China Pharma Pure Powder manufacturer

USP BP Leflunomide For Rheumatoid Arthritis 75706-12-6 Analysis Standard

Product Details:
Place of Origin: Xi'an ,China
Brand Name: Wango
Certification: USP, BP
Model Number: WG-0089
Payment & Shipping Terms:
Minimum Order Quantity: 100 gram every time
Price: FOB price USD 720-750/Kilogram,can be Negotiable together .
Packaging Details: 1kg with double plastic container inside/Aluminum foil bag ; 25kg with double plastic container inside/Fiber drum outside.Or as your request.
Delivery Time: 3-5 working days
Payment Terms: Western Union, L/C, T/T, MoneyGram
Supply Ability: 1000kilogram 0ne month

Detail Information

Appearence: White Fine Powder Function1: Antirheumatic
Function2: Arthritis Cas: 75706-12-6
High Light:

BP Leflunomide For Rheumatoid Arthritis

,

USP Leflunomide For Rheumatoid Arthritis

,

75706-12-6 Leflunomide

Product Description

Leflunomide is a pyrimidine synthesis inhibitor indicated to treat rheumatoid arthritis 

USP BP Leflunomide For Rheumatoid Arthritis 75706-12-6 Analysis Standard 0

 

 

 

Leflunomide Chemical Properties

Ref. Standard
According to enterprise internal control standard inspection

Results Of Analysis Tests

Test

Analysis Standard

Results

Description

Powder

Powder

Identification

(1)304nm,260nm.

confirmed

Melting Point

192°C~196°C

192°C~196°C

Specific Rotation

+124°~ +129°

+127.1°

(HPLC)
Related substances

(1)(Single):≤0.5%

0.31%
 
(2)(Total):≤1.0%

0.59%

Loss On Drying

≤0.5%

0.1%

Assay

≥99.2%

99.5%

Sieve analysis

≤30μm

confirmed

Conclusion

This product conforms to enterprise internal control standards
 
1. 
Leflunomide is a pyrimidine synthesis inhibitor belonging to the DMARD (disease-modifying antirheumatic drug) class of drugs, which are chemically and pharmacologically very heterogeneous. Leflunomide was approved by FDA and in many other countries (e.g., Canada, Europe) in 1999.
 
2. Leflunomide is a pyrimidine synthesis inhibitor indicated in adults for the treatment of active rheumatoid arthritis (RA). RA is an auto-immune disease characterized by high T-cell activity. T cells have two pathways to synthesize pyrimidines: the salvage pathways and the de novo synthesis. At rest, T lymphocytes meet their metabolic requirements by the salvage pathway. Activated lymphocytes need to expand their pyrimidine pool 7- to 8-fold, while the purine pool is expanded only 2- to 3-fold. To meet the need for more pyrimidines, activated T cells use the de novo pathway for pyrimidine synthesis. Therefore, activated T cells, which are dependent on de novo pyrimidine synthesis, will be more affected by leflunomide's inhibition of dihydroorotate dehydrogenase than other cell types that use the salvage pathway of pyrimidine synthesis.
 
3. Leflunomide is a prodrug that is rapidly and almost completely metabolized following oral administration to its pharmacologically active metabolite, A77 1726. This metabolite is responsible for essentially all of the drug's activity in-vivo. The mechanism of action of leflunomide has not been fully determined, but appears to primarily involve regulation of autoimmune lymphocytes. It has been suggested that leflunomide exerts its immunomodulating effects by preventing the expansion of activated autoimmune lymphocytes via interferences with cell cycle progression. In-vitro data indicates that leflunomide interferes with cell cycle progression by inhibiting dihydroorotate dehydrogenase (a mitochondrial enzyme involved in de novo pyrimidine ribonucleotide uridine monophosphate (rUMP)synthesis) and has antiproliferative activity. Human dihydroorotate dehydrogenase consists of 2 domains: an α/β-barrel domain containing the active site and an α-helical domain that forms a tunnel leading to the active site. A77 1726 binds to the hydrophobic tunnel at a site near the flavin mononucleotide. Inhibition of dihydroorotate dehydrogenase by A77 1726 prevents production of rUMP by the de novo pathway; such inhibition leads to decreased rUMP levels, decreased DNA and RNA synthesis, inhibition of cell proliferation, and G1 cell cycle arrest. It is through this action that leflunomide inhibits autoimmune T-cell proliferation and production of autoantibodies by B cells. Since salvage pathways are expected to sustain cells arrested in the G1 phase, the activity of leflunomide is cytostatic rather than cytotoxic. Other effects that result from reduced rUMP levels include interference with adhesion of activated lymphocytes to the synovial vascular endothelial cells, and increased synthesis of immunosuppressive cytokines such as transforming growth factor-β (TGF-β). Leflunomide is also a tyrosine kinase inhibitor. Tyrosine kinases activate signalling pathways leading to DNA repair, apoptosis and cell proliferation. Inhibition of tyrosine kinases can help to treating cancer by preventing repair of tumor cells.
4. The active metabolite is eliminated by further metabolism and subsequent renal excretion as well as by direct biliary excretion. In a 28 day study of drug elimination (n=3) using a single dose of radiolabeled compound, approximately 43% of the total radioactivity was eliminated in the urine and 48% was eliminated in the feces. It is not known whether leflunomide is excreted in human milk. Many drugs are excreted in human milk, and there is a potential for serious adverse reactions in nursing infants from leflunomide.
 
F.A.Q

1:Can I get some samples before bulk order?
Most products provide free samples, but the shipping cost be paid by customers.

2: What's your MOQ?
For the high value product, our MOQ starts from 10g,100g and 1kg.

3: Which kind of payment terms do you accept?
PI will be sent first after confirmation of order,enclosed our bank information.Payment by T/T, Western Union, L/C, Alibaba trade assurance, Cashapp,Moneygram or Bitcoin.

4.How to place an order?
You can contact me through Trademanager, WhatsApp, Skype Online and other contact methods, tell me the product and quantity you need, and then we will give you a quote. If you choose one of the above payment methods, we will arrange the delivery for you.

5:How about your delivery time?
A: Generally, it will take 3 to 5 days after receiving your advance payment.

6:How do you treat quality complaint?
A:First of all, our quality control will reduce the quality problem to near zero. If there is a real quality problem caused by us, we will send you free goods for replacement or refund your loss.

 

 


 

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