| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg | |||
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| Targets |
The primary target of Tixocortol pivalate is the glucocorticoid receptor (GR). As a glucocorticoid receptor agonist, the compound binds to the cytoplasmic glucocorticoid receptor, and the drug-receptor complex translocates to the nucleus, where it modulates the transcription of various genes involved in the inflammatory response. This leads to a broad spectrum of anti-inflammatory and immunosuppressive effects, including the inhibition of pro-inflammatory cytokine production and the suppression of immune cell activation.
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| ln Vitro |
In vitro, Tixocortol pivalate demonstrates glucocorticoid receptor agonist activity. Its activity is assessed in cell-based assays that measure glucocorticoid receptor activation, such as reporter gene assays or assays measuring the expression of glucocorticoid-responsive genes. The compound's anti-inflammatory activity is demonstrated by its ability to inhibit the production of pro-inflammatory cytokines in immune cells. However, detailed IC50 or EC50 values are not extensively reported.
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| ln Vivo |
In vivo, Tixocortol pivalate demonstrates potent anti-inflammatory and immunosuppressive activity when applied topically. It is effective in the treatment of various inflammatory skin conditions, including eczema, psoriasis, and dermatitis. The compound's efficacy is attributed to its ability to activate the glucocorticoid receptor and suppress the inflammatory response in the skin. It is also used as an allergen in diagnostic testing for corticosteroid hypersensitivity.
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| Enzyme Assay |
In vitro receptor binding assays for Tixocortol pivalate typically involve measuring its binding affinity to the glucocorticoid receptor. The receptor is incubated with a radiolabeled glucocorticoid ligand in the presence of varying concentrations of the compound. After incubation, bound and free ligands are separated, and the radioactivity is measured. The compound's affinity is expressed as the IC50 or Ki for displacement of the radiolabeled ligand.
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| Cell Assay |
Cellular assays for Tixocortol pivalate are performed using glucocorticoid-responsive cell lines. Cells are treated with the compound, and the expression of glucocorticoid-responsive genes is measured by quantitative PCR or reporter gene assays. The compound's ability to inhibit the production of pro-inflammatory cytokines is also assessed. These assays are used to study the cellular pharmacology of the compound.
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| Animal Protocol |
In vivo animal studies with Tixocortol pivalate are typically performed in models of skin inflammation. The compound is applied topically to the skin of animals with induced dermatitis or other inflammatory skin conditions. The reduction in inflammation, edema, and other clinical signs is measured. These studies are used to evaluate the compound's therapeutic efficacy and safety profile for dermatological use.
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| ADME/Pharmacokinetics |
Tixocortol pivalate has a molecular weight of 462.64 and a molecular formula of C26H38O5S. It is applied topically for dermatological use. When administered topically, systemic absorption is limited, minimizing the risk of systemic side effects. However, detailed pharmacokinetic parameters such as half-life, bioavailability, and clearance are not extensively reported in the available literature.
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| Toxicity/Toxicokinetics |
Tixocortol pivalate is generally well-tolerated when applied topically at therapeutic doses. Common side effects include local skin irritation, dryness, and redness. Systemic side effects, such as adrenal suppression, are rare due to the limited systemic absorption of the compound. However, long-term use of topical corticosteroids can be associated with various adverse effects, including skin atrophy and telangiectasia. Comprehensive toxicology data are available from its clinical use.
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| References | |
| Additional Infomation |
Tesotropilpitava is the pitava thioester of tesotrop. It has dual effects as an anti-allergic agent, a glucocorticoid receptor agonist, and an allergen. It is a corticosteroid, thioester, pitava ester, and tertiary α-hydroxy ketone. Its function is related to tesotrop. Tesotropilpitava is a standardized chemical allergen. The physiological effects of tesotropilpitava are achieved through increased histamine release and cell-mediated immunity.
Tixocortol pivalate is a topical corticosteroid used in dermatological preparations for the treatment of inflammatory skin conditions such as eczema, psoriasis, and dermatitis. It is also used as an allergen in diagnostic testing for corticosteroid hypersensitivity. The compound's anti-inflammatory activity is mediated through the activation of the glucocorticoid receptor. It is generally well-tolerated and has a favorable safety profile for topical use. |
| Molecular Formula |
C26H38O5S
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|---|---|
| Molecular Weight |
462.64
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| Exact Mass |
462.244
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| CAS # |
55560-96-8
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| PubChem CID |
15052414
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.23g/cm3
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| Boiling Point |
607ºC at 760mmHg
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| Flash Point |
320.9ºC
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| Index of Refraction |
1.581
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| LogP |
4.481
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
32
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| Complexity |
872
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| Defined Atom Stereocenter Count |
7
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| SMILES |
CC12CCC(=O)C=C1CCC3C2C(CC4(C3CCC4(C(=O)CSC(=O)C(C)(C)C)O)C)O
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| InChi Key |
BISFDZNIUZIKJD-XDANTLIUSA-N
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| InChi Code |
InChI=1S/C26H38O5S/c1-23(2,3)22(30)32-14-20(29)26(31)11-9-18-17-7-6-15-12-16(27)8-10-24(15,4)21(17)19(28)13-25(18,26)5/h12,17-19,21,28,31H,6-11,13-14H2,1-5H3/t17-,18-,19-,21+,24-,25-,26-/m0/s1
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| Chemical Name |
S-(2-((8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-10,13-dimethyl-3-oxo-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2-oxoethyl) 2,2-dimethylpropanethioate
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| Synonyms |
Tixocortol pivalate JO-1016 JO1016 JO 1016Pivalone
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.1615 mL | 10.8075 mL | 21.6151 mL | |
| 5 mM | 0.4323 mL | 2.1615 mL | 4.3230 mL | |
| 10 mM | 0.2162 mL | 1.0808 mL | 2.1615 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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