LY83583
(Synonyms: 6-苯胺基-5,8-喹啉二酮) 目录号 : GC13857A soluble guanylate cyclase inhibitor
Cas No.:91300-60-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
| Cas No. | 91300-60-6 | SDF | |
| 别名 | 6-苯胺基-5,8-喹啉二酮 | ||
| 化学名 | 6-(phenylamino)-5,8-quinolinedione | ||
| Canonical SMILES | O=C1C=C(Nc2ccccc2)C(=O)c2cccnc12 | ||
| 分子式 | C15H10N2O2 | 分子量 | 250.3 |
| 溶解度 | 25mg/ml in DMSO;25mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.9952 mL | 19.976 mL | 39.9521 mL |
| 5 mM | 0.799 mL | 3.9952 mL | 7.9904 mL |
| 10 mM | 0.3995 mL | 1.9976 mL | 3.9952 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。