Nα-Tosyl-PheChloromethylKetone , Irreversibleinhibitorofchymotrypsin. , 402-71-1

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

CAS NO.：402-71-1

Empirical Formula: C25H34O6

Molecular Weight: 430.53

MDL number: MFCD00083259

EINECS: 257-139-7

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