Lasofoxifene
Lasofoxifene Basic information
- Product Name:
- Lasofoxifene
- Synonyms:
-
- Lasofoxifene Base
- Lasofoxifene
- (5R,6S)-
- CP-336,156
- (5R,6S)-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]tetralin-2-ol
- (5R,6S)-5,6,7,8-Tetrahydro-6-phenyl-5-[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-2-naphthalenol
- (5R-cis)-5,6,7,8-Tetrahydro-6-phenyl-5-[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-2-naphthalenol
- 2-Naphthalenol, 5,6,7,8-tetrahydro-6-phenyl-5-[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-, (5R,6S)-
- CAS:
- 180916-16-9
- MF:
- C28H31NO2
- MW:
- 413.55
- Product Categories:
-
- Aromatics
- Chiral Reagents
- Heterocycles
- Intermediates & Fine Chemicals
- Pharmaceuticals
- Mol File:
- 180916-16-9.mol
Lasofoxifene Chemical Properties
- Melting point:
- 110-113°C
- Boiling point:
- 572.4±50.0 °C(Predicted)
- Density
- 1.150±0.06 g/cm3(Predicted)
- storage temp.
- Refrigerator
- solubility
- Chloroform (Slightly), Methanol (Slightly)
- form
- Solid
- pka
- 10.31±0.60(Predicted)
- color
- White to Off-White
Lasofoxifene Usage And Synthesis
Chemical Properties
Off-White Solid
Uses
A next-generation selective estrogen receptor modulator for treating disorders associated with increased bone turnover and osteopenia.
Definition
ChEBI: Lasofoxifene is a member of the class of tetralins that is 5,6,7,8-tetrahydronaphthalen-2-ol in which the hydrogens at positions 5 and 6 are replaced by 4-[2-(pyrrolidin-1-yl)ethoxy]phenyl and phenyl groups, respectively (the 5R,6S-stereoisomer). It is a selective estrogen receptor modulator indicated for the prevention and treatment of osteoporosis in post-menopausal women. It has a role as an antineoplastic agent, a cardioprotective agent, an estrogen receptor agonist, an estrogen receptor antagonist and a bone density conservation agent. It is a member of tetralins, an aromatic ether, a member of naphthols and a N-alkylpyrrolidine.
Clinical Use
Lasofoxifene is a very potent second-generation SERM currently in phase III clinical trials for the treatment and prevention of osteoporosis in postmenopausal women.
in vivo
Lasofoxifene (4 mg/mice; s.c.; 5 day/week; for 43 d) decreases arthritis severity, by reducing cartilage oligomeric matrix protein (COMP), the serum marker of cartilage destruction and reducing serum IL-6 (inflammatory cytokine) levels in mice[1].
Lasofoxifene (4 mg/mice; s.c.; 5 day/week; for 43 d) protects against generalised bone loss in CIA by increasing trabecular bone mineral density (BMD), cortical thickness in mice[1].
Lasofoxifene (5, and 10 mg/kg; s.c.; 5 day/week; for 70 d) exerts function of inhibiting primary tumor growth and reducing metastases to the lung and the liver in mice[3].
| Animal Model: | Post-menopausal RA model on OVX (ovariectomised) DBA/1 mice (female DBA/1 mice, 8-10 weeks old, CIA-treated)[1] |
| Dosage: | 4 mg/mouse/day |
| Administration: | Subcutaneous injection; 5 days a week from the first signs of arthritis (day 18); 43 days |
| Result: | Reduced in arthritis severity, including synovial inflammation and destruction of joints reduction. The mean arthritis frequency was 47% while the vehicle group was 81% at 42 days post immunization. |
| Animal Model: | NSG mices with xenograft tumors model (MIND, mammary intraductal): WT, Y537S and D538G ERα render tumors[3] |
| Dosage: | 1, 5, or 10 mg/kg |
| Administration: | Subcutaneous injection; 5 days per week; for 70 days |
| Result: | Elicited a superior inhibitory effect at a dose of 10 mg/kg, resulted potential tumor shrinkage in Y537S and D538G tumors. And also reduced tumor weight to 60% for Y537S and 50% for D538G at 5 and 10 mg/kg, respectively. |
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