Eplerenone CAS 107724-20-9
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Factory Supply Eplerenone CAS 107724-20-9 with Best Price
- Appearance: White powder
- Purity: 99. 0%min
- Stock: In stock
- Sample: Available
- Zhishang Chemical: Eplerenone Supplier & Manufacturer
Eplerenone: The Complete Guide
Eplerenone for Sale
Basic Info of Eplerenone
Basic Info
Chemical Properties
Other Info
Basic Info
Chemical Name: | Eplerenone |
Other Name: | (7α,11α,17α)-9,11-Epoxy-17-hydroxy-3-oxo-pregn-4-ene-7,21-dicarboxylicacidγ-lactoneMethylester; Eplerenone cas 107724-20-9 |
CAS: | 107724-20-9 |
EINECS: | 600-850-8 |
Type: | Pharmaceuticals, pesticides, dye intermediates; Pharmaceutical raw materials |
Molecular Formula: | C24H30O6 |
Molecular Weight: | 414.49 |
Chemical Properties
Melting point | 241-243°C |
alpha | D +5° (c = 0.437 in chloroform) |
Boiling point | 597.9±50.0 °C(Predicted) |
density | 1.31±0.1 g/cm3(Predicted) |
storage temp. | Store at RT |
solubility | DMSO: soluble2mg/mL, clear (warmed) |
form | powder |
color | white to beige |
Other Info
Brand Name: | Zhishang Chemical |
Provide: | Eplerenone MSDS; Eplerenone COA |
What is Eplerenone?
Eplerenone is utilized alone or in mix with various other drugs to treat hypertension. Eplerenone comes from a course of medicines called mineralocorticoid receptor villains. It works by blocking the activity of aldosterone, an all-natural compound in the body that can elevate blood pressure.
Eplerenone, an aldosterone receptor villain similar to spironolactone, has been revealed to create continual boosts in plasma renin and product aldosterone, which is consistent with the unfavorable governing comments of hindering aldosterone on renin secretion. The resulting rise in plasma renin activity and also aldosterone distributing degrees did not conquer the effects of eplerenone. Compared to its binding to recombinant human glucocorticoid, progesterone and also androgen receptors, eplerenone uniquely binds to recombinant human mineralocorticoid receptors.
Eplerenone is a new type of careful aldosterone receptor antagonist. It was approved by the State Fda for professional application in 2002. The pure product is white or white like crystal, and its aldosterone antagonistic effect is more powerful than spironolactone, and its fondness for androgen and progesterone receptors is very low. The adverse responses are little. It has a certain result on the therapy of hypertension, cardiac arrest and myocardial infarction, with less negative reactions and excellent resistance, It is a good substitute for spironolactone. For serious hypertension that can not be controlled by multiple antihypertensive drugs, the enhancement of eplerenone can dramatically lower blood pressure, particularly systolic high blood pressure. With angiotensin converting enzyme prevention (ACEI) and β The mix of receptor blockers can enhance the lifestyle as well as decrease the death of individuals with serious cardiac arrest as well as coronary infarction.
Eplerenone Uses
- Eplerenone selectively acts on aldosterone receptors and is highly selective for mineralocorticoid receptors, but has less effect on androgen and progesterone receptors, and its affinity for mineralocorticoids is 15-20% of that of spironolactone. It has a 500-fold smaller affinity for androgen and progesterone receptors than spironolactone, so there are fewer sex hormone-related adverse reactions.
- Eplerenone can reduce hypertension C, because aldosterone may play an important role in the pathophysiological process of obesity hypertension, so eplerenone also has a good antihypertensive effect on diet-induced obesity-related hypertension; In addition, eplerenone can significantly reduce glomerular ultrafiltration, thereby reducing proteinuria in hypertensive patients, and this renoprotective effect is more pronounced in hypertensive patients with diabetes.
- Eplerenone is not an inhibitor of CYP1A2, CYP3A4, CYP2C19, CYP2C9, or CYP2D6, and does not inhibit diclofenac, methylphenidate, losartan, amiodarone, dexamethasone, phenytoin, phenacetin, Dextromethorphan, metoprolol, tolbutamide, amlodipine, astemizole, cisapride, diazepam, 17-ethinyl estradiol, fluoxetine, lovastatin, methylprednisone Metabolism of drugs such as dragon, midazolam, nifedipine, glyburide and warfarin.
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This is William, CEO of Zhishang Chemical Co., Ltd.
Welcome to visit our factory . As the top chemical manufacturer, we have been striving for product quality, innovation , R&D, and customer service for the past 7 years. In the next 10 years or even longer, we are committed to becoming the most reliable chemical supplier in the world , creating a well-known international brand trusted by customers, with the spirit of “one meter wide, ten thousand meters deep”, we continue to focus on product research and development, continue to focus on customer service, continue to improve the supply chain service system, to create a professional chemical supply service team, to achieve win-win long-term cooperation. Please feel free to contact us if you have any questions.
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Application of Eplerenone
Cardiovascular disease
EPL and Nephropathy
Cardiovascular disease
- Heart failure: The EPHESUS trial showed that for patients with left ventricular ejection fraction (LVEF) < 40% and heart failure within 3 to 14 days after myocardial infarction, the addition of EPL on the basis of standard treatment can reduce 15 % of all-cause deaths, 17% of the primary composite endpoint (cardiovascular death or hospitalization for a cardiovascular event), and 21% of sudden cardiac death (SCD). For patients with a history of hypertension after acute myocardial infarction, heart failure, and LVEF ≤ 40%, the addition of EPL significantly reduced all-cause mortality, combined primary endpoints, and SCD. In patients without a history of hypertension, EPL reduced HF hospitalizations but did not reduce mortality or other end points. Hospitalization for hypertension is a risk factor for cardiovascular death, and EPL reduces the risk of hospitalization for hypertension in people without a history of hypertension. Because the use of EPL early (3-7 days) after acute myocardial infarction can reduce the primary composite end-point event by 24% and SCD by 34%. However, if EPL was used again for ≥ 7 days, the effect of improving the prognosis was not obvious.
- Hypertension: For patients with mild to moderate hypertension, the blood pressure reduction in the spironolactone 50 mg bid group was greater than that in the EPL 50 mg bid or 100 mg qd group. In patients with hypertension caused by primary aldosteronism, the antihypertensive effect of spironolactone is also better than that of EPL. For hypertensive patients ≥ 50 years old, EPL (50-200 mg/d) and the calcium antagonist amlodipine (2.5-10 mg/d) have similar systolic blood pressure lowering effects. For patients with grade 1 and 2 hypertension, EPL (50-200 mg/d) and the ACEI drug enalapril (10-40 mg/d) are equally effective in the long-term control of SBP and DBP. In black hypertensive patients, EPL was more effective in reducing SBP than the ARB drug losartan, which was not observed in whites. EPL has similar antihypertensive effect on blacks and whites. In patients with high renin hypertension, the antihypertensive effect of EPL is similar to that of losartan. In patients with low renin hypertension, EPL is more effective than losartan in antihypertensive effect. For hypertensive patients who are poorly controlled by ARB alone, adding EPL (50-100 mg·d) for 8 weeks can further enhance the effect of reducing SBP and DBP. For elderly hypertensive patients with poor control of ACEI or ARB, the addition of low-dose (25-50 mg/d, mean 37.5 mg) EPL can effectively reduce SBP and DBP for an average of 24 hours. However, EPL has poor antihypertensive effect in children with hypertension.
EPL and Nephropathy
- EPL in non-diabetic nephropathy can effectively reduce glomerulosclerosis and proteinuria caused by hypertension, independent of the reduction of blood pressure, and the improvement effect is better in patients with mild renal impairment than in patients with normal renal function. For non-diabetic chronic kidney disease (CKD) patients, if RAAS blockers are not effective in controlling proteinuria, adding low-dose EPL (25-50 mg/d) can effectively reduce proteinuria, and its long-term effect and safety are better. it is good.
- Diabetic nephropathy Glomerulosclerosis is an important pathological change in diabetic nephropathy. Its occurrence is related to the high expression of glomerulosclerosis-related molecules such as collagen type I, type IV, PAI-1, TGF-β and fibronectin. The effect of EPL on the expression of glomerulosclerosis-related molecules increased with increasing dose. Low doses of EPL can reduce the expression of various glomerulosclerosis-related molecules. High doses of EPL can improve glomerulosclerosis. For type 2 diabetic mice, although the effect of EPL alone in reducing proteinuria is not obvious, the combination of EPL and lisinopril can reduce proteinuria more effectively than lisinopril alone. The combined use of EPL and lisinopril can more significantly reduce glomerular perfusion and lower creatinine clearance than lisinopril alone, so the increase in serum creatinine level is more obvious.
Preparation of Eplerenone
A preparation method of eplerenone. The method includes the following steps:
- 17α-hydroxy-3-keto-γ-lactone-pregnant-4,9(11) in a solvent, in the presence of a side reaction inhibitor, in a trichloroacetonitrile, an oxidant and a phosphate buffer system -diene-7α, 21-dicarboxylate methyl ester IV carries out double bond selective epoxidation to prepare eplerenone crude product, the reaction formula is as follows:
- The eplerenone crude product is recrystallized to obtain the eplerenone fine product.
Reference
- Eplerenone – PubChem
- CN200910049351.0 Preparation method of eplerenone – ChemicalBook
Eplerenone Supplier and Manufacturer
As a eplerenone supplier and manufacturer with a strict standard product quality system certificate, Zhishang Chemical has long been providing the best eplerenone raw materials to customers all over the world.
Over the years, relying on professional team experience and customer-centric team concept to meet customer needs in a timely manner, our company enjoys a high reputation in the world. At present, our company has served more than 6,000 customers and has established long-term cooperative relations with customers from many countries.
If you have a demand for eplerenone and related products, please contact our service staff Zhishang Chemical – White directly, and we will provide you with high-quality products at the best price.
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FAQ
Do you accept sample order?
We will make samples before mass production, and after the sample is approved, we’ll begin mass production. Doing 100% inspection during production, then doing random inspection before packing.
What’s your MOQ?
Our MOQ is 1kg. But usually we accept less quantities, such as 100g on the condition that the sample charge is 100% paid.
Is there a discount?
The different quantity has different discount.
HOW TO CONFIRM THE PRODUCT QUALITY BEFORE PLACING ORDERS?
You can get free samples for some products, you only need to pay the shipping cost or arrange a courier to us and take the samples. You can send us your product specifications and requests, we will manufacture the products according to your requests.
Do you supply product report?
Yes. We’ll give you product analysis report before shipping.
Shipping
1. ≤50kg, Express delivery recommended, usually called DDU service;
2. ≤500kg, Air shipping recommended, usually called FOB, CFR, or CIF service;
3. >500kg, sea shipping recommended, usually called FOB, CFR, or CIF service;
4. For high-value products, please select air shipping and express delivery for safe.
Quality Control of Eplerenone
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