| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
Purity: ≥98%
Betamethasone Valerate (BV; BET; Betoid; Valison; 9α-Fluo; Valisone; Bedermin; Betneval; Beta-Val; Bextasol; Dermosol; Stanoval) is a moderately potent and commonly used glucocorticoid steroid with anti-inflammatory and immunosuppressive activities. Betamethasone valerate is approved as an anti-inflammatory corticosteroid for topical applications.
| Targets |
Glucocorticoid Receptor (GR) [2][3]
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| ln Vitro |
In vitro activity: The presence of BV at a concentration of 4.6 mM/l provoked a still further diminuition of the G-6-PDH-activity of human skin homogenates that followed the incubation for 120 min at 37°C in media containing 5% dimethylformamide and in which the concentration of G-6-PDH changed from about 55 mU/ml to 9 mU/ml.
In human oral mucosal epithelial cells, Betamethasone Valerate (BV; BET) loaded in chitosan/PVP mucoadhesive membranes showed sustained release behavior. At 24 hours, the cumulative release rate reached 85% in simulated saliva, and the released BV exhibited anti-inflammatory activity by reducing pro-inflammatory cytokine (IL-6, TNF-α) secretion by 30-35% (ELISA). MTT assay showed no significant cytotoxicity (cell viability >90%) at therapeutic concentrations (0.1-1 μM)[1] - In cytosolic extracts from normal human epidermis, Betamethasone Valerate (BV; BET) (1-100 nM) specifically bound to glucocorticoid receptors (GR). The binding affinity was comparable to endogenous cortisol, with a receptor occupancy rate of 60% at 10 nM, confirming GR-mediated biological effects[2] - In vitro leukocyte migration assay, Betamethasone Valerate (BV; BET) (0.5-5 μM) dose-dependently inhibited inflammatory cell chemotaxis. At 2 μM, it reduced leukocyte migration by 55% compared to vehicle, suppressing the early stage of inflammatory response[4] |
| ln Vivo |
When applied to the inflamed region using a microspatula, bebemethasone valerate (10 mg) ointment for five minutes controls approximately fifty percent of the ear edema without causing thymus atrophy[4]. Ointment containing 50 mg of betamethasone-17-valerate reduces homologous passive cutaneous anaphylaxis [4].
In a mouse ear edema model induced by croton oil, topical application of Betamethasone Valerate (BV; BET) ointment (0.05%, 0.1%, 0.25%) dose-dependently reduced ear swelling. The 0.25% ointment decreased edema volume by 65% at 4 hours post-induction, which was comparable to the reference glucocorticoid ointment[4] - In clinical trials for inflammatory skin diseases, topical Betamethasone Valerate (BV; BET) (0.1% ointment) twice daily for 2 weeks reduced erythema, induration, and pruritus scores by 50-70% in patients with contact dermatitis. No significant systemic absorption was detected (plasma concentration <0.1 ng/mL)[3] |
| Enzyme Assay |
Glucocorticoid Receptor (GR) binding assay: Normal human epidermis was homogenized to prepare cytosolic extracts. Betamethasone Valerate (BV; BET) (1 nM, 10 nM, 100 nM) was incubated with the extracts and [3H]-labeled cortisol (competitive ligand) at 4°C for 18 hours. Bound and free ligands were separated by charcoal adsorption, and radioactivity was quantified to assess GR binding specificity and occupancy rate[2]
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| Cell Assay |
Oral mucosal epithelial cell assay: Human oral mucosal epithelial cells were seeded in 24-well plates and treated with Betamethasone Valerate (BV; BET) (0.05 μM, 0.1 μM, 1 μM) released from chitosan/PVP membranes for 48 hours. Cell viability was measured by MTT assay. Culture supernatants were collected for ELISA detection of IL-6 and TNF-α secretion[1]
- Leukocyte migration assay: Peripheral blood leukocytes were isolated and suspended in culture medium. Betamethasone Valerate (BV; BET) (0.5 μM, 2 μM, 5 μM) was added to the upper chamber of transwell inserts, and a chemoattractant was added to the lower chamber. After 2 hours of incubation, migrated leukocytes in the lower chamber were counted to evaluate migration inhibition[4] |
| Animal Protocol |
Animal/Disease Models: Female SD (Sprague-Dawley) rats weighing 60-70 g (croton oil edema experiment)[4]
Doses: 10 mg Route of Administration: Applied to the irritated site with a micro spatula; 5 minutes Experimental Results: Inhibited about 50% of the ear edema without thymus atrophy. Mouse ear edema model: Male BALB/c mice (20-25 g) were randomly grouped. Betamethasone Valerate (BV; BET) ointment (0.05%, 0.1%, 0.25%) was topically applied to the right ear (20 μL/ear) 30 minutes before croton oil (1% in acetone) induction. The left ear was treated with vehicle as control. Four hours after induction, ear thickness was measured with a micrometer to calculate edema rate[4] - Topical anti-inflammatory evaluation model: Rats with dermatitis induced by DNCB (dinitrochlorobenzene) were treated with Betamethasone Valerate (BV; BET) ointment (0.1%) topically twice daily for 7 days. Skin lesions were scored for erythema, edema, and scaling, and skin biopsies were collected to assess inflammatory cell infiltration[3] |
| ADME/Pharmacokinetics |
Absorption: Systemic absorption is minimal after local administration (the dose detected in plasma is <0.5%). Mucosal administration via chitosan/PVP membrane enhances local absorption in the oral mucosa, with a local bioavailability of approximately 45% [1][3]
- Release kinetics: Betamethasone valerate (BV; BET) released from the chitosan/PVP membrane exhibits a biphasic release pattern in simulated saliva—rapid release in the initial phase (30% release within 2 hours), followed by sustained release (85% cumulative release within 24 hours) [1] - Distribution: After local or mucosal administration, it is mainly distributed in local tissues (skin, oral mucosa), with no significant systemic distribution [3] |
| Toxicity/Toxicokinetics |
Local toxicity: Topical application may cause mild skin irritation (occurrence rate of about 5%), including transient erythema, which resolves spontaneously. Mucosal administration via chitosan/PVP membrane does not cause mucosal irritation or ulceration of oral mucosal epithelial cells [1][3]
- Cytotoxicity: At concentrations up to 5 μM, betamethasone valerate (BV; BET) showed no significant cytotoxicity to oral mucosal epithelial cells (cell viability >85%) [1] - Systemic toxicity: No significant changes in liver and kidney function indicators or hematological parameters were observed after long-term local application in animal models [3] |
| References | |
| Additional Infomation |
Betamethasone valerate is a steroidal ester, the product of the conversion of the 17α-hydroxy group of betamethasone to its corresponding valerate ester. It is an anti-inflammatory drug. It is a steroidal ester, 20-oxosteroid, 21-hydroxysteroid, 11β-hydroxysteroid, fluorosteroid, 3-oxo-Δ⁹,Δ⁴-steroid, and primary α-hydroxy ketone. Its function is related to betamethasone. Betamethasone valerate is the 17-valerate ester of betamethasone, a synthetic glucocorticoid with metabolic, immunosuppressive, and anti-inflammatory effects. Betamethasone valerate binds to specific intracellular glucocorticoid receptors, subsequently binding to DNA, thereby regulating gene expression. The synthesis of certain anti-inflammatory proteins is induced, while the synthesis of certain inflammatory mediators is inhibited. Therefore, chronic inflammation and autoimmune responses are generally reduced. It is a 17-valerate ester derivative of betamethasone. It has significant local anti-inflammatory activity and relatively low systemic anti-inflammatory activity. See also: betamethasone (containing active fraction); betamethasone valerate; gentamicin sulfate (component)... See more...
Betamethasone valerate (BV; BET) is a synthetic topical glucocorticoid with potent anti-inflammatory and immunosuppressive effects [3][4] - Its core mechanism involves specific binding to glucocorticoid receptors (GR) in target tissues (skin, oral mucosa), regulating the transcription of anti-inflammatory genes and inhibiting pro-inflammatory mediators (IL-6, TNF-α) [2][4] - Clinical indications include recurrent aphthous ulcers (mucosal preparation) and inflammatory skin diseases (eczema, contact dermatitis) (ointment preparation) [1][3] - It is formulated as an ointment or mucosal adhesive film for local administration to minimize systemic absorption and reduce systemic side effects [1][3] - Compared with other topical glucocorticoids, it has strong local anti-inflammatory efficacy and low local side effects. Because of its low irritation, it is suitable for long-term local treatment of mild to moderate inflammation [3][4] |
| Molecular Formula |
C27H37FO6
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| Molecular Weight |
476.58
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| Exact Mass |
476.257
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| CAS # |
2152-44-5
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| Related CAS # |
Betamethasone;378-44-9;Betamethasone hydrochloride;956901-32-9
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| PubChem CID |
16533
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
598.9±50.0 °C at 760 mmHg
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| Melting Point |
183-184ºC
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| Flash Point |
316.0±30.1 °C
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| Vapour Pressure |
0.0±3.8 mmHg at 25°C
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| Index of Refraction |
1.560
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| LogP |
3.78
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
34
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| Complexity |
957
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| Defined Atom Stereocenter Count |
8
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| SMILES |
CCCCC(=O)O[C@@]1([C@H](C[C@@H]2[C@@]1(C[C@@H]([C@]3([C@H]2CCC4=CC(=O)C=C[C@@]43C)F)O)C)C)C(=O)CO
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| InChi Key |
SNHRLVCMMWUAJD-SUYDQAKGSA-N
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| InChi Code |
InChI=1S/C27H37FO6/c1-5-6-7-23(33)34-27(22(32)15-29)16(2)12-20-19-9-8-17-13-18(30)10-11-24(17,3)26(19,28)21(31)14-25(20,27)4/h10-11,13,16,19-21,29,31H,5-9,12,14-15H2,1-4H3/t16-,19-,20-,21-,24-,25-,26-,27-/m0/s1
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| Chemical Name |
(8S,9R,10S,11S,13S,14S,16S,17R)-9-fluoro-11-hydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl pentanoate
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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 (5.25 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 (5.25 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.25 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0983 mL | 10.4914 mL | 20.9828 mL | |
| 5 mM | 0.4197 mL | 2.0983 mL | 4.1966 mL | |
| 10 mM | 0.2098 mL | 1.0491 mL | 2.0983 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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