Isosakuranetin是一种存在于柑橘类植物中的黄烷酮，具有多种生物活性，对TRPM3的IC50值为50nM。
Cas No.:480-43-3
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
Isosakuranetin, a flavanone found in Citrus species with diverse biological activities, has an IC50 value of 50nM for TRPM3 [1]. Isosakuranetin can inhibit the activity of Sortase A (SrtA) and the transcription and expression of α-Hemolysin (Hla) in Staphylococcus aureus, and regulate the transcription of the upstream operon RNAIII of Hla [2]. Isosakuranetin has been widely used in rat models of peripheral neuropathy to alleviate mechanical, thermal, and cold hypersensitivity[3].
In vitro, Isosakuranetin treatment for 48 hours significantly increased the viability of HL-60 and U937 cells with IC50 values of 115.6µM and 30.4µM, respectively[4]. Treatment of HaCaT cells with 20µM Isosakuranetin for 24 hours significantly inhibited ultraviolet (UV)-B-mediated induction of MMP-1 and inhibited UV-B-induced phosphorylation of mitogen-activated protein kinase (MAPK) signaling pathway components ERK1/2, JNK1/2, and p38 proteins[5]. Treatment with 30µM Isosakuranetin for 48h significantly increased Tyr, TRP1, and TRP2 expression, upregulated MITF expression, and decreased MITF phosphorylation in B16 melanoma cells[6].
In vivo, Isosakuranetin treatment via oral administration at a dose of 5mg/kg daily for 1 week significantly increased the abundance of Parabacteroides in the intestinal tract of mice and affected amino acid metabolism pathways[7]. Intraperitoneal injection of a 2mg/kg dose of Isosakuranetin every other day for 8 weeks, which inhibited the formation of osteoclasts beneath the cartilage in the osteoarthritis (OA) mouse model, improved the degeneration of joint cartilage, and delayed the progression of OA[8].
References:
[1] Straub I, Krügel U, Mohr F, et al. Flavanones that selectively inhibit TRPM3 attenuate thermal nociception in vivo[J]. Molecular pharmacology, 2013, 84(5): 736-750.
[2] Tian L, Wang L, Yang F, et al. Exploring the modulatory impact of isosakuranetin on Staphylococcus aureus: Inhibition of sortase A activity and α-haemolysin expression[J]. Virulence, 2023, 14(1): 2260675.
[3] Jia S, Zhang Y, Yu J. Antinociceptive effects of isosakuranetin in a rat model of peripheral neuropathy[J]. Pharmacology, 2017, 100(3-4): 201-207.
[4] Tseng R H, Lai K M, Chou C M, et al. Isosakuranetin lnduces autophagy and apoptosis through AMPK and PI3K/Akt signaling in human leukemia cells[J]. Anticancer Research, 2025, 45(4): 1481-1500.
[5] Jung H, Lee E H, Lee T H, et al. The methoxyflavonoid isosakuranetin suppresses UV-B-induced matrix metalloproteinase-1 expression and collagen degradation relevant for skin photoaging[J]. International journal of molecular sciences, 2016, 17(9): 1449.
[6] Drira R, Sakamoto K. Isosakuranetin, a 4′-O-methylated flavonoid, stimulates melanogenesis in B16BL6 murine melanoma cells[J]. Life sciences, 2015, 143: 43-49.
[7] Cao X, Guo X, Fang X, et al. Effects of poncirin, a citrus flavonoid and its aglycone, isosakuranetin, on the gut microbial diversity and metabolomics in mice[J]. Molecules, 2022, 27(11): 3641.
[8] Lu S, Fang C. Isosakuranetin inhibits subchondral osteoclastogenesis for attenuating osteoarthritis via suppressing NF-κB/CXCL2 axis[J]. International Immunopharmacology, 2024, 143: 113321.
Isosakuranetin是一种存在于柑橘类植物中的黄烷酮，具有多种生物活性，对TRPM3的IC50值为50nM[1]。Isosakuranetin可抑制金黄色葡萄球菌中Sortase A（SrtA）的活性以及α-溶血素（Hla）的转录和表达，并调控Hla上游操纵子RNAIII的转录[2]。Isosakuranetin已被广泛用于大鼠周围神经病变模型，以缓解机械性、热性和冷性痛觉过敏[3]。
在体外，Isosakuranetin处理48小时显著提高了HL-60和U937细胞的活力，IC50值分别为115.6µM和30.4µM[4]。使用20µM的Isosakuranetin处理HaCaT细胞24小时，显著抑制了紫外线（UV）-B介导的MMP-1诱导，并抑制了UV-B诱导的丝裂原活化蛋白激酶（MAPK）信号通路组分ERK1/2、JNK1/2和p38蛋白的磷酸化[5]。使用30µM的Isosakuranetin处理48小时，显著增加了B16黑色素瘤细胞中Tyr、TRP1和TRP2的表达，上调了MITF的表达，并降低了MITF的磷酸化[6]。
在体内，每日口服给予5mg/kg剂量的Isosakuranetin，连续一周，显著增加了小鼠肠道中副拟杆菌属的丰度，并影响了氨基酸代谢通路[7]。每隔一天腹腔注射2mg/kg剂量的Isosakuranetin，持续八周，抑制了骨关节炎（OA）小鼠模型中软骨下方破骨细胞的形成，改善了关节软骨的退变，并延缓了OA的进展[8]。
| Cell experiment [1]: | |
Cell lines | HL-60 cells |
Preparation Method | HL-60 cells were cultured in RPMI‑1640 medium containing 20% FBS (fetal bovine serum), 10mM HEPES, 1.0mM sodium pyruvate, and 100U/ml penicillin-streptomycin and incubated at 37°C in the presence of 5% CO2. Cells were seeded in 96-well plates at a density of 4×104 cells/ml, 100μl medium was added to each well, and cultured overnight. The cells were treated with different concentrations of Isosakuranetin (0.12.5, 25, 50, 100, and 200µM) for 48 hours and then analyzed for cell viability. |
Reaction Conditions | 0.12.5, 25, 50, 100, and 200µM; 48h |
Applications | Isosakuranetin treatment reduced the cell viability of HL-60 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Male C57BL/6J mice |
Preparation Method | 10-week-old male C57BL/6J mice were housed in a specific pathogen-free (SPF) animal house maintained at 23°C with a 12h light/dark cycle and free access to water and food. After mice underwent inhalation anesthesia with sevoflurane, Anterior cruciate ligament transaction (ACLT) surgery was adopted on the right knee to establish the mechanical instability OA model. All mice were randomly divided into 3 groups (n=6 per group): Sham group (mice with the joint capsule open and treated with PBS), ACLT group (ACLT mice treated with PBS), and Isosakuranetin group (ACLT mice treated with Isosakuranetin). Isosakuranetin (2mg/kg) was intraperitoneally injected into the mice 3 days after ACLT surgery, administering treatment every other day for 8 weeks for 8 weeks. Mouse knee joint samples were collected for analysis. |
Dosage form | 2mg/kg; every other day for 8 weeks; i.p. |
Applications | Isosakuranetin treatment improved aberrant angiogenesis and nociceptive reaction in the subchondral bone marrow and hindered the loss of articular cartilage proteoglycan in mice. |
References: | |
| Cas No. | 480-43-3 | SDF | |
| 别名 | 异野樱素 | ||
| Canonical SMILES | O=C1C[C@@H](C2=CC=C(OC)C=C2)OC3=CC(O)=CC(O)=C13 | ||
| 分子式 | C16H14O5 | 分子量 | 286.28 |
| 溶解度 | DMSO : 125 mg/mL (436.64 mM) | 储存条件 | Store at 2-8°C,protect from light |
| 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.4931 mL | 17.4654 mL | 34.9308 mL |
| 5 mM | 698.6 μL | 3.4931 mL | 6.9862 mL |
| 10 mM | 349.3 μL | 1.7465 mL | 3.4931 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet