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S1765450

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Synonym(s):
16,17-Butylidenebis(oxy)-11,21-dihydroxypregna-1,4-diene-3,20-dione

CAS NO.:

Empirical Formula: C25H34O6

Molecular Weight: 430.53

MDL number: MFCD00083259

EINECS: 257-139-7

Pack Size Price Stock Quantity
500G RMB1041.14 In Stock
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Update time: 2022-07-08

PRODUCT Properties

Melting point: 221-232°C (dec.)
Boiling point: 464.79°C (rough estimate)
alpha  D25 +98.9° (c = 0.28 in methylene chloride)
Density  1.1046 (rough estimate)
refractive index  1.4593 (estimate)
storage temp.  Store at RT
solubility  Practically insoluble in water, freely soluble in methylene chloride, sparingly soluble in ethanol (96 per cent).
form  powder
pka 12.87±0.10(Predicted)
color  White to Off-White
Water Solubility  21.53mg/L(temperature not stated)
Merck  14,1468
BCS Class 2
InChIKey VOVIALXJUBGFJZ-KWVAZRHASA-N
CAS DataBase Reference 51333-22-3(CAS DataBase Reference)

Description and Uses

Budesonide is composed of a 1:1 mixture of epimers of the 16,17-butylacetal, creating a chiral center. The 22R-epimer binds to the GR with higher affinity than does the 22S-epimer (Table 33.5). The butyl acetal chain provided the highest potency for the homologous acetal chains. Its rate of topical uptake into epithelial tissue is more than 100 times faster than that for hydrocortisone and dexamethasone. Approximately 85% of the IV administered dose of budesonide undergoes extensive first-pass hepatic metabolism by CYP3A4 to its primary metabolites, 6β-hydroxybudesonide and 16α-hydroxyprednisolone, which have approximately 1/100 the potency of budesonide. This is an important inactivation step in limiting budesonide's systemic effect on adrenal suppression.

The oral capsule is used for the treatment of mild to moderate active Crohn's disease. The oral tablet is used for induction of remission in patients with active, mild to moderate ulcerative colitis. The oral inhalation formulation is used for the treatme

Safety

Symbol(GHS) 
GHS08,GHS07
Signal word  Danger
Hazard statements  H361-H332-H317-H334-H312
Precautionary statements  P261-P272-P280-P302+P352-P333+P313-P321-P363-P501-P201-P202-P281-P308+P313-P405-P501-P261-P271-P304+P340-P312-P280-P302+P352-P312-P322-P363-P501-P261-P285-P304+P341-P342+P311-P501
Hazard Codes  Xn
Risk Statements  40-36/37/38-20/21/22
Safety Statements  22-36-26
WGK Germany  3
RTECS  TU3723000
HS Code  29372900
Hazardous Substances Data 51333-22-3(Hazardous Substances Data)
Toxicity LD50 oral in rat: > 3200mg/kg

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