Cell Viability Assay[2]
Cell Types: HaCaT, THP-1 Tested
Tested Concentrations: 0.05-12.85 μM
Incubation Duration: 24 h
Experimental Results: Affected decreasing the viability in both cell lines up to 50% corresponding to dilution 1/20.

Animal/Disease Models: New Zealand male albino rabbits[2]
Doses: 0.5 ml
Route of Administration: Intradermal injection
Experimental Results: Generated blisters were approximately 35% smaller.

Absorption, Distribution and Excretion
The peak plasma concentration (Cmax) of urobetasol emulsion was 201.1 ± 157.5 pg/mL, the time to peak concentration (Tmax) was 3 hours, and the area under the curve (AUC) was 1632 ± 1147 pgh/mL. Skin integrity, excipients used, inflammation, or disease processes can all affect absorption. Corticosteroids are primarily excreted in the urine. Biological Half-Life In vitro studies showed that the half-life of urobetasol's derivative, halobetasol propionate, is 33 minutes.

Protein Binding
Urobetasol may bind to corticosteroid-binding globulin in serum.

[1]. Schwicker D, et al. A cost-comparison study: Ulobetasol versus clobetasol in severe localized psoriasis. J Dermatolog Treat. 1992;2(4):127-131.

Halobetasol is a corticosteroid. Halobetasol is a potent corticosteroid with a structure related to clobetasol. Due to its high potency, it is primarily used to treat severe plaque psoriasis and corticosteroid-sensitive skin diseases. Halobetasol was approved by the U.S. Food and Drug Administration (FDA) on December 17, 1990. Halobetasol is a corticosteroid. Its mechanism of action is as a corticosteroid hormone receptor agonist. Halobetasol is a synthetic corticosteroid with anti-inflammatory, antipruritic, and vasoconstrictive effects. Halobetasol is a topical steroid that diffuses across cell membranes and interacts with cytoplasmic corticosteroid receptors located in dermal and intradermal cells, thereby activating the expression of anti-inflammatory protein genes mediated by corticosteroid receptor response elements. Specifically, the drug induces the expression of phospholipase A2 inhibitory protein, thereby inhibiting the release of arachidonic acid, and subsequently inhibiting the biosynthesis of potent inflammatory mediators such as prostaglandins and leukotrienes. Therefore, urobetasol reduces edema, erythema, and itching through its vasodilatory and permeable skin effects.
See also: urobetasol propionate (active ingredient).
Indications
Urobetasol cream and ointment are indicated for the treatment of inflammatory and pruritic skin conditions that respond to corticosteroids. Urobetasol lotion is indicated for the treatment of plaque psoriasis.
FDA Label
Mechanism of Action
The short-term effects of corticosteroids are to reduce capillary vasodilation and permeability, and to reduce the migration of leukocytes to sites of inflammation. Corticosteroids bind to glucocorticoid receptors, mediating alterations in gene expression that produce a variety of downstream effects over hours to days. Glucocorticoids inhibit phospholipase 2 and neutrophil apoptosis and marginalization, leading to reduced production of arachidonic acid derivatives. They also inhibit NF-κB and other inflammatory transcription factors while promoting the expression of anti-inflammatory genes such as interleukin-10. Low-dose corticosteroids have anti-inflammatory effects, while high-dose corticosteroids have immunosuppressive effects. Long-term use of high-dose glucocorticoids can bind to mineralocorticoid receptors, leading to increased sodium and decreased potassium levels.

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Pharmacodynamics
Corticosteroids bind to glucocorticoid receptors, inhibiting pro-inflammatory signaling and promoting anti-inflammatory signaling. Urobetasol has a moderate duration of action and only needs to be used once or twice daily. Corticosteroids have a wide therapeutic window, and patients may require doses several times higher than the body's naturally produced levels. Patients taking corticosteroids should be informed of the risks of hypothalamic-pituitary-adrenal axis suppression and increased susceptibility to infection.

C22H27CLF2O4

428.90

428.157

98651-66-2

5311167

White to off-white solid powder

200-216

3.09

2

6

2

29

843

9

CC1CC2C3CC(C4=CC(=O)C=CC4(C3(C(CC2(C1(C(=O)CCl)O)C)O)F)C)F

LEHFPXVYPMWYQD-XHIJKXOTSA-N

InChI=1S/C22H27ClF2O4/c1-11-6-13-14-8-16(24)15-7-12(26)4-5-19(15,2)21(14,25)17(27)9-20(13,3)22(11,29)18(28)10-23/h4-5,7,11,13-14,16-17,27,29H,6,8-10H2,1-3H3/t11-,13-,14-,16-,17-,19-,20-,21-,22-/m0/s1

(6S,8S,9R,10S,11S,13S,14S,16S,17R)-17-(2-chloroacetyl)-6,9-difluoro-11,17-dihydroxy-10,13,16-trimethyl-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-3-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)

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

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.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*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).

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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)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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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).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)