Randialic acid B
目录号 : GC66363
Randialic acid B 是一种三萜化合物，是一种甲酰肽受体 1 (FPR1) 拮抗剂。Randialic acid B 阻断人中性粒细胞中的 FPR1 并在体内减轻银屑病样炎症。
Cas No.:14021-14-8
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
Randialic acid B, a triterpenoid compound, is a formyl peptide receptor 1 (FPR1) antagonist. Randialic acid B blocks FPR1 in human neutrophils and attenuates psoriasis-like inflammation in vivo[1].
Randialic acid B (0.1-3 μM; for 5 min) selectively inhibits reactive oxygen species production, elastase release, and CD11b expression in human neutrophils activated by FPR1. Randialic acid B inhibits the binding of N-formyl peptide to FPR1 in human neutrophils, neutrophil-like THP-1 cells, and hFPR1-transfected HEK293 cells, indicating FPR1 antagonism[1].
Randialic acid B acts competitively for its binding to the FPR1 receptor. The FPR1-downstream signaling such as Ca2+ mobilisation and activation of Akt and MAPKs is also competitively inhibited[1].
Randialic acid B shows significant cell-protective effects against H2O2-induced H9c2 cardiomyocyte injury[2].
Randialic acid B (10 mg/kg; i.v.; every other day; for 5 days) significantly reduces Imiquimod-induced psoriasis-like symptom, including epidermal hyperplasia, desquamation with scaling, neutrophil skin infiltration, and transepidermal water loss[1].
| Animal Model: | BALB/c white female mice (20 g weight; 7-week-old) treated with Imiquimod[1] |
| Dosage: | 10 mg/kg |
| Administration: | i.v.; every other day; for 5 days |
| Result: | Significantly reduced Imiquimod-induced psoriasis-like symptoms. |
| Cas No. | 14021-14-8 | SDF | Download SDF |
| 分子式 | C30H46O3 | 分子量 | 454.68 |
| 溶解度 | DMSO : 100 mg/mL (219.93 mM; ultrasonic and warming and heat to 60°C) | 储存条件 | 4°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。 |
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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 | 2.1993 mL | 10.9967 mL | 21.9935 mL |
| 5 mM | 0.4399 mL | 2.1993 mL | 4.3987 mL |
| 10 mM | 0.2199 mL | 1.0997 mL | 2.1993 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。
Randialic acid B and tomentosolic acid block formyl peptide receptor 1 in human neutrophils and attenuate psoriasis-like inflammation in vivo
Biochem Pharmacol 2021 Aug;190:114596.PMID:33964283DOI:10.1016/j.bcp.2021.114596.
Psoriasis is a long-lasting inflammatory skin disease lacking proper cure. Dysregulated activation of neutrophils is a major pathogenic factor in psoriasis. Formyl peptide receptor 1 (FPR1) triggers neutrophil activation in response to bacteria- or mitochondria-derived N-formyl peptides, but its significance in neutrophilic psoriasis remains unknown. In this study, we discovered two derivatives of ursolic acid, 3β-hydroxyurs-12,18-dien-28-oic acid (Randialic acid B, RAB) and 3β-hydroxyurs-12,19-dien-28-oic acid (tomentosolic acid, TA), as FPR1 inhibitors in human neutrophils with ability to suppress psoriatic symptoms in mice. Both RAB and TA, triterpenoids of traditional medicinal plant Ilex kaushue, selectively inhibited reactive oxygen species production, elastase release, and CD11b expression in human neutrophils activated by FPR1, but not non-FPR1 agonists. Importantly, RAB and TA inhibited the binding of N-formyl peptide to FPR1 in human neutrophils, neutrophil-like THP-1 cells, and hFPR1-transfected HEK293 cells, indicating FPR1 antagonism. Moreover, in assays induced by various concentrations of FPR1 agonist, both RAB and TA acted competitively for its binding to the FPR1 receptor. The FPR1-downstream signaling such as Ca2+ mobilisation and activation of Akt and MAPKs was also competitively inhibited. In addition, imiquimod-induced psoriasis-like symptoms, including epidermal hyperplasia, desquamation with scaling, neutrophil skin infiltration, and transepidermal water loss were significantly reduced by both RAB and TA. The results illustrate a possible role of human neutrophils FPR1 receptor in psoriasis-like inflammation. Accordingly, triterpenoids RAB and TA represent novel FPR1 antagonists and exhibit therapeutic potential for treating neutrophilic inflammatory skin diseases.
Three new triterpenoids isolated from the aerial parts of Ilex cornuta and protective effects against H2O2-induced myocardial cell injury
Chin J Nat Med 2017 Feb;15(2):115-120.PMID:28284425DOI:10.1016/S1875-5364(17)30027-4.
In the present study, three new triterpenoids, 23-hydroxyurs-12, 18-dien-28-oic acid 3β-O-α-L-arabinopyranoside (1), 23-hydroxyurs-12, 18-dien-28-oic acid 3β-O-β-D-glucuronopyranoside-6-O-methyl ester (2), and urs-12, 18-dien-28-oic acid 3β-O-β-D-glucuronopyranoside-6-O-methyl ester (3), and a known triterpenoid, 3β-hydroxy-urs-2, 18-dien-28-oic acid (4, Randialic acid B), were isolated from the aerial parts of Ilex cornuta. Their structures were identified by the spectroscopic analyses (IR, ESI-MS, HR-ESI-MS, and 1D and 2D NMR) and chemical reactions. Compound 4 showed significant cell-protective effects against H2O2-induced H9c2 cardiomyocyte injury. Compounds 1-4 did not show any significant DPPH radical scavenging activity.