LDC7559
目录号 : GC65393
LDC7559是一种新型Gasdermin D（GSDMD）选择性抑制剂。
Cas No.:2407782-01-6
Sample solution is provided at 25 µL, 10mM.
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LDC7559 is a novel selective inhibitor of Gasdermin D (GSDMD)[1]. GSDMD is a pore-forming protein and an executor of pyroptosis[2]. LDC7559 can antagonize the depressive effects of acrylamide (AM) and improve chronic unpredictable mild stress (CUMS) depression in mice[3].
In vitro, pretreatment of A549 cells with LDC7559 (5μM) for 6h significantly reduced the release of intracellular lactate dehydrogenase (LDH) after irradiation and increased cell survival[4]. LDC7559 (10μM) treatment of mouse melanoma B16 cells for 24h significantly inhibited VSV-CHIKV (an oncolytic virus)-induced pyroptosis, reduced the protein level of GSDMD-N (the active form of the pyroptosis executor protein), and inhibited cell membrane rupture[5].
In vivo, LDC7559 (10, 20, 30mg/kg) was intraperitoneally injected into rats with subarachnoid hemorrhage (SAH) model, which alleviated the neurological deficits after SAH, inhibited microglial activation and inflammatory response, and suppressed neuronal pyroptosis and apoptosis as well as GSDMD-mediated signal transduction[6].
References:
[1] Sollberger G, Choidas A, Burn G L, et al. Gasdermin D plays a vital role in the generation of neutrophil extracellular traps[J]. Science immunology, 2018, 3(26): eaar6689.
[2] Pandeya A, Li L, Li Z, et al. Gasdermin D (GSDMD) as a new target for the treatment of infection[J]. Medchemcomm, 2019, 10(5): 660-667.
[3] Liu J F, Han C, Shen J, et al. Acrylamide exposure promotes the progression of depression-like behavior in mice with CUMS via GSDMD-mediated pyroptosis[J]. Ecotoxicology and Environmental Safety, 2025, 289: 117443.
[4] Zhang J, Jiang Z, Liu X, et al. Regulator of G protein signaling 20 contributes to radioresistance of non-small cell lung cancer cells by suppressing pyroptosis[J]. Radiation Medicine and Protection, 2024, 5(3): 178-184.
[5] Wu F, Zhan Y, Wang S, et al. VSV-CHIKV activates antitumor immunity by inducing pyroptosis in a melanoma model[J]. Discover Oncology, 2025, 16(1): 1-15.
[6] Cai W, Wu Z, Lai J, et al. LDC7559 inhibits microglial activation and GSDMD-dependent pyroptosis after subarachnoid hemorrhage[J]. Frontiers in Immunology, 2023, 14: 1117310.
LDC7559是一种新型Gasdermin D（GSDMD）选择性抑制剂[1]。GSDMD是一种成孔蛋白，也是细胞焦亡的执行者[2]。LDC7559能够拮抗丙烯酰胺（AM）的促抑郁症作用并改善小鼠慢性不可预测轻度应激（CUMS）抑郁[3]。
在体外，LDC7559（5μM）预处理A549细胞6h，显著降低了辐照处理后细胞内乳酸脱氢酶（LDH）的释放，提高了细胞的存活率[4]。LDC7559（10μM）处理小鼠黑色素瘤B16细胞24h，显著抑制了VSV-CHIKV（一种溶瘤病毒）诱导的细胞焦亡，减少了GSDMD-N（焦亡执行蛋白的活性形式）的蛋白水平，抑制了细胞膜破裂[5]。
在体内，LDC7559（10, 20, 30mg/kg）通过腹腔注射治疗蛛网膜下腔出血（SAH）模型大鼠，缓解了SAH后大鼠的神经功能缺损，抑制了小胶质细胞活化和炎症反应，抑制了神经元焦亡和凋亡以及GSDMD介导的信号传导[6]。
| Cell experiment [1]: | |
Cell lines | A549 cells |
Preparation Method | A549 cells were incubated with 5μM LDC7559 at 6h before irradiation. After 48h of irradiation, the levels of released LDH were detected as indicated. |
Reaction Conditions | 5μM; 6h |
Applications | LDC7559 significantly decreased LDH release in irradiated A549 cells. |
| Animal experiment [2]: | |
Animal models | Sprague-Dawley rats |
Preparation Method | Adult male Sprague-Dawley rats (weighing 230-280g) were used, rat model of subarachnoid hemorrhage (SAH) was built. Before SAH, anesthetization was administered with 1% sodium pentobarbital. A marked filament (4-0) was used to puncture the origin of the left middle cerebral artery. Sham-operated rats received the same treatment, but not with vessel perforation. In vivo experiments, rats were randomly allotted to sham group (n=18), SAH+vehicle group (n=22, 4 animals died), SAH + LDC7559 group (n=60, 6 animals died), and SAH+LDC7559+nigericin group (n=21, 3 animals died). LDC7559 was diluted in 10% DMSO and 90% corn oil before use. LDC7559 (10, 20, or 30mg/kg) or vehicle was treated at 2h after SAH by intraperitoneally administration and then once a day. Nigericin (2mg) was prepared in 2mL ethanol and physiologic saline and was intracerebroventricularly administered at 2h before SAH. |
Dosage form | 10, 20, 30mg/kg; i.p. |
Applications | LDC7559 treatment alleviated neurological deficits after SAH, inhibited microglial activation and inflammatory response, suppressed neuronal pyroptosis and apoptosis, and suppressed GSDMD-mediated signaling. |
References: | |
| Cas No. | 2407782-01-6 | SDF | Download SDF |
| 分子式 | C20H19N3O3 | 分子量 | 349.38 |
| 溶解度 | DMSO : ≥ 125 mg/mL (357.78 mM) | 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 | 2.8622 mL | 14.3111 mL | 28.6221 mL |
| 5 mM | 572.4 μL | 2.8622 mL | 5.7244 mL |
| 10 mM | 286.2 μL | 1.4311 mL | 2.8622 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。
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
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