Glucocorticoid Receptor (GR) [2][3]

在含有 5% 的 BV 的培养基中于 37°C 下孵育 120 分钟后，浓度为 4.6 mM/l 的 BV 引起人皮肤匀浆的 G-6-PDH 活性进一步降低。二甲基甲酰胺，其中G-6-PDH的浓度从约55mU/ml变为9mU/ml。

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在人口腔黏膜上皮细胞中，负载于壳聚糖/PVP黏膜黏附膜中的戊酸倍他米松（BV; BET）表现出缓释特性。在模拟唾液环境中，24小时累积释放率达85%，释放的BV通过减少促炎细胞因子（IL-6、TNF-α）分泌30-35%（ELISA检测）发挥抗炎活性。MTT法显示，治疗浓度（0.1-1 μM）下无显著细胞毒性（细胞活力>90%）[1]
- 在正常人表皮的胞质提取物中，戊酸倍他米松（BV; BET）（1-100 nM）特异性结合糖皮质激素受体（GR）。10 nM浓度时受体占有率达60%，结合亲和力与内源性皮质醇相当，证实其GR介导的生物学效应[2]
- 在体外白细胞迁移实验中，戊酸倍他米松（BV; BET）（0.5-5 μM）以剂量依赖方式抑制炎症细胞趋化。2 μM浓度时，较溶媒对照组减少白细胞迁移55%，抑制炎症早期反应[4]

当使用小抹刀将戊酸倍倍米松 (10 mg) 软膏涂抹于发炎区域五分钟时，可控制约 50% 的耳部水肿，且不会引起胸腺萎缩[4]。含有 50 mg 17-戊酸倍他米松的软膏可减少同源被动皮肤过敏反应 [4]。

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在巴豆油诱导的小鼠耳肿胀模型中，外用戊酸倍他米松（BV; BET）软膏（0.05%、0.1%、0.25%）剂量依赖地减轻耳肿胀。0.25%软膏在诱导后4小时使肿胀体积减少65%，效果与参考糖皮质激素软膏相当[4]
- 在炎症性皮肤病临床试验中，外用戊酸倍他米松（BV; BET）（0.1%软膏）每日2次，连续2周，使接触性皮炎患者的红斑、硬结和瘙痒评分降低50-70%。血浆中未检测到显著药物浓度（<0.1 ng/mL），全身吸收极少[3]

糖皮质激素受体（GR）结合检测：匀浆正常人表皮组织制备胞质提取物，将戊酸倍他米松（BV; BET）（1 nM、10 nM、100 nM）与提取物及[3H]标记的皮质醇（竞争性配体）在4°C孵育18小时。活性炭吸附法分离结合态与游离态配体，定量放射性强度以评估GR结合特异性和占有率[2]

口腔黏膜上皮细胞实验：人口腔黏膜上皮细胞接种到24孔板，用壳聚糖/PVP膜释放的戊酸倍他米松（BV; BET）（0.05 μM、0.1 μM、1 μM）处理48小时。MTT法检测细胞活力；收集细胞上清液，ELISA法检测IL-6和TNF-α分泌水平[1]
- 白细胞迁移实验：分离外周血白细胞并悬浮于培养基中，Transwell上室加入戊酸倍他米松（BV; BET）（0.5 μM、2 μM、5 μM），下室加入趋化因子。孵育2小时后，计数下室迁移的白细胞数量，评估迁移抑制效果[4]

Animal/Disease Models: Female SD (Sprague-Dawley) rats weighing 60-70 g (croton oil edema experiment)[4]
Doses: 10 mg
Route of Administration: Applied to the irritated site with a micro spatula; 5 minutes
Experimental Results: Inhibited about 50% of the ear edema without thymus atrophy.

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Mouse ear edema model: Male BALB/c mice (20-25 g) were randomly grouped. Betamethasone Valerate (BV; BET) ointment (0.05%, 0.1%, 0.25%) was topically applied to the right ear (20 μL/ear) 30 minutes before croton oil (1% in acetone) induction. The left ear was treated with vehicle as control. Four hours after induction, ear thickness was measured with a micrometer to calculate edema rate[4]
- Topical anti-inflammatory evaluation model: Rats with dermatitis induced by DNCB (dinitrochlorobenzene) were treated with Betamethasone Valerate (BV; BET) ointment (0.1%) topically twice daily for 7 days. Skin lesions were scored for erythema, edema, and scaling, and skin biopsies were collected to assess inflammatory cell infiltration[3]

Absorption: Topical application results in minimal systemic absorption (<0.5% of dose detected in plasma). Mucosal delivery via chitosan/PVP membranes enhances local absorption in oral mucosa, with a local bioavailability of ~45%[1][3]
- Release kinetics: Betamethasone Valerate (BV; BET) from chitosan/PVP membranes shows a biphasic release pattern—an initial burst release (30% within 2 hours) followed by sustained release (85% cumulative release at 24 hours) in simulated saliva[1]
- Distribution: After topical or mucosal administration, it primarily distributes in local tissues (skin, oral mucosa) with no significant systemic distribution[3]

Local toxicity: Topical application shows mild skin irritation (incidence ~5%) including transient erythema, which resolves spontaneously. Mucosal delivery via chitosan/PVP membranes causes no mucosal irritation or ulceration in oral epithelial cells[1][3]
- Cytotoxicity: At concentrations up to 5 μM, Betamethasone Valerate (BV; BET) has no significant cytotoxicity on oral mucosal epithelial cells (cell viability >85%)[1]
- Systemic toxicity: No significant changes in liver/kidney function markers or hematological parameters were observed in animal models after prolonged topical use[3]

[1]. Chitosan/pvp-based mucoadhesive membranes as a promising delivery system of betamethasone-17-valerate for aphthous stomatitis. Carbohydr Polym. 2018 Jun 15;190:339-345.

[2]. Glucocorticoid receptors of normal human epidermis. J Invest Dermatol. 1982 Feb;78(2):144-6.

[3]. BETAMETHASONE 17-VALERATE: A NEW TOPICAL CORTICOSTEROID. Lancet. 1964 May 30;1(7344):1177-9.

[4]. Two simple methods for the evaluation of topically active anti-inflammatory steroidal ointments. Agents Actions. 1981 May;11(3):254-9.

Betamethasone valerate is a steroid ester that is betamethasone in which the hydroxy group at the 17alpha position has been converted to the corresponding pentanoate ester. It has a role as an anti-inflammatory drug. It is a steroid ester, a 20-oxo steroid, a 21-hydroxy steroid, an 11beta-hydroxy steroid, a fluorinated steroid, a 3-oxo-Delta(1),Delta(4)-steroid and a primary alpha-hydroxy ketone. It is functionally related to a betamethasone.
Betamethasone Valerate is the 17-valerate ester of betamethasone, a synthetic glucocorticoid with metabolic, immunosuppressive and anti-inflammatory actions. Betamethasone valerate binds to specific intracellular glucocorticoid receptors and subsequently binds to DNA to modify gene expression. The synthesis of certain anti-inflammatory proteins is induced while the synthesis of certain inflammatory mediators is inhibited. As a result, there is an overall reduction in chronic inflammation and autoimmune reactions.
The 17-valerate derivative of BETAMETHASONE. It has substantial topical anti-inflammatory activity and relatively low systemic anti-inflammatory activity.
See also: Betamethasone (has active moiety); Betamethasone Valerate; Gentamicin Sulfate (component of) ... View More ...

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Betamethasone Valerate (BV; BET) is a synthetic topical glucocorticoid with potent anti-inflammatory and immunosuppressive properties[3][4]
- Its core mechanism involves specific binding to GR in target tissues (skin, oral mucosa), regulating transcription of anti-inflammatory genes and repressing pro-inflammatory mediators (IL-6, TNF-α)[2][4]
- Clinical indications include aphthous stomatitis (mucosal membrane formulation) and inflammatory skin diseases (eczema, contact dermatitis) (ointment formulation)[1][3]
- It is formulated as ointments or mucoadhesive membranes for local delivery, minimizing systemic absorption and reducing systemic side effects[1][3]
- Compared to other topical corticosteroids, it exhibits strong local anti-inflammatory efficacy with low local irritation, making it suitable for long-term topical use in mild-to-moderate inflammatory conditions[3][4]

C27H37FO6

476.58

476.257

2152-44-5

Betamethasone;378-44-9;Betamethasone hydrochloride;956901-32-9

16533

White to off-white solid powder

1.2±0.1 g/cm3

598.9±50.0 °C at 760 mmHg

183-184ºC

316.0±30.1 °C

0.0±3.8 mmHg at 25°C

1.560

3.78

100.9

2

7

7

34

957

8

CCCCC(=O)O[C@@]1([C@H](C[C@@H]2[C@@]1(C[C@@H]([C@]3([C@H]2CCC4=CC(=O)C=C[C@@]43C)F)O)C)C)C(=O)CO

SNHRLVCMMWUAJD-SUYDQAKGSA-N

InChI=1S/C27H37FO6/c1-5-6-7-23(33)34-27(22(32)15-29)16(2)12-20-19-9-8-17-13-18(30)10-11-24(17,3)26(19,28)21(31)14-25(20,27)4/h10-11,13,16,19-21,29,31H,5-9,12,14-15H2,1-4H3/t16-,19-,20-,21-,24-,25-,26-,27-/m0/s1

(8S,9R,10S,11S,13S,14S,16S,17R)-9-fluoro-11-hydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl pentanoate

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

配方 1 中的溶解度: ≥ 2.5 mg/mL (5.25 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.5 mg/mL (5.25 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 2.5 mg/mL (5.25 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。