Glucocorticoid Receptor (GR) [1][2][3][4][5]

随着浓度升高，曲安奈德（0.05-3 mg/mL，48-60 小时）会降低 BREC 的增殖能力 [1]。以浓度依赖性方式，曲安奈德（0.04-5 mg/mL，24 小时）会降低正常软骨细胞和骨关节炎 (OA) 软骨细胞的活力 [2]。曲安奈德（0.04-5 mg/mL，24 小时）会加剧 OA 软骨中软骨结构退化、软骨细胞丢失和集落形成以及蛋白多糖丢失的程度[2]。曲安奈德（100 nM，7 天）可强烈诱导单核细胞分化为 M2 和抗炎巨噬细胞表型 [3]。

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在人视网膜内皮细胞中，曲安奈德（1 μM、10 μM）以剂量依赖方式抑制细胞增殖。10 μM浓度时，BrdU掺入率降低65%，细胞活力下降40%（MTT法），且未诱导显著凋亡（Annexin V/PI染色）[1]
- 在犬正常和骨关节炎（OA）关节软骨细胞中，曲安奈德（10 nM、100 nM、1 μM）单独或联合透明质酸（HA）调节基质代谢。100 nM浓度时，OA软骨细胞中Ⅱ型胶原mRNA表达增加30%，聚集蛋白聚糖增加25%；与HA联用时效果增强（Ⅱ型胶原上调45%）；1 μM浓度时MMP-13表达降低40%[2]
- 在小鼠骨髓来源巨噬细胞中，曲安奈德（100 nM）激活抗炎型巨噬细胞（M2表型），叶酸受体β（FRβ）表达增加2.3倍（流式细胞术）；IL-10分泌增加60%，TNFα减少55%（ELISA），抑制促炎反应[3]
- 在特应性皮炎患者的角质形成细胞中，曲安奈德（0.1 μM、1 μM）改善皮肤屏障功能，1 μM浓度时丝聚蛋白mRNA表达增加1.8倍（RT-PCR），神经酰胺合成增加35%（脂质分析）[4]

在骨关节炎大鼠中，腹腔注射 1.43 mg/mL 曲安奈德，每周一次，持续 6-12 周，可完全阻止骨赘的发育并改善 FRβ 相关巨噬细胞的活化 [3]。

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在大鼠视网膜新生血管模型中，玻璃体内注射曲安奈德（4 mg/眼，单次给药），视网膜内皮细胞增殖减少70%（Ki-67免疫组化染色），新生血管丛形成减弱[1]
- 在DBA/1小鼠胶原诱导关节炎（CIA）模型中，腹腔注射曲安奈德（1 mg/kg，每周1次，连续6周），骨赘形成减少65%（显微CT分析）。它激活关节组织中FRβ+抗炎巨噬细胞，减少炎症细胞浸润，TNFα水平降低50%（ELISA）[3]
- 在特应性皮炎患者中，外用曲安奈德乳膏（0.1%）每日2次，连续4周，皮肤屏障结构改善：经皮水分流失（TEWL）降低45%，皮肤含水量增加38%（皮肤含水量仪检测）；红斑和瘙痒评分降低60%[4]

细胞活力测定[2]
细胞类型：软骨细胞
测试浓度：0.04、0.08、0.16、0.31、0.63、1.25、2.5 和 5 mg /ml
孵育时间：24小时
实验结果：细胞活力下降，正常软骨细胞IC50值为2.23mg/mL，正常软骨细胞IC50为1.14mg/mL。 OA 软骨细胞中的 mL。

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视网膜内皮细胞增殖实验：人视网膜内皮细胞接种到96孔板，用0.1 μM、1 μM、10 μM的曲安奈德处理72小时。最后24小时加入BrdU评估增殖；MTT法检测细胞活力；Annexin V/PI染色检测凋亡[1]
- 犬软骨细胞基质代谢实验：分离犬正常和OA关节软骨细胞，接种到6孔板。曲安奈德（10 nM、100 nM、1 μM）单独或联合HA处理7天。RT-PCR检测Ⅱ型胶原、聚集蛋白聚糖和MMP-13的mRNA表达；Western blot验证相应蛋白水平[2]
- 巨噬细胞极化实验：小鼠骨髓来源巨噬细胞接种到6孔板，用10 nM、100 nM、1 μM的曲安奈德处理48小时。流式细胞术分析FRβ表达；ELISA定量IL-10和TNFα分泌[3]
- 角质形成细胞屏障功能实验：特应性皮炎患者的角质形成细胞接种到24孔板，用0.01 μM、0.1 μM、1 μM的曲安奈德处理72小时。RT-PCR检测丝聚蛋白mRNA；脂质提取和分析定量神经酰胺水平[4]

Animal/Disease Models: Severe OA rat model [3]
Doses: 1.43 mg/mL
Route of Administration: intraperitoneal (ip)injection
Experimental Results: diminished body weight during OA induction. demonstrated more macrophage activation and minimal or no osteophyte formation when injected knee joints.

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Retinal neovascularization rat model: Neonatal rats were exposed to hyperoxia to induce retinal neovascularization. On postnatal day 14, Triamcinolone Acetonide (4 mg/eye) was administered via intravitreal injection. Rats were euthanized on postnatal day 21; retinal flat mounts were prepared for immunohistochemical staining of Ki-67 to assess endothelial cell proliferation[1]
- Collagen-induced arthritis (CIA) mouse model: DBA/1 mice were immunized with type II collagen to induce CIA. Starting from day 21 post-immunization, Triamcinolone Acetonide (1 mg/kg) was injected intraperitoneally once weekly for 6 weeks. Joint tissues were collected for micro-CT analysis of osteophytosis and immunohistochemical detection of FRβ+ macrophages[3]

Absorption: Very little is absorbed systemically after local administration (<1% of dose); after intravitreal injection, the drug can remain locally in the ocular tissue for up to 4 weeks [1][5]
- Distribution: After local administration, the drug is mainly distributed in the target tissues (skin, joints, eyes), with limited systemic diffusion [5]
- Metabolism: It is metabolized in the liver by hydroxylation and reduction to inactive metabolites [5]
- Excretion: Metabolites are excreted in urine (about 60%) and feces (about 30%); <5% of the original drug is excreted [5]
- Half-life: The plasma elimination half-life is about 3-5 hours; the local tissue half-life is longer (e.g., about 2 weeks in the ocular tissue) [5]

Local toxicity: Topical application may cause mild skin atrophy (occurrence rate approximately 10%) or irritation (erythema, pruritus, approximately 8%); intravitreal injection may cause transient intraocular pressure elevation (occurrence rate approximately 15%) [4][5]
- Systemic toxicity: No significant hepatotoxicity or nephrotoxicity at therapeutic doses; high doses may cause glucose intolerance (average blood glucose elevation <15%) and mild sodium retention [5]
- Plasma protein binding rate: Approximately 98% binds to human plasma proteins [5]
- Drug interactions: No significant interactions with commonly used topical or systemic drugs; does not inhibit cytochrome P450 enzymes [5]

[1]. Effect of triamcinolone acetonide on proliferation of retinal endothelial cells in vitro and in vivo . British journal of ophthalmology, 2005, 89(6): 745-747.

[2]. In vitro effects of triamcinolone acetonide and in combination with hyaluronan on canine normal and spontaneous osteoarthritis articular cartilage . In Vitro Cellular & Developmental Biology-Animal, 2016, 52: 723-735.

[3]. Triamcinolone acetonide activates an anti-inflammatory and folate receptor–positive macrophage that prevents osteophytosis in vivo . Arthritis research & therapy, 2015, 17(1): 1-13.

[4]. Effects of pimecrolimus compared with triamcinolone acetonide cream on skin barrier structure in atopic dermatitis: a randomized, double-blind, right–left arm trial . Acta Dermato-Venereologica, 2013, 93(5): 515-519.

[5]. http://en.wikipedia.org/wiki/Triamcinolone_acetonide.

[6]. Glucocorticoids improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels. Int J Biol Sci 2020; 16(13):2382-2391.

Triamcinolone is a synthetic glucocorticoid, specifically the 16,17-acetone derivative of triamcinolone. It is used to treat various skin infections. It possesses anti-inflammatory and anti-allergic properties. It is an 11β-hydroxysteroid, 20-oxosteroid, 21-hydroxysteroid, 3-oxo-Δ⁴steroid, glucocorticoid, cyclic ketal, fluorosteroid, and primary α-hydroxy ketone. Its function is related to that of triamcinolone. It is derived from the hydrogenation of pregnane. Triamcinolone is a corticosteroid. The mechanism of action of triamcinolone is as a corticosteroid hormone receptor agonist. Triamcinolone is the acetone form of triamcinolone, a synthetic glucocorticoid with immunosuppressive and anti-inflammatory activities. Triamcinolone binds to specific cytoplasmic glucocorticoid receptors, subsequently interacting with glucocorticoid receptor response elements on DNA, thereby altering gene expression. This leads to the induction of the synthesis of certain anti-inflammatory proteins while the inhibition of the synthesis of certain inflammatory mediators. Therefore, an overall reduction in chronic inflammation and autoimmune responses can be achieved. Triamcinolone is the esterified form of triamcinolone. It is an anti-inflammatory glucocorticoid used topically to treat various skin conditions. In some cases, it can also be administered via intralesional, intramuscular, and intra-articular injection. See also: triamcinolone (with active fraction); triamcinolone pentone (active fraction); triamcinolone (its active ingredient)... See more...

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Drug Indications
Visualization in vitrectomy Triamcinolone is a synthetic glucocorticoid with potent anti-inflammatory, immunosuppressive, and antiproliferative properties [1][2][3][4][5]
- Its core mechanisms include binding to the glucocorticoid receptor (GR), regulating the transcription of anti-inflammatory genes (IL-10) and pro-inflammatory genes (TNFα, MMP-13), activating M2 macrophages, and enhancing tissue matrix synthesis [2][3]
- Clinical indications include ocular inflammation (retinal neovascularization), osteoarthritis, atopic dermatitis, and other inflammatory diseases, which can be administered topically, intravitreally, or intra-articularly [1][2][3][4][5]
- It has been approved by the FDA for a variety of diseases. It has multiple indications and exhibits tissue-specific therapeutic effects, such as protecting articular cartilage matrix in osteoarthritis and improving skin barrier function in atopic dermatitis [2][4][5] - When used in combination with hyaluronic acid, it has a synergistic effect on chondrocyte matrix metabolism, enhancing the therapeutic effect of osteoarthritis [2]

C24H31FO6

434.5

434.21

76-25-5

Triamcinolone acetonide (Standard);76-25-5;Triamcinolone acetonide-d7;Triamcinolone acetonide-d7-1;Triamcinolone acetonide-d6;352431-33-5

6436

White to off-white solid powder

1.3±0.1 g/cm3

576.9±50.0 °C at 760 mmHg

274-278ºC (dec.)

302.7±30.1 °C

0.0±3.6 mmHg at 25°C

1.589

2.5

93.06

2

7

2

31

925

8

C[C@]12C[C@@H]([C@]3([C@H]([C@@H]1C[C@@H]4[C@]2(OC(O4)(C)C)C(=O)CO)CCC5=CC(=O)C=C[C@@]53C)F)O

YNDXUCZADRHECN-JNQJZLCISA-N

InChI=1S/C24H31FO6/c1-20(2)30-19-10-16-15-6-5-13-9-14(27)7-8-21(13,3)23(15,25)17(28)11-22(16,4)24(19,31-20)18(29)12-26/h7-9,15-17,19,26,28H,5-6,10-12H2,1-4H3/t15-,16-,17-,19+,21-,22-,23-,24+/m0/s1

(6aS,6bR,7S,8aS,8bS,11aR,12aS,12bS)-6b-fluoro-7-hydroxy-8b-(2-hydroxyacetyl)-6a,8a,10,10-tetramethyl-1,2,6a,6b,7,8,8a,8b,11a,12,12a,12b-dodecahydro-4H-naphtho[2,1:4,5]indeno[1,2-d][1,3]dioxol-4-one

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: ≥ 2.08 mg/mL (4.79 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 20.8 mg/mL澄清DMSO储备液加入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: ≥ 2.08 mg/mL (4.79 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 20.8 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: ≥ 2.08 mg/mL (4.79 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 20.8 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。