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Raloxifene powder, Raloxifen, chemical formula C28H27NO4S, CAS 84449-90-1, molecular weight 473.6 g/mole. The molecular structure contains a benzothiophene ring and a benzene ring, which are connected together by a ketone group. A white to light yellow crystalline powder. It is almost insoluble in water, but soluble in organic solvents such as ethanol, dichloromethane, and ethyl acetate. Its solubility in water is relatively low, approximately 0.0002 mg/mL. However, its solubility is high in organic solvents, such as in ethanol, which can reach 0.8 mg/mL. It has moderate fat solubility and a n-hexane/water partition coefficient (logP value) of approximately 3.3. The crystal structure has been determined by X-ray diffraction technology. According to relevant literature, the crystal of Raloxifen belongs to the monoclinic system and has specific lattice parameters and spatial groups. It is a drug with selective estrogen receptor modulator (SERM) effects. Mainly used in clinical treatment of postmenopausal osteoporosis in women.
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Chemical Formula |
C28H27NO4S |
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Exact Mass |
473 |
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Molecular Weight |
473 |
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m/z |
473 (100.0%), 474 (30.3%), 475 (4.5%), 475 (2.7%), 475 (1.7%), 476 (1.4%) |
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Elemental Analysis |
C, 71.01; H, 5.75; N, 2.96; O, 13.51; S, 6.77 |
Melting point 250-253 ° C, Boiling point 728.2 ± 60.0 ° C (predicted), Density 1.289 ± 0.06 g / cm3 (predicted), Storage condition desicate at + 4 ° C, Solubility DMSO: 28 mg / ml, soluble, Acidity coefficient (PKA) 8.83 ± 0.15 (predicted), Form solid, Color light yellow
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Raloxifene, as a selective estrogen receptor modulator (SERM), has become a core drug for the treatment of osteoporosis in postmenopausal women since its launch in the 1990s. It exerts a dual regulatory effect in target organs such as bone, cardiovascular, breast, and uterus through tissue-specific mechanisms, retaining the bone protective effect of estrogen while avoiding reproductive system risks.
The core indication of raloxifene is to prevent and treat osteoporosis in postmenopausal women, especially for those at high risk of fractures. Global multicenter studies have shown that a daily dose of 60mg can significantly reduce the incidence of vertebral fractures by 30% -50%, but the preventive effect on hip fractures is not yet clear. Its mechanism of action is achieved by inhibiting bone resorption:
Bone metabolism regulation: Raloxifene binds to estrogen receptors on the surface of bone cells, activating osteoblast activity while inhibiting osteoclast differentiation, resulting in a decrease in bone turnover markers (such as β - CTX) levels to the premenopausal range.
Bone density improvement: After 2 years of treatment, the average bone density of the lumbar spine increased by 2.6%, and the hip bone density increased by 1.6%, which is comparable to the effect of bisphosphonates.
Fracture risk stratification: For patients with FRAX scores ≥ 3% or a history of vertebral fractures, raloxifene can reduce the risk of recurrent fractures, but it needs to be combined with calcium supplements (1000-1200mg per day) and vitamin D (800IU per day) to optimize efficacy.
Raloxifene powder exhibits excitatory or antagonistic effects in different tissues by binding to estrogen receptor (ER) alpha and beta subtypes, forming unique pharmacological features:
Skeletal system: It exhibits potent estrogenic effects in bone tissue, activating the ER α pathway, promoting bone formation, and inhibiting bone resorption. Animal experiments have shown that its bone protective effect is 60% stronger than estrogen, but there is no risk of uterine hyperplasia.
Cardiovascular system: Through ER β - mediated lipid metabolism regulation, it reduces total cholesterol (TC) by 5% -10% and low-density lipoprotein cholesterol (LDL-C) by 10% -15%, while not altering high-density lipoprotein cholesterol (HDL-C) and triglyceride levels. A large-scale randomized controlled trial (MORE study) has confirmed that it can reduce the risk of coronary heart disease events by 35%.
Breast and uterus: in breast tissue, it shows ER antagonism, inhibits estrogen induced cell proliferation, and reduces the risk of breast cancer by 76%. There is no stimulating effect on the endometrium, and there is no significant change in endometrial thickness before and after treatment, avoiding the bleeding risk of hormone replacement therapy (HRT).
Risk of venous thrombosis: It is important to be aware that the risk of deep vein thrombosis (DVT) and pulmonary embolism (PE) increases by 2-3 times, especially during the first 4 months of treatment when the risk is highest. It is recommended to discontinue use in patients with a history of venous thromboembolism (VTE), immobilization status, or hypercoagulability.
MORE study (Multiple Outcomes of breast cancer Evaluation): 7705 postmenopausal women were included. Follow up for 4 years showed that the risk of vertebral fracture in the raloxifene group was reduced by 30%, the risk of breast cancer was reduced by 76%, and the risk of endometrial cancer was not increased. But the incidence of hot flashes increased by 10% compared to the placebo group.
The CORE study (Continuing Outcomes Relevant to Evista): Extended follow-up to 8 years confirmed the sustained preventive effect of raloxifene on non vertebral fractures and a 35% reduction in cardiovascular event risk.
Real world data: Analysis of the US healthcare database shows that treatment compliance with raloxifene is 68%, higher than that of bisphosphonates (52%), mainly due to daily single dose administration and fewer gastrointestinal side effects. However, it should be noted that its anti fracture effect is weaker than that of denosumab in patients with severe osteoporosis (T value ≤ -3.5).
This is our advanced product raloxifene powder
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Raloxifen is an anti estrogen drug that can be synthesized by reacting Raloxifen hydrochloride with other reagents. The following is the synthesis process of raloxifene and its corresponding chemical equation:
1) React para bromobenzoic acid with ethyl acrylate under alkaline conditions to produce ethyl propylene para bromobenzoic acid ester.
C6H5CH2COOH+CH2=CHCOOC2H5 → C6H5CH2COOCH2CHO(CH3)C2H5
2) The reaction of ethylpropenyl p-bromobenzoate with hydrocyanic acid generates corresponding nitrile compounds.
C6H5CH2COOCH2CH(CH3)C2H5+HCN → C6H5CH2C(CN)(COOCH2CH(CH3)C2H5)
3) React nitrile compounds with water and sulfuric acid to produce amino acids.
C6H5CH2C(CN)(COOCH2CH(CH3)C2H5) +2H2O+H2SO4 → C6H5CH2CH(NH2)COOH+CO2+(CH3)2CHOH
4) Finally, the amino acids are reacted with hydrochloric acid to produce raloxifene hydrochloride.
C6H5CH2CH(NH2)COOH+HCl → C6H5CH2CH(NH3)ClCOOH
Raloxifene synthesis method of raloxifen :
(1)
2-(4-hydroxyphenyl ) benzo [b] thiophene-6-ol was esterified by methylsulfonyl chloride, and the resulting diester reacted with 4-(2-piperidinylethoxy ) benzoyl chloride to obtain raloxifen by hydrolysis.
(2)
Using 3-methoxyphenylthiophenol and 4-methoxy-α-bromoacetophenone as starting materials, 6-methoxy-2-(4-acetyloxyphenyl ) benzo [b] thiophene was obtained through substitution reaction and cyclization reaction.
(3)
Friedel-Crafts reaction was carried out with 4-[2-(1-piperidinyl)ethoxy ] benzoyl chloride, followed by demethylation reaction.
(4)
The target product was obtained through salt formation reaction in five main steps.
(5)
Results : The structure of the target compound was confirmed by IR, 1H NMR and MS.
Conclusion : This method has mild reaction conditions, simple operation, and improved yield. Raloxifene is a benzothiophene selective estrogen receptor modulator (SERM), which has estrogen agonistic effects on bone and blood lipids, and has estrogen antagonistic effects on breast and uterus. Raloxifene is used in breast cancer and osteoporosis research.
Raloxifen powder is a selective estrogen receptor modulator (SERM) primarily used for the prevention and treatment of osteoporosis. The following is the research and development history of Raloxifen:
Early research:
Raloxifen's research was initially conducted by Eli Lilly and Company in the United States. They hope to develop a drug that can replace traditional estrogen therapy, providing the benefits of increased bone density while reducing adverse effects on the breast and uterus.
Clinical trial:
In early clinical trials, researchers found that Raloxifene has the effect of protecting bones and can reduce the risk of breast cancer. In addition, compared to traditional estrogen therapy, Raloxifene also showed fewer adverse side effects, such as breast hyperplasia and endometrial hyperplasia.
Approval for listing:
Based on clinical trial results, Raloxifene obtained approval from the US Food and Drug Administration (FDA) in 1997 for the prevention and treatment of osteoporosis. It has also been approved by other countries and regions as an important therapeutic drug.
Further research:
Over time, the research focus of Raloxifen has further expanded, exploring its potential applications in other fields. For example, researchers have found that Raloxifene also has certain effects in the treatment of breast cancer, and are conducting research on its combined use with other drugs.
Overall, the research and development history of raloxifene powder has gone through a process from early testing to approval for market launch. As a SERM, it plays an important role in the treatment of osteoporosis and continues to be explored and applied in research on other diseases. In the process of this research and development history, safer and more effective alternative treatment options have been brought, providing more benefits for patients.
Frequently Asked Questions
Is it an "actor" or an "audience" in bone cells? Why is it completely different from ibuprofen?
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Inside bone cells, it is the true 'audience' rather than the 'actor'. After binding to estrogen receptors, it does not activate the classical estrogen response element (ERE), but instead inhibits the activity of other agonists such as estradiol. This is completely different from Idoxifene, which is a potent agonist of ERE in bone cells. Although both are SERMs that ultimately protect bones, their performance styles are vastly different.
What is its powder afraid of? How harsh are the storage conditions?
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It's actually quite sturdy. The raw material powder can be stored in the dark at -20 ° C during drying, and its stability can last up to 3 years. Once prepared into a solution, it must be stored at -20 ° C and used within one month. Repeated freeze-thaw cycles can lead to a decrease in potency. It is almost insoluble in water, but has excellent solubility in DMSO (>90 mg/mL), making it a commonly used solvent for in vitro experiments.
How does it achieve "selectivity"? Which two keys are relied upon?
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It relies on the switch of AF-1 and AF-2 domains. In breast and uterine cells, it binds to receptors and blocks key AF-2 functions, causing gene transcription to 'silence'; In bone cells and liver, it allows AF-1 to be activated, activating the expression of some beneficial genes. The conformational changes that this organization relies on are the molecular basis for its selectivity.
Over 90% of it stays in the bloodstream, who is the best 'travel companion'?
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It binds to over 95% of plasma proteins, mainly albumin, and also partially binds to alpha 1-acid glycoproteins. This means that it is basically not 'free to move'. Therefore, when used in combination with drugs with the same high protein binding rate (such as warfarin and diazepam), it may cause fluctuations in free concentration and should be carefully monitored.
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