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Purity: >99%
Brand Name: NJBN STEROID
Grade Standard:
Type:
CAS No.: 75706-12-6
Model Number: 75706-12-6
Place of Origin: China (Mainland)
EINECS No.: 200-035-3
MF: C32H36ClNO8
Other Names: Leflunomide
Classification: High Purity Reagents
Standard: Standard
Usage: An unducer of ovulation. A gonad-stimulating principle,Synthetic estrogen agonist antagonist. Gonad-stimulating principle)
Delivery: Express courier

Specifications

Nonsteroidal anti-inflammatory Drug Anti-Altzheimer Therapeutic Leflunomide CAS 75706-12-6


Product Name:Leflunomide
Synonyms:LEFLUNOMIDE;HWA 486;ALPHA,ALPHA,ALPHA-TRIFLUORO-5-METHYL-4-ISOXAZOLECARBOXY-P-TOLUIDIDE;5-METHYLISOXAZOLE-4-(4-TRIFLUOROMETHYLCARBOXANILIDE);5-METHYL-N-[4-(TRIFLUOROMETHYL)PHENYL]-4-ISOXAZOLECARBOXAMIDE;N-(4-TRIFLUOROMETHYLPHENYL)-5-METHYLISOXAZOL-4-CARBOXAMIDE;5-methylisoxazole-4-carboxylicacid(4-trifluoromethyl)anilide;5-methyl-n-(4-(trifluoromethyl)phenyl)-4-isoxazolecarboxamid
CAS:75706-12-6
MF:C12H9F3N2O2
MW:270.21
Product Categories:Active Pharmaceutical Ingredients;API;Osteoarthritis and Rheumatoid Arthritis;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;Cytokine signaling;Aromatics;Heterocycles;An immunosuppressive agent;CARDENE;Other APIs;leflunomide
Melting point: 163-168C
Storage temp.: 2-8C
Chemical Properties: off White Crystalline Solid
Uses: An immunosuppressive. Inhibits T and B cell proliferation. Activity is attributed mainly to its metabolite, a malononitrile derivative, which is beleived to inhibit dihydroorotate dehydrogenase as well as several protein tyrosine kinases. Therapeutical
Uses: vasodilator
Uses: anti-Altzheimer therapeutic.


Leflunomide Immunosuppressants

Leflunomide is a kind of isoxazole immunosuppressive drugs with anti-proliferative activity, modern pharmacology classifies  this product  as antipyretic, analgesic and anti-inflammatory drugs. this product can be rapidly converted to the active metabolites  and play a role by the liver and intestinal cytoplasm and microsomes, its  main mechanism is  during DNA synthesis, inhibiting a key enzyme-DHODH (DHODH) activity, so that the nucleotides within the B lymphocyte  are depleted, it terminates the biosynthesis of DNA and RNA, the cells can not enter s phase, and ultimately can not proliferate, resulting in anti-rheumatic effects, it is suitable for the treatment of adults with active rheumatoid arthritis, ankylosing spondylitis, it can slow bone destruction, alleviate the symptoms and signs. In addition, leflunomide can also inhibit the tyrosine kinase activity, thereby inhibiting proliferation of T cell, B cell  and non-immune cells, but it can also, by biosynthesis inhibition of cyclooxygenase-2 (COX2), inhibit prostaglandin synthesis and exert anti-inflammatory effects and inhibit mast cells and basophils histamine release. When  this product is used in organ transplant patients,the  dose adjustment is difficult, it is mainly used to treat rheumatoid arthritis and other autoimmune diseases.

after oral administration of the product, it is rapidly transformed to the active metabolite  in the intestinal wall and liver , F is 80%,it  does not affect the  absorption of the meal. Tmax is 6~12 h, if the first dose is administered as a loading dose of 100mg, it can reach steady-state plasma concentrations in 3 days, otherwise it needs numbers of months to reach steady-state plasma concentrations. Active metabolite PPB is 99.3%, which is mainly  distributed in the liver, kidney and skin, less in brain tissue. after further metabolization of the active metabolite,  43% of the marker is excreted in the urine of, 48% is excreted by the fecal, T1/2 is about 2 weeks, enterohepatic circulation leads to a longer half-life of the active metabolite  which is the main factor. High-fat diet does not have a big effect on the plasma concentrations of drugs. Activated charcoal or cholestyramine inhibits absorption of the drug.

the main side effects of leflunomide include  anorexia, vomiting, abdominal pain, diarrhea, gastritis and gastroenteritis, skin rashes, hair loss and reversible transaminase elevation.


Leflunomide Uses

(1) It is hydrogenated acid dehydrogenase inhibitor with immunosuppressive and anti-inflammatory effects for the treatment of adults with active rheumatoid arthritis.
(2) Nonsteroidal anti-inflammatory drug.




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