TACROLIMUS MONOHYDRATE

PRODUCT IDENTIFICATION

CAS NO. 104987-11-3 (Parent)
109581-93-3 (monohydrate)

TACROLIMUS

EINECS NO.  
FORMULA C44H69NO12·H2O
MOL WT. 822.03

H.S. CODE

 

TOXICITY

 

PRICE

 

SYNONYMS Tacrolimus hydrate;
(-)-(3S,4R,5S,8R,9E,12S,14S,15R,16S,18R,19R,26aS)-8-Allyl-5,6,8,11,12,13,14,15,16,17, 18,19,24,25,26,26a- Hexadecahydro-5,19-dihydroxy-3-((E)-2-((1R,3R,4R)-4- hydroxy-3- methoxycyclohexyl)-1- methylvinyl)- 14, 16-dimethoxy-4,10,12,18-tetramethyl- 15,19-epoxy-3H-pyrido(2,1-c)(1,4)oxaazacyclotricosine- 1,7,20,21(4H,23H)-tetrone) monohydrate; Tsukubaenolide hydrate;

CLASSIFICATION

 

PHYSICAL AND CHEMICAL PROPERTIES

PHYSICAL STATE white to off-white crystalline powder
MELTING POINT 127 - 129 C
BOILING POINT

 

RELATIVE DENSITY  
SOLUBILITY IN WATER

insoluble (soluble in ethanol, methanol, chloroform, DMSO)

pH  
VAPOR DENSITY

 

REFRACTIVE INDEX

 

NFPA RATINGS

 

AUTOIGNITION

 

FLASH POINT

 

STABILITY Stable under normal conditions.

GENERAL DESCRIPTION & APPLICATIONS

Tacrolimus (known as FK-506) is a 23-membered macrocyclic lactone compound isolated from the strain of Streptomyces tsukubaensis. It acts as an immunosuppressant in vivo and prevents the activation of both T-lymphocyte signal transduction and IL-2 transcription in response to antigenic or mitogenic stimulation in vitro. It's action is similar to that of cyclosporine to prevent rejection of organ transplants and topically to treat severe atopic dermatitis, vitiligo and to treat severe refractory uveitis after bone marrow transplants. Chemical designation is (3S-(3R',(E(1S',3S',4S')),4S',5R',8S',9E,12R',14R',15S',16R',18S',19S',26aR'))- 5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-5,19-dihydroxy-3-(2- (4-hydroxy-3- methoxycyclohexyl)-1-methylethenyl)-14,16-dimethoxy-4,10,12,18-tetramethyl-8-(2-propenyl)- 15,19-epoxy-3H-pyrido(2,1-c)(1,4)oxaazacyclotricosine-1,7,20,21(4H,23H)-tetrone monohydrate. Tacrolimus is a white crystalline powder; practically insoluble in water, soluble in ethanol, methanol, chloroform, DMSO.

SALES SPECIFICATION

APPEARANCE

white to off-white crystalline powder

ASSAY

98.0 - 102.0%

SPECIFIC ROTATION -84° ~ -85°

HEAVY METALS

10ppm max

MELTING POINT

127 - 129 C

WATER

3.0% max

TRANSPORTATION
PACKING
 
HAZARD CLASS 6.1 (Packing Group: III)
UN NO.

2811

PRICE

U$2,800 (5g)