Lesinurad sodium is a uric acid transporter inhibitor that is used in combination with other medications to treat gout. It was approved by the US Food and Drug Administration (FDA) in 2015 and is marketed under the brand name Zurampic. Lesinurad sodium is a small molecule that selectively inhibits the uric acid transporter 1 (URAT1) and organic anion transporter 4 (OAT4), which are responsible for the reabsorption of uric acid in the kidneys. This paper aims to provide a comprehensive review of lesinurad sodium, including its method of synthesis or extraction, chemical structure and biological activity, biological effects, applications, and future perspectives and challenges.
Lesinurad sodium is synthesized using a multi-step process that involves the reaction of 2,4-dichloro-5-nitropyrimidine with 4-methylbenzenesulfonamide to form 2,4-dichloro-5-nitro-N-(4-methylbenzenesulfonyl)pyrimidine. This intermediate is then reduced to 2,4-dichloro-5-amino-N-(4-methylbenzenesulfonyl)pyrimidine using palladium on carbon as a catalyst. The final step involves the reaction of 2,4-dichloro-5-amino-N-(4-methylbenzenesulfonyl)pyrimidine with sodium hydroxide to form lesinurad sodium. The efficiency and yield of the synthesis process depend on the reaction conditions and the quality of the starting materials. The overall yield of the synthesis process is around 20%, which is considered moderate. The synthesis process is relatively safe and environmentally friendly, as it does not involve any hazardous reagents or byproducts.
Chemical Structure and Biological Activity
Lesinurad sodium has a molecular formula of C17H13Cl2N5NaO3S and a molecular weight of 476.28 g/mol. It is a white to off-white crystalline powder that is soluble in water and ethanol. The chemical structure of lesinurad sodium consists of a pyrimidine ring with two chlorine atoms, a sulfonamide group, and a sodium ion. The mechanism of action of lesinurad sodium involves the inhibition of URAT1 and OAT4, which are responsible for the reabsorption of uric acid in the kidneys. By inhibiting these transporters, lesinurad sodium increases the excretion of uric acid in the urine, thereby reducing the serum uric acid levels. Lesinurad sodium has been shown to be effective in reducing serum uric acid levels in patients with gout when used in combination with other medications, such as allopurinol.
Lesinurad sodium has been shown to have several biological effects on cell function and signal transduction. It has been shown to inhibit the activity of URAT1 and OAT4, which are involved in the reabsorption of uric acid in the kidneys. Lesinurad sodium has also been shown to reduce the production of pro-inflammatory cytokines, such as interleukin-1β and tumor necrosis factor-α, which are involved in the pathogenesis of gout. In terms of potential therapeutic and toxic effects, lesinurad sodium has been shown to be effective in reducing serum uric acid levels in patients with gout when used in combination with other medications. However, it may cause some adverse effects, such as headache, influenza-like symptoms, and renal impairment. Therefore, it is important to monitor the renal function of patients receiving lesinurad sodium.
Lesinurad sodium has several applications in medical research, such as its role in drug development, clinical trials, and findings, benefits, and potential side effects. Lesinurad sodium has been shown to be effective in reducing serum uric acid levels in patients with gout when used in combination with other medications, such as allopurinol. Clinical trials have shown that lesinurad sodium is well-tolerated and effective in reducing serum uric acid levels in patients with gout. In environmental research, lesinurad sodium has been shown to have effects on ecosystems and its role in pollution management and sustainability and environmental impact. Lesinurad sodium has not been extensively studied in terms of its environmental impact, but it is expected to have a low environmental impact due to its low toxicity and biodegradability. In industrial research, lesinurad sodium has been used in manufacturing processes to improve product quality and efficiency. Health and safety considerations are important when using lesinurad sodium in industrial processes, as it may cause adverse effects if not handled properly.
Future Perspectives and Challenges
The current limitations in the use and study of lesinurad sodium include its potential adverse effects, such as renal impairment, and its limited efficacy in some patients with gout. Possible solutions and improvements include the development of new formulations and dosing regimens that minimize the risk of adverse effects and improve the efficacy of lesinurad sodium. Future trends and prospects in the application of lesinurad sodium in scientific research include the development of new medications that target other transporters involved in the reabsorption of uric acid in the kidneys. This may lead to the development of more effective and safer medications for the treatment of gout. Conclusion: Lesinurad sodium is a uric acid transporter inhibitor that is used in combination with other medications to treat gout. It is synthesized using a multi-step process that is relatively safe and environmentally friendly. Lesinurad sodium has a chemical structure that consists of a pyrimidine ring with two chlorine atoms, a sulfonamide group, and a sodium ion. Its mechanism of action involves the inhibition of URAT1 and OAT4, which are responsible for the reabsorption of uric acid in the kidneys. Lesinurad sodium has several biological effects on cell function and signal transduction and has several applications in medical, environmental, and industrial research. The future perspectives and challenges in the use and study of lesinurad sodium include the development of new formulations and dosing regimens and the development of new medications that target other transporters involved in the reabsorption of uric acid in the kidneys.
Q1: How Can I Obtain a Quote for a Product I'm Interested In?
To receive a quotation, send us an inquiry about the desired product.
The quote will cover pack size options, pricing, and availability details.
If applicable, estimated lead times for custom synthesis or sourcing will be provided.
Quotations are valid for 30 days, unless specified otherwise.
Q2: What Are the Payment Terms for Ordering Products?
New customers generally require full prepayment.
NET 30 payment terms can be arranged for customers with established credit.
Contact our customer service to set up a credit account for NET 30 terms.
We accept purchase orders (POs) from universities, research institutions, and government agencies.
Q3: Which Payment Methods Are Accepted?
Preferred methods include bank transfers (ACH/wire) and credit cards.
Request a proforma invoice for bank transfer details.
For credit card payments, ask sales representatives for a secure payment link.
Checks aren't accepted as prepayment, but they can be used for post-payment on NET 30 orders.
Q4: How Do I Place and Confirm an Order?
Orders are confirmed upon receiving official order requests.
Provide full prepayment or submit purchase orders for credit account customers.
Send purchase orders to firstname.lastname@example.org.
A confirmation email with estimated shipping date follows processing.
Q5: What's the Shipping and Delivery Process Like?
Our standard shipping partner is FedEx (Standard Overnight, 2Day, FedEx International Priority), unless otherwise agreed.
You can use your FedEx account; specify this on the purchase order or inform customer service.
Customers are responsible for customs duties and taxes on international shipments.
Q6: How Can I Get Assistance During the Ordering Process?
Reach out to our customer service representatives at email@example.com.
For ongoing order updates or questions, continue using the same email.
Remember, we're here to help! Feel free to contact us for any queries or further assistance.
Note: Kindly utilize formal channels such as professional, corporate, academic emails, etc., for inquiries. The use of personal email for inquiries is not advised.
Lesinurad is a novel uric acid transporter 1 (URAT1) inhibitor that has been approved by the US Food and Drug Administration (FDA) for the treatment of hyperuricemia associated with gout. It is a small molecule drug that has shown promising results in clinical trials and has the potential to become a valuable addition to the current treatment options for gout.
Sodium 4-pentynoate is a chemical compound that belongs to the family of alkynoates. It is a white crystalline powder that is soluble in water and organic solvents. Sodium 4-pentynoate has gained significant attention in scientific research due to its potential therapeutic and industrial applications.
GW791343 (dihydrochloride) is a small molecule inhibitor that has gained significant attention in the scientific community due to its potential therapeutic and environmental applications. It is a selective antagonist of the P2X7 receptor, which is involved in various physiological and pathological processes.
Telotristat is a small molecule drug that is used to treat carcinoid syndrome, a rare condition that occurs in patients with neuroendocrine tumors. It works by inhibiting the production of serotonin, a hormone that is overproduced in patients with carcinoid syndrome. This paper will discuss the method of synthesis or extraction of telotristat, its chemical structure and biological activity, its biological effects, applications in medical, environmental, and industrial research, and future perspectives and challenges.
Bisoctrizole is a chemical compound that belongs to the class of benzotriazole derivatives. It is widely used in various fields, including medical, environmental, and industrial research. Bisoctrizole is known for its excellent UV-absorbing properties, making it a popular ingredient in sunscreens and other cosmetic products.
AZ 505 is an inhibitor of the lysine N-methyltransferase SMYD2 (IC50 = 0.12 μM). It is selective for SMYD2 over SMYD3, DOT1L, EZH2, GLP, G9A, and SET7/9 (IC50s = >83.3 μM). AZ 505 (10 mg/kg) delays cyst growth in early- and late-stage Pdk1 conditional knockout mouse models of polycystic kidney disease. AZ505 is a potent and highly selective inhibitor of SMYD2 with potential anticancer activity. AZ505 is composed of three distinct moieties: benzooxazinone, cyclohexyl, and dichlorophenethyl substituents. The structure of the ternary complex reveals that a single AZ505 molecule is bound in the peptide binding groove of SMYD2.
4'-(3-((3R)-3-(Dimethylamino)pyrrolidinyl)propoxy)(1,1'-biphenyl)-4-carbonitrile, also known as DPCPX, is a potent and selective antagonist of the adenosine A1 receptor. It has been extensively studied for its potential therapeutic applications in various diseases, including cardiovascular, neurological, and inflammatory disorders.
KX2-391 dihydrochloride is a small molecule inhibitor that has shown promising results in preclinical studies for the treatment of various cancers, including melanoma, prostate, and breast cancer. It is a derivative of the Src kinase inhibitor, PP1, and has been shown to inhibit the activity of Focal Adhesion Kinase (FAK), a protein that plays a crucial role in cell migration, invasion, and survival.