5630-53-5 Usage
Description
Tibolone is a synthetic steroid with weak progestational and estrogenic properties,
reportedly useful in controlling symptoms resulting from natural or surgical menopause.
It has thus far shown no significant antithrombotic effect in post-menopausal patients.
Chemical Properties
White Solid
Originator
Akzo (Organon) (The Netherklands)
Uses
A synthetic steroid with weak estrogenic, androgenic and progestogenic activity. A pharamceutical used in the treatment of menopausal syndrome
Definition
ChEBI: Estran-3-one with a double bond between positions 5 and 10, and bearing both an ethynyl group and a hydroxy group at position 17 (R-configuration). A synthetic steroid hormone drug which acts as an agonist at all five type I steroid hormon
receptors, it is used in the prevention of postmenopausal osteoporosis and for treatment of endometriosis.
Brand name
Livial
Pharmacokinetics
Raloxifene is rapidly absorbed following oral administration, with an estimated 60% absorption, but it has a
very low bioavailability (2%), associated with extensive phase II metabolism. The metabolites are excreted via
the bile, with potential enterohepatic recycling that could account for the interaction with cholestyramine.
Supportive of the enterohepatic recycling is the half-life of 28 hours. Metabolism of raloxifene occurs to a great
extent in the intestine and consists of glucuronide conjugation catalyzed by uridine diphosphate
glucuronosyltransferase (UGT).
Clinical Use
Tibolone is a synthetic steroid that has been shown to increase bone mineral density similar to
alendronate. The U.S. FDA approval is pending; overseas, this agent is used for the treatment of
menopausal symptoms as well as the prevention of osteoporosis. It is considered to be a viable
alternative to conjugated equine estrogen plus micronized progesterone.
Side effects
The most common reason for
patient withdrawal from clinical trials was vaginal bleeding (also a common side effect when estrogen
therapy is used).
Check Digit Verification of cas no
The CAS Registry Mumber 5630-53-5 includes 7 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 4 digits, 5,6,3 and 0 respectively; the second part has 2 digits, 5 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 5630-53:
(6*5)+(5*6)+(4*3)+(3*0)+(2*5)+(1*3)=85
85 % 10 = 5
So 5630-53-5 is a valid CAS Registry Number.
InChI:InChI=1/C21H28O2/c1-4-21(23)10-8-18-19-13(2)11-14-12-15(22)5-6-16(14)17(19)7-9-20(18,21)3/h1,13,17-19,23H,5-12H2,2-3H3/t13-,17-,18+,19-,20+,21+/m1/s1
5630-53-5Relevant articles and documents
Preparation method of tibolone
-
, (2020/11/25)
The invention discloses a preparation method of tibolone, and belongs to the technical field of preparation and processing of steroid hormone drugs. According to the method, 6,7-didehydronorethindroneis used as an initial raw material, and tibolone is prepared through Grignard reaction, dietherification reaction and hydrolysis reaction. The 7-methyl introduction step is included in the Grignard reaction step in the synthesis route, so that special protection on 17-site hydroxyl is avoided, and the ratio of the 7-alpha methyl intermediate to the 7-beta methyl isomer obtained through the reaction is larger than 20:1; therefore, the single 7-alpha methyl intermediate can be obtained through simple treatment without chromatographic separation, the purification process is simple, and the purity of the final product reaches 99.0% or above, and the yield is higher than 60%; the raw materials are cheap and easily available, the reaction steps are few, the reaction conditions are mild and safe, and the control operation is easy; in addition, reagents used in the reaction are low in environmental pollution, and good economic and social benefits are achieved.
FLUORESCENCE BASED DETECTION OF SUBSTANCES
-
, (2009/09/28)
A method for the fluorescent detection of a substance, the method comprising providing particles comprising a metal or a metal oxide core, wherein one or more optionally fluorescently tagged antibodies or human specific peptide nucleic acid (PNA) oligomers for binding to a substance is/are bound, directly or indirectly, to the surface of the metal or metal oxide; contacting a substrate, which may or may not have the substance on its surface, with the particles for a time sufficient to allow the antibody/PNA oligomer to bind with the substance; removing those particles which have not bound to the substrate; if the antibodies or PNA oligomers are not fluorescently tagged, contacting the substrate with one or more fluorophores that selectively bind with the antibody and/or substance, then optionally washing the substrate to remove unbound fluorophores; and illuminating the substrate with appropriate radiation to show the fluorophores on the substrate.
PROCESS FOR THE PRODUCTION OF TIBOLONE
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Page 41, (2010/02/08)
Disclosed is a process for the synthesis of 17β-hydroxy-7α-methyl- 19-nor-17α-pregn-5(10)-ene-20-yne-3-one (tibolone, 11) and intermediates useful for the synthesis thereof: (11).
