119-125.
[2] Denninger J W, Marletta M A. Guanylate cyclase and the NO/cGMP signaling pathway[J]. Biochimica et Biophysica Acta (BBA)-Bioenergetics, 1999, 1411(2): 334-350.
[3] Mülsch A, Busse R, Liebau S, et al. LY 83583 interferes with the release of endothelium-derived relaxing factor and inhibits soluble guanylate cyclase[J]. Journal of Pharmacology and Experimental Therapeutics, 1988, 247(1): 283-288.
[4] Barbier A J M, Lefebvre R A. Effect of LY 83583 on relaxation induced by non-adrenergic non-cholinergic nerve stimulation and exogenous nitric oxide in the rat gastric fundus[J]. European journal of pharmacology, 1992, 219(2): 331-334.
[5] Wyatt T A, Lincoln T M, Pryzwansky K B. Regulation of human neutrophil degranulation by LY-83583 and L-arginine: role of cGMP-dependent protein kinase[J]. American Journal of Physiology-Cell Physiology, 1993, 265(1): C201-C211.
产品性质
| 物理外观 | A crystalline solid |
| CAS号 | 91300-60-6 |
| 分子式 | C15H10N2O2 |
| 分子量 | 250.3 |
| 化学名称 | 6-(phenylamino)-5,8-quinolinedione |
| 溶解度 | ≤3.8mg/ml in ethanol;25mg/ml in DMSO;25mg/ml in dimethyl formamide |
| SMILES | O=C(C=C1Nc2ccccc2)c(nccc2)c2C1=O |
| 存储条件 | -20°C |
| 运输条件 | 蓝冰 |
产品应用 (实验数据来自文献,APExBIO并未验证,仅供参考)
IC50和靶点
| 生物活性描述 | LY83583 是一种具有细胞渗透性的可溶性鸟苷酸环化酶(sGC)竞争性抑制剂,其 IC50 值为 2 μM。 |



沪公网安备 31011002003500