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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.
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Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Halobetasol has not been studied during breastfeeding. Since only extensive application of the most potent corticosteroids may cause systemic effects in the mother, it is unlikely that short-term application of topical corticosteroids would pose a risk to the breastfed infant by passage into breastmilk. However, it would be prudent to use the least potent drug on the smallest area of skin possible. It is particularly important to ensure that the infant's skin does not come into direct contact with the areas of skin that have been treated. Only the lower potency corticosteroids should be used on the nipple or areola where the infant could directly ingest the drugs from the skin; avoid halobetasol on the nipple. Only water-miscible cream or gel products should be applied to the breast because ointments may expose the infant to high levels of mineral paraffins via licking. Any topical corticosteroid should be wiped off thoroughly prior to nursing if it is being applied to the breast or nipple area. ◉ Effects in Breastfed Infants Topical application of a corticosteroid with relatively high mineralocorticoid activity (isofluprednone acetate) to the mother's nipples resulted in prolonged QT interval, cushingoid appearance, severe hypertension, decreased growth and electrolyte abnormalities in her 2-month-old breastfed infant. The mother had used the cream since birth for painful nipples. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
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| References |
Indian J Dermatol Venereol Leprol.2009 Mar-Apr;75(2):186-7;Am J Clin Dermatol.2005;6(5):311-6.
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| Additional Infomation |
Halobetasol Propionate can cause developmental toxicity according to state or federal government labeling requirements.
Ulobetasol propionate is a corticosteroid hormone. Halobetasol Propionate is the propionate salt form of halobetasol, a synthetic corticosteroid with anti-inflammatory, antipruritic, and vasoconstrictor activities. Halobetasol, a topical steroid, diffuses across cell membranes to interact with cytoplasmic corticosteroid receptors located in both the dermal and intradermal cells, thereby activating gene expression of anti-inflammatory proteins mediated via corticosteroid receptor response element. Specifically, this agent induces phospholipase A2 inhibitory proteins, which inhibit the release of arachidonic acid, thereby inhibiting the biosynthesis of potent mediators of inflammation, such as prostaglandins and leukotrienes. As a result, halobetasol reduces edema, erythema, and pruritus through its cutaneous effects on vascular dilation and permeability. See also: Halobetasol (has active moiety); Halobetasol propionate; tazarotene (component of). |
| Molecular Formula |
C25H31CLF2O5
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| Molecular Weight |
484.96
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| Exact Mass |
484.183
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| CAS # |
66852-54-8
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| Related CAS # |
Halobetasol propionate-d5
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| PubChem CID |
6918178
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| Appearance |
White to off-white solid powder
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| Density |
0.934 g/mL at 25 °C(lit.)
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| Boiling Point |
55 °C0.3 mm Hg(lit.)
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| Melting Point |
-32°C
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| Flash Point |
185 °F
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| Index of Refraction |
n20/D 1.539(lit.)
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| LogP |
4.051
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
33
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| Complexity |
964
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| Defined Atom Stereocenter Count |
9
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| 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
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| InChi Key |
BDSYKGHYMJNPAB-LICBFIPMSA-N
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| 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
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| 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
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| Synonyms |
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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 |
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| 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) |
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| 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 |
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