GlpBio

Dexamethasone palmitate

目录号: GC38573纯度: >98.00%同义词: 地塞米松棕榈酸酯; DXP
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。
Dexamethasone palmitate
Cas No.: 14899-36-6
规格价格库存数量操作
1mg¥134.00现货
1
5mg¥314.00现货
1
10mg¥468.00现货
1
25mg¥814.00现货
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50mg¥1,217.00现货
1
100mg¥1,847.00现货
1
200mg¥2,582.00现货
1
10mM (in 1mL DMSO)¥435.00现货
1
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产品描述 Description

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]。

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

RAW 264.7 cells

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.

Reaction Conditions

100 μg/mL Dexamethasone palmitate，24h

Applications

A decrease of cytokines concentration was clearly observed resulting from the anti-inflammatory effect of Dexamethasone palmitate-NPs.
Animal experiment [2]:

Animal models

Brown Norway male rats

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.

Dosage form

4 μg Dexamethasone palmitate；0.5 μL

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.

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号
14899-36-6
同义词
地塞米松棕榈酸酯; DXP
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 g/mol
溶解性
DMSO: 250 mg/mL (396.28 mM)
保存条件
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°C，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。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol