Description Chemical Properties Application Adverse effects Precautions Drug interactions Preparation References
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Deflazacort

Description Chemical Properties Application Adverse effects Precautions Drug interactions Preparation References
Product Name
Deflazacort
CAS No.
14484-47-0
Chemical Name
Deflazacort
Synonyms
oxaz;deflan;Cortax;l-5458;calcort;azacort;MDL 458;Dezacor;Azaeort;Caltort
CBNumber
CB8705963
Molecular Formula
C25H31NO6
Formula Weight
441.52
MOL File
14484-47-0.mol
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Deflazacort Property

Melting point:
255-256.5°C
alpha 
D +62.3° (c = 0.5 in chloroform)
Boiling point:
595.4±50.0 °C(Predicted)
Density 
1.41
storage temp. 
2-8°C
solubility 
DMSO: ≥20mg/mL
pka
14.30±0.70(Predicted)
form 
powder
color 
white to tan
Merck 
14,2862
InChIKey
FBHSPRKOSMHSIF-UBRVQRTASA-N
SMILES
C12(C(COC(C)=O)=O)[C@]3(C)C(C4C([C@H](C3)O)[C@]3(C)C(=CC(C=C3)=O)CC4)CC1OC(C)=N2
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Safety

Safety Statements 
24/25
WGK Germany 
3
RTECS 
TU4157050
HS Code 
29349990
Toxicity
LD50 orally in mice: 5200 mg/kg (Schiatti)
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H360May damage fertility or the unborn child

H373May cause damage to organs through prolonged or repeated exposure

Precautionary statements

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P314Get medical advice/attention if you feel unwell.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML0123
Product name
Deflazacort
Purity
≥98% (HPLC)
Packaging
10mg
Price
$138
Updated
2024/03/01
Sigma-Aldrich
Product number
1166116
Product name
Deflazacort
Purity
United States Pharmacopeia (USP) Reference Standard
Packaging
100mg
Price
$436
Updated
2024/03/01
TCI Chemical
Product number
D4523
Product name
Deflazacort
Purity
>98.0%(HPLC)(N)
Packaging
1g
Price
$234
Updated
2024/03/01
TCI Chemical
Product number
D4523
Product name
Deflazacort
Purity
>98.0%(HPLC)(N)
Packaging
5g
Price
$697
Updated
2024/03/01
Cayman Chemical
Product number
20386
Product name
Deflazacort
Purity
≥98%
Packaging
25mg
Price
$32
Updated
2024/03/01
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Deflazacort Chemical Properties,Usage,Production

Description

Deflazacort (trade name Emflaza among others) is a glucocorticoid used as an anti-inflammatory and immunosuppressant. It belongs to a group of medicines called corticosteroids. It is sometimes referred to simply as an oral steroid.
Deflazacort is an inactive prodrug which is metabolized rapidly to the active drug 21-desacetyldeflazacort.It is used to treat a wide variety of conditions. Some examples include autoimmune diseases (for example, systemic lupus erythematosus (SLE), autoimmune hepatitis, sarcoidosis), joint and muscle diseases (for example, rheumatoid arthritis), and allergies and asthma.
Cardiff can be specially designed for the third generation of corticosteroids, anti-inflammatory, anti-allergy, and it increased gluconeogenesis and so on. It acts as prednisolone 10~20 times of the dragon, 40 times as hydrocortisone. This product has no mutagenic effect. This product, labeled with C14 study, shows that the product of the gastrointestinal tract rapidly absorbed, reaching the peak blood concentration after 1~2h, forming the active substance by hydrolysis, and the latter further metabolic processes is similar with other corticosteroids, as well as the active metabolite T1/2 is 2 h and the rats are mainly distributed in the kidney and hematopoietic system and other organizations.

Figure 1 is a deflazacort formula.

Chemical Properties

Acetone-hexane, m.p. 255-256.5 ℃. [Α] D + 62.3 ° (C = 0.5, chloroform). UV absorption maximum (methanol): 241~242nm (E1cm1% 352.5). Acute toxicity LD50 in mice (mg/kg): 5200 oral; 1610 subcutaneous injection. Rats Acute toxicity LD50 (mg/kg): 109 subcutaneously. Dog Acute toxicity LD50 (mg/kg):> 4000 Oral; 50 subcutaneous injection.

Application

 The third generation of corticosteroids, anti-inflammatory, anti-allergy, increased gluconeogenesis and so on. For the use of the primary and secondary adrenocortical insufficiency, rheumatism, collagen diseases, skin diseases, allergic diseases, eye diseases, and fulminant disseminated tuberculosis, hematopoietic system disorders, ulcerative colitis, idiopathic nephrotic syndrome, and other hematopoietic malignancies.

Adverse effects

Deflazacort carries the risks common to all corticosteroids, including immune suppression, decreased bone density, and endocrine insufficiency. In clinical trials, the most common side effects (>10% above placebo) were Cushing's-like appearance, weight gain, and
increased appetite.
Long-term medication can affect the normal growth of children, induced peptic ulcer perforation, which can cause euphoria, depression, insomnia and other psychiatric symptoms. Sudden withdrawal after long-term use can cause secondary adrenal insufficiency withdrawal reactions, which should gradually decrease until disabled.

Precautions

  • Like other glucocorticoids, it is general contraindicated in systemic infections.
  • Used with caution in diverticulitis, recent gastrointestinal surgery, renal failure, hypertension, diabetes, osteoporosis, myasthenia gravis embolism. Pregnancy and lactation women should used with caution.

Drug interactions

  • Cardiff may have unique row potassium, and it should pay more attention when combined with diuretics.
  • When combined with the drug having enzymatic action (rifampicin, phenobarbital, etc.), the corticosteroids should be properly increment.
  • Erythromycin, estrogen can inhibit the activity of this product and the metabolism, when combined with appropriate reductions.

Preparation

Compound 10g (1) was dissolved in 350ml methanol, and then added 8.3g of semicarbazide hydrochloride and 5.75ml of pyridine in 50ml of water, after the reaction. We can obtain compound 11g (Ⅱ). Compound 9g (Ⅱ) was dissolved 230ml 95% ethanol, the solution was added 3.6g of potassium carbonate and 2.34g of sodium borohydride in 36ml of water, which was refluxed for 30min and then added 2.34g of sodium borohydride. After the reaction, we can obtain compound 8.5g (Ⅲ). Compound 7.7g (Ⅲ) was dissolved in 154ml 10% hydrochloric acid in methanol, refluxed for 1h, to give Compound 6g (Ⅳ). Compound 12.5g (Ⅳ) was dissolved in 500ml of anhydrous toluene and 90ml of cyclohexanone. It was added 6.24g triisopropyl aluminum, 9g obtained by reacting the compound (V). 6.5g compound (V) was dissolved in 123ml dry dioxane, and 25% hydrogen bromide in acetic acid solution is heated, and then added 5.5g of bromine in dioxane; the reaction solution was poured into the water, collected by filtration after the crystals were carefully dried, redissolved in dimethylformamide. It  was added 7.5g of lithium bromide and lithium carbonate (1: 2) mixture. After heating the reaction, we can obtain the compound 5.1g (ⅵ). 2g compound (Ⅵ) was dissolved in tetrahydrofuran-methanol (1: 1), added to 3.9g calcium oxide and 0.1g of azobisisobutyronitrile. It was added 2g of iodine in tetrahydrofuran-methanol mixture; After the reaction was filtered off precipitate , which was dissolved in acetone,  it was then added triethylamine 20ml, 20ml and 12ml acetone, acetic acid, atter the reaction, we can obtain 1.6g deflazacort.

References

https://en.wikipedia.org/wiki/Deflazacort
http://patient.info/medicine/deflazacort-tablets-calcort

Description

Deflazacort is an antiinflammatory treatment of rheumatoid arthritis. Its antirheumatic potency i s similar to that of prednisone, while its hyperglycernic and calcium depleting effects are reportedly less.

Chemical Properties

Off-White to Pale Yellow Solid

Originator

Dow Lepetit (Italy)

Uses

Deflazacort-d3, is the labeled analogue of Deflazacort (D228975), a systemic corticosteroid, and a derivative of prednisolone. Used for rheumatoid arthritis and lupus.

Uses

antiinflammatory

Uses

A systemic corticosteroid. A derivative of prednisolone. Used for rheumatoid arthritis and lupus

Definition

ChEBI: Deflazacort is a corticosteroid hormone.

brand name

LANTADIN; DEFLAN

Biochem/physiol Actions

Deflazacort is an anti-inflammatory and immunosuppressant glucocorticoid.

Clinical Use

Glucocorticoid:
Suppression of inflammatory and allergic disorders

Drug interactions

Potentially hazardous interactions with other drugs
Aldesleukin: avoid concomitant use
Antibacterials: metabolism accelerated by rifamycins; metabolism possibly inhibited by erythromycin; concentration of isoniazid possibly reduced.
Anticoagulants: efficacy of coumarins and phenindione may be altered.
Antiepileptics: metabolism accelerated by carbamazepine, fosphenytoin, phenobarbital, phenytoin and primidone
Antifungals: increased risk of hypokalaemia with amphotericin - avoid; metabolism possibly inhibited by itraconazole and ketoconazole
Antivirals: concentration possibly increased by ritonavir.
Ciclosporin: rare reports of convulsions in patients on ciclosporin and high-dose corticosteroids; increased half-life of deflazacort.
Cobicistat: concentration increased by cobicistat - avoid.
Diuretics: enhanced hypokalaemic effects of acetazolamide, loop diuretics and thiazide diuretics.
Vaccines: high dose corticosteroids can impair immune response to vaccines; avoid with live vaccines.

Metabolism

Deflazacort is immediately converted by plasma esterases to the pharmacologically active metabolite (D 21-OH). It is 40% protein-bound and has no affinity for corticosteroid-binding-globulin (transcortin). Elimination takes place primarily through the kidneys; 70% of the administered dose is excreted in the urine. The remaining 30% is eliminated in the faeces. Metabolism of D 21-OH is extensive; only 18% of urinary excretion represents D 21-OH. The metabolite of D 21-OH, deflazacort 6-beta-OH, represents one third of the urinary elimination.

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Deflazacort Suppliers

Hunan Jiuwei Biopharmaceutical Co., Ltd
Tel
19176660800
Email
alexybw@hnjwpharma.com
Country
China
ProdList
23
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58
Wuhan Yuqing Jiaheng Pharmaceutical Co., Ltd
Tel
18207128853 18207128853
Email
3860188266@qq.com
Country
China
ProdList
915
Advantage
58
Xuzhou Maikai Biotechnology Co., Ltd.
Tel
13921770081
Email
SVP01@magicbiotech.cn
Country
China
ProdList
511
Advantage
58
Shanghai Boyle Chemical Co., Ltd.
Tel
021-50182298 021-50180596
Fax
+86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2208
Advantage
55
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6005
Advantage
61
TAIYUAN RHF CO.,LTD.
Tel
+86 351 7031519
Fax
+86 351 7031519
Email
sales@RHFChem.com
Country
China
ProdList
2338
Advantage
56
Pure Chemistry Scientific Inc.
Tel
001-857-928-2050 or 1-888-588-9418
Fax
001-617-206-9595
Email
sales@chemreagents.com
Country
United States
ProdList
10186
Advantage
62
LGM Pharma
Tel
1-(800)-881-8210
Fax
615-250-9817
Email
inquiries@lgmpharma.com
Country
United States
ProdList
2123
Advantage
70
Chemsky(shanghai)International Co.,Ltd.
Tel
021-50135380
Email
shchemsky@sina.com
Country
China
ProdList
32321
Advantage
50
Nanjing MeiBo Biological Technology Co., Ltd.
Tel
025-58619198
Fax
025-58619197
Email
sales@mbbio.com
Country
China
ProdList
319
Advantage
60
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View Lastest Price from Deflazacort manufacturers

WUHAN FORTUNA CHEMICAL CO., LTD
Product
Deflazacort 14484-47-0
Price
US $0.00/Kg/Bag
Min. Order
1KG
Purity
97%-102%
Supply Ability
100KGS
Release date
2021-06-10
Hangzhou Hyper Chemicals Limited
Product
Deflazacort 14484-47-0
Price
US $0.00-0.00/KG
Min. Order
1KG
Purity
99%, USP
Supply Ability
1,000KG
Release date
2024-05-22
Wuhan Senwayer Century Chemical Co.,Ltd
Product
Deflazacort 14484-47-0
Price
US $1840.00/kg
Min. Order
0.1kg
Purity
99% HPLC
Supply Ability
20 tons
Release date
2022-10-21

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