| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g | |||
| Other Sizes |
Purity: ≥98%
Halobetasol Propionate (BMY30056, CGP14458; BMY 30056, CGP 14458; BMY-30056; CGP-14458; Ulobetasol propionate) is a potent and synthetic corticosteroid with anti-inflammatory activity. It is used as a dermatologic agent for the treatment of psoriasis.
| ln Vitro |
|
||
|---|---|---|---|
| ln Vivo |
|
||
| Animal Protocol |
|
||
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Medication Use During Lactation The use of halometasone during lactation has not been studied. Since only large-area application of potent corticosteroids is likely to have systemic effects on the mother, short-term topical application of corticosteroids is unlikely to pose a risk to the nursing infant through breast milk. However, it is advisable to use the least potent medication on the smallest possible area of skin. It is especially important to ensure that the infant's skin does not come into direct contact with the treated area. Only use less potent corticosteroids on the nipple or areola, where the infant may ingest the medication directly through the skin; avoid using halometasone on the nipple. Only water-soluble creams or gels should be applied to the breast, as ointments may expose the infant to high concentrations of mineral oil through licking. If topical corticosteroids are applied to the breast or nipple area, they should be thoroughly wiped off before breastfeeding. ◉ Effects on Breastfed Infants A mother applied a topical corticosteroid (isofluprednisolone acetate) with high mineralocorticoid activity to her nipples, resulting in QT interval prolongation, Cushing's syndrome-like symptoms, severe hypertension, growth retardation, and electrolyte imbalance in her 2-month-old breastfed infant. The mother had been using the cream due to nipple pain since the infant's birth. ◉ Effects on Lactation and Breast Milk As of the revision date, no relevant published information was found. |
||
| References |
Indian J Dermatol Venereol Leprol.2009 Mar-Apr;75(2):186-7;Am J Clin Dermatol.2005;6(5):311-6.
|
||
| Additional Infomation |
Halobetasol propionate may cause developmental toxicity, depending on state or federal labeling requirements. Halobetasol propionate is a corticosteroid hormone. Halobetasol propionate is the propionate form of halobetasol, 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 gene expression of anti-inflammatory proteins mediated by corticosteroid receptor response elements. Specifically, the drug induces phospholipase A2 inhibitory protein, thereby inhibiting the release of arachidonic acid, which in turn inhibits the biosynthesis of potent inflammatory mediators such as prostaglandins and leukotrienes. Therefore, halobetasol reduces edema, erythema, and itching through its vasodilatory and permeable skin effects. See also: Halobetasol (with active fraction); Halobetasol propionate; Tazarotene (ingredient).
|
| Molecular Formula |
C25H31CLF2O5
|
|
|---|---|---|
| Molecular Weight |
484.96
|
|
| Exact Mass |
484.183
|
|
| CAS # |
66852-54-8
|
|
| Related CAS # |
Halobetasol propionate-d5
|
|
| PubChem CID |
6918178
|
|
| Appearance |
White to off-white solid powder
|
|
| Density |
0.934 g/mL at 25 °C(lit.)
|
|
| Boiling Point |
55 °C0.3 mm Hg(lit.)
|
|
| Melting Point |
-32°C
|
|
| Flash Point |
185 °F
|
|
| Index of Refraction |
n20/D 1.539(lit.)
|
|
| LogP |
4.051
|
|
| Hydrogen Bond Donor Count |
1
|
|
| Hydrogen Bond Acceptor Count |
7
|
|
| Rotatable Bond Count |
5
|
|
| Heavy Atom Count |
33
|
|
| Complexity |
964
|
|
| Defined Atom Stereocenter Count |
9
|
|
| SMILES |
ClC([H])([H])C([C@]1([C@@]([H])(C([H])([H])[H])C([H])([H])[C@@]2([H])[C@]3([H])C([H])([H])[C@@]([H])(C4=C([H])C(C([H])=C([H])[C@]4(C([H])([H])[H])[C@]3([C@]([H])(C([H])([H])[C@@]21C([H])([H])[H])O[H])F)=O)F)OC(C([H])([H])C([H])([H])[H])=O)=O
|
|
| InChi Key |
BDSYKGHYMJNPAB-LICBFIPMSA-N
|
|
| InChi Code |
InChI=1S/C25H31ClF2O5/c1-5-21(32)33-25(20(31)12-26)13(2)8-15-16-10-18(27)17-9-14(29)6-7-22(17,3)24(16,28)19(30)11-23(15,25)4/h6-7,9,13,15-16,18-19,30H,5,8,10-12H2,1-4H3/t13-,15-,16-,18-,19-,22-,23-,24-,25-/m0/s1
|
|
| Chemical Name |
[(6S,8S,9R,10S,11S,13S,14S,16S,17R)-17-(2-chloroacetyl)-6,9-difluoro-11-hydroxy-10,13,16-trimethyl-3-oxo-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-17-yl] propanoate
|
|
| Synonyms |
|
|
| HS Tariff Code |
2934.99.9001
|
|
| 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)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.16 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.16 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0620 mL | 10.3101 mL | 20.6203 mL | |
| 5 mM | 0.4124 mL | 2.0620 mL | 4.1241 mL | |
| 10 mM | 0.2062 mL | 1.0310 mL | 2.0620 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03298581 | Withdrawn | Drug: Halobetasol Propionate | Plaque Psoriasis | Sun Pharmaceutical Industries Limited | January 1, 2017 | Phase 2 |
| NCT03212963 | Terminated Has Results | Drug: Halobetasol Topical Lotion | Plaque Psoriasis | Sun Pharmaceutical Industries Limited | March 21, 2017 | Phase 4 |
| NCT04720105 | Completed Has Results | Drug: Duobrii® | Palmoplantar Psoriasis Plaque Psoriasis |
Icahn School of Medicine at Mount Sinai |
November 19, 2020 | Phase 4 |
| NCT00715975 | Completed | Drug: halobetasol Drug: clobetasol |
Psoriasis | Azidus Brasil | July 2008 | Phase 2 Phase 3 |