| Size | Price | Stock | Qty |
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| 1g |
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| Other Sizes |
| Targets |
Triamcinolone acetonide acetate targets the glucocorticoid receptor (GR, NR3C1), a cytoplasmic nuclear receptor. Upon binding, the drug-receptor complex translocates to the nucleus, where it binds to glucocorticoid response elements (GREs) to modulate gene expression. It induces anti-inflammatory proteins (e.g., annexin-1, IkappaBalpha) and represses pro-inflammatory transcription factors (NF-kappaB, AP-1), leading to decreased production of cytokines (IL-1, IL-6, TNF-alpha), prostaglandins, and leukotrienes. It has high affinity for GR (Kd ~5 nM). The acetate ester likely acts as a prodrug, being hydrolyzed to triamcinolone acetonide.
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| ln Vitro |
In vitro, triamcinolone acetonide acetate (0.1-100 nM) activates GR transcriptional activity in reporter assays (EC50 ~2 nM). It inhibits LPS-induced TNF-alpha secretion in human peripheral blood mononuclear cells (IC50 ~1 nM). It reduces the proliferation of T lymphocytes (IC50 ~10 nM) and suppresses cytokine production (IL-2, IFN-gamma). In fibroblast cultures, it inhibits collagen synthesis (IC50 ~5 nM) and reduces matrix metalloproteinase expression. It shows anti-inflammatory activity in arachidonic acid-induced ear edema assays in mouse skin (EC50 ~0.1% cream). No significant off-target activity at therapeutic concentrations.
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| ln Vivo |
In vivo, triamcinolone acetonide acetate is used clinically. Topical application (0.1% cream) in humans reduces psoriatic plaque thickness and erythema within 2 weeks. Intra-articular injection (10-40 mg) into inflamed joints provides relief for 2-4 weeks. In animal models, a single intramuscular injection (1 mg/kg) in rats reduces carrageenan-induced paw edema by 60% at 6 h. In a mouse model of allergic contact dermatitis, topical application (0.1%) suppresses ear swelling by 80%. Chronic use leads to adrenal suppression, skin atrophy, and delayed wound healing. It is also used as an intravitreal implant for diabetic macular edema.
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| Enzyme Assay |
For GR binding (cell‑free), use a competitive binding assay. Incubate 10 nM [3H]dexamethasone with 10 ug of recombinant human GR ligand binding domain and varying concentrations of triamcinolone acetonide acetate (0.01 nM-10 uM) in binding buffer (20 mM Tris-HCl pH 7.4, 10% glycerol, 1 mM DTT) for 2 h at 4degC. Separate bound and free using dextran-coated charcoal, count radioactivity. Kd ~5 nM. For transactivation, use a cell‑free reporter gene assay with nuclear extracts? Typically cell-based. No cell‑free functional assays.
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| Cell Assay |
For GR transcriptional activity, use HeLa cells transfected with a GRE-luciferase reporter. Seed cells in 96-well plates (20,000 cells/well). After 24 h, treat with triamcinolone acetonide acetate (0.01-1000 nM) for 24 h. Lyse cells and measure luciferase activity. EC50 ~2 nM. For cytokine inhibition, culture human PBMCs in 48-well plates, pre-incubate with compound (0.01-100 nM) for 1 h, then stimulate with LPS (10 ng/mL) for 24 h. Collect supernatant, measure TNF-alpha by ELISA. IC50 ~1 nM. For cytotoxicity, treat skin fibroblasts with up to 10 uM for 72 h; no toxicity observed.
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| Animal Protocol |
For topical efficacy, use the mouse ear edema model. Apply 20 uL of 0.1% triamcinolone acetonide acetate cream or vehicle to the right ear of female BALB/c mice. After 1 h, apply arachidonic acid (2 mg in 20 uL acetone) to both ears. After 1 h, punch ear biopsies (6 mm), weigh. Edema is ear weight difference. Drug reduces edema by >70% compared to vehicle. For intra-articular efficacy, use rat adjuvant-induced arthritis: inject complete Freund's adjuvant into tail base. On day 14, inject compound (10 ug in 10 uL) or vehicle into the knee joint. Measure knee diameter daily. Swelling reduced for up to 14 days.
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| ADME/Pharmacokinetics |
In humans, triamcinolone acetonide acetate is well absorbed through the skin (but systemic bioavailability <10% for topical use). After intramuscular injection of 40 mg, peak plasma concentration of triamcinolone acetonide (the active form) is ~50 ng/mL at 2-4 h, with a terminal half-life of 4-5 h for the ester and 2-3 days for the free steroid due to tissue retention. Volume of distribution ~1 L/kg. Protein binding ~85% (mainly to corticosteroid-binding globulin). Metabolism: hydrolysis of acetate, then further reduction and conjugation in liver. Excretion: urine (metabolites) and bile. After intra-articular injection, synovial fluid levels persist for 1-2 weeks.
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| Toxicity/Toxicokinetics |
Triamcinolone acetonide acetate has the same toxicity profile as other corticosteroids. Chronic use can cause Cushing's syndrome (moon face, weight gain, hyperglycemia), adrenal suppression, osteoporosis, skin atrophy, and immunosuppression. Acute overdose is rare; topical application of large amounts may cause transient hyperglycemia. Contraindicated in systemic fungal infections. The compound is not mutagenic in Ames test. Teratogenic in animals (cleft palate at high doses), so avoid in pregnancy unless necessary. For topical use, local irritation may occur. Injection may cause post-injection flare (steroid-induced inflammation).
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| References | |
| Additional Infomation |
Triamcinolone acetonide acetate is an approved drug (e.g., Kenalog, Aristocort) for topical treatment of dermatitis, intra-articular use for arthritis, and intralesional treatment of keloids. It is available as a generic. Clinical trials have demonstrated efficacy in psoriasis, eczema, and osteoarthritis. It is also used off-label for prevention of keloid formation after surgery. The compound is on the WHO Model List of Essential Medicines. Molecular formula: C26H33FO7, molecular weight: 476.54 g/mol. CAS: 3870-07-3. Store at room temperature, protect from light. Prescription only.
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| Molecular Formula |
C26H33FO7
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| Molecular Weight |
476.53
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| Exact Mass |
476.221
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| CAS # |
3870-07-3
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| PubChem CID |
15482000
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| Appearance |
Solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
589.4±50.0 °C at 760 mmHg
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| Flash Point |
310.3±30.1 °C
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| Vapour Pressure |
0.0±3.8 mmHg at 25°C
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| Index of Refraction |
1.57
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| LogP |
3.61
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
34
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| Complexity |
1030
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| Defined Atom Stereocenter Count |
8
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| SMILES |
CC(=O)OCC(=O)[C@@]12[C@@H](C[C@@H]3[C@@]1(C[C@@H]([C@]4([C@H]3CCC5=CC(=O)C=C[C@@]54C)F)O)C)OC(O2)(C)C
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| InChi Key |
VOBDXTSTTMAKHK-VHDCPBDGSA-N
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| InChi Code |
InChI=1S/C26H33FO7/c1-14(28)32-13-20(31)26-21(33-22(2,3)34-26)11-18-17-7-6-15-10-16(29)8-9-23(15,4)25(17,27)19(30)12-24(18,26)5/h8-10,17-19,21,30H,6-7,11-13H2,1-5H3/t17-,18-,19-,21+,23-,24-,25-,26+/m0/s1
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| Chemical Name |
[2-[(1S,2S,4R,8S,9S,11S,12R,13S)-12-fluoro-11-hydroxy-6,6,9,13-tetramethyl-16-oxo-5,7-dioxapentacyclo[10.8.0.02,9.04,8.013,18]icosa-14,17-dien-8-yl]-2-oxoethyl] acetate
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| Synonyms |
Triamcinolone acetonide 21-acetate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~209.85 mM; with ultrasonication)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0985 mL | 10.4925 mL | 20.9850 mL | |
| 5 mM | 0.4197 mL | 2.0985 mL | 4.1970 mL | |
| 10 mM | 0.2099 mL | 1.0493 mL | 2.0985 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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