Dexamethasone palmitate
(Synonyms: 地塞米松棕榈酸酯; DXP) 目录号 : GC38573
地塞米松棕榈酸酯 (DXP) 是地塞米松 (DXM) 的亲脂性前药，是一种糖皮质激素受体激动剂，与糖皮质激素受体的亲和力比 DXM 低 47 倍。
Cas No.:14899-36-6
Sample solution is provided at 25 µL, 10mM.
Dexamethasone palmitate (DXP), a lipophilic prodrug of Dexamethasone (DXM), is a glucocorticoid receptor agonist with a 47-fold lower affinity for the glucocorticoid receptor than DXM[1].
A decrease of cytokines concentration was clearly observed resulting from the anti-inflammatory effect of Dexamethasone palmitate-NPs .the MCP-1 chemokine was strongly and significantly reduced by Dexamethasone palmitate-NPs and TNFα in presence of LPS[2].
Rat efficacy data demonstrated that IVT administration of Dexamethasone palmitate emulsions is effective for delivering therapeutic concentrations of DXM at the level of the choroid[2]. Dexamethasone palmitate-NPs could benefit from the typical high vascular permeability of inflamed joints and diffuse passively to accumulate and be retained in the diseased sites. This accumulation in inflamed joints led to improvement of the joint inflammation and eventually disease remission[3].
References:
[1]:Romero IA, Radewicz K, Jubin E, Michel CC, Greenwood J, Couraud PO, Adamson P. Changes in cytoskeletal and tight junctional proteins correlate with decreased permeability induced by dexamethasone in cultured rat brain endothelial cells. Neurosci Lett. 2003 Jun 26;344(2):112-6. doi: 10.1016/s0304-3940(03)00348-3. PMID: 12782340.
[2]: Daull P, Paterson CA, Kuppermann BD, Garrigue JS. A preliminary evaluation of dexamethasone palmitate emulsion: a novel intravitreal sustained delivery of corticosteroid for treatment of macular edema. J Ocul Pharmacol Ther. 2013 Mar;29(2):258-69. doi: 10.1089/jop.2012.0044. Epub 2013 Jan 18. PMID: 23331052.
[3]: Lorscheider M, Tsapis N, Ur-Rehman M, Gaudin F, Stolfa I, Abreu S, Mura S, Chaminade P, Espeli M, Fattal E. Dexamethasone palmitate nanoparticles: An efficient treatment for rheumatoid arthritis. J Control Release. 2019 Feb 28;296:179-189. doi: 10.1016/j.jconrel.2019.01.015. Epub 2019 Jan 16. PMID: 30659904.
地塞米松棕榈酸酯 (DXP) 是地塞米松 (DXM) 的亲脂性前药，是一种糖皮质激素受体激动剂，与糖皮质激素受体的亲和力比 DXM 低 47 倍[1]。
由于地塞米松棕榈酸酯-NP 的抗炎作用，清楚地观察到细胞因子浓度降低。在 LPS 存在的情况下，MCP-1 趋化因子被地塞米松棕榈酸酯-NP 和 TNFα 强烈而显着地降低[2 ].
大鼠疗效数据表明，IVT 给予地塞米松棕榈酸酯乳剂可有效地在脉络膜水平递送治疗浓度的 DXM[2]。地塞米松棕榈酸酯-NPs 可以受益于发炎关节典型的高血管通透性，并被动扩散以积聚并保留在患病部位。这种在发炎关节中的积累导致关节炎症的改善，并最终缓解了疾病[3]。
| Cell experiment [1]: | |
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Cell lines |
RAW 264.7 cells |
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Preparation Method |
After 24 h of incubation with 100 μg/mL Dexamethasone palmitate, cell supernatants were collected and frozen at 20 C until analysis was performed. Cells were detached and counted. |
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Reaction Conditions |
100 μg/mL Dexamethasone palmitate，24h |
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Applications |
A decrease of cytokines concentration was clearly observed resulting from the anti-inflammatory effect of Dexamethasone palmitate-NPs. |
| Animal experiment [2]: | |
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Animal models |
Brown Norway male rats |
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Preparation Method |
Choroidal neovascularization (CNV) was induced with a 532-nm argon laser photocoagulator in the right eyes of the anesthetized animals. Following the laser procedure on day 0 supratemporal IVT injections of either the vehicle [phosphate- buffered saline (PBS); 0.8% Dexamethasone palmitate emulsion (4 μg Dexamethasone palmitate; 0.5 μL), and Kenacort were administered to the treated right eyes. |
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Dosage form |
4 μg Dexamethasone palmitate；0.5 μL |
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Applications |
Rat efficacy data demonstrated that IVT administration of Dexamethasone palmitate emulsions is effective for delivering therapeutic concentrations of DXM at the level of the choroid. |
|
References: [1]. Romero IA, Radewicz K, et,al. Changes in cytoskeletal and tight junctional proteins correlate with decreased permeability induced by dexamethasone in cultured rat brain endothelial cells. Neurosci Lett. 2003 Jun 26;344(2):112-6. doi: 10.1016/s0304-3940(03)00348-3. PMID: 12782340. [2]. Daull P, Paterson CA, et,al. A preliminary evaluation of dexamethasone palmitate emulsion: a novel intravitreal sustained delivery of corticosteroid for treatment of macular edema. J Ocul Pharmacol Ther. 2013 Mar;29(2):258-69. doi: 10.1089/jop.2012.0044. Epub 2013 Jan 18. PMID: 23331052. |
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| Cas No. | 14899-36-6 | SDF | |
| 别名 | 地塞米松棕榈酸酯; DXP | ||
| Canonical SMILES | C[C@@]12[C@](C[C@@H](C)[C@]2(O)C(COC(CCCCCCCCCCCCCCC)=O)=O)([H])[C@@]3([H])[C@@](F)([C@@]4(C(CC3)=CC(C=C4)=O)C)[C@@H](O)C1 | ||
| 分子式 | C38H59FO6 | 分子量 | 630.87 |
| 溶解度 | DMSO: 250 mg/mL (396.28 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.5851 mL | 7.9256 mL | 15.8511 mL |
| 5 mM | 0.317 mL | 1.5851 mL | 3.1702 mL |
| 10 mM | 0.1585 mL | 0.7926 mL | 1.5851 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%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet