A-771726
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
A771726 is dihydroorotate dehydrogenase inhibitor.
The dihydroorotate dehydrogenase (DHODH) is a mitochondrial protein. Inhibitors of DHODH can be used to treat autoimmune diseases such as rheumatoid arthritis.
A771726, leflunomide's active metabolite, showed significantly inhibitory effect on TNF-α and IL-1 at protein and transcription levels, and reduced production of IL-1 in monocultures of Kupffer cells (KCs) [1]. A-771726 reversibly inhibited dihydroorotate dehydrogenase, the rate-limiting step in the de novo synthesis of pyrimidines. A-771726 prevented activated lymphocytes from accumulating sufficient pyrimidines to support DNA synthesis with the IC50 values of 0.09, 3.5, and 12.5 μM for rat, mouse, and human, respectively [2]. A-771726 inhibited the activity of tyrosine kinases responsible for early T cell and B cell signaling in the G0/G1 phase of the cell cycle at higher doses [2]. A-771726 also inhibited the production of prostaglandin E2 in synoviocytes activated by TNF-α and IL-1α with the IC50 values of 7 and 3 μM, respectively. A771726 also inhibited MMP-1 and IL-6 production at concentrations >10 μM [3]. A771726 is a novel immunosuppressive compound that has been shown to be a powerful antiproliferative agent for mononuclear and T-cells. A771726 potently inhibited the activity of DHODase with the Ki of 179 ± 19 nM. A771726 was a competitive inhibitor of the ubiquinone binding site [4].
References:
[1] Yao H W, Li J, Chen J Q, et al. A 771726, the active metabolite of leflunomide, inhibits TNF-α and IL-1 from Kupffer cells[J]. Inflammation, 2004, 28(2): 97-103.
[2] Breedveld F C, Dayer J M. Leflunomide: mode of action in the treatment of rheumatoid arthritis[J]. Annals of the rheumatic diseases, 2000, 59(11): 841-849.
[3] Burger D, Begué‐Pastor N, Benavent S, et al. The active metabolite of leflunomide, A77 1726, inhibits the production of prostaglandin E2, matrix metalloproteinase 1 and interleukin 6 in human fibroblast‐like synoviocytes[J]. Rheumatology, 2003, 42(1): 89-96.
[4] Davis J P, Cain G A, Pitts W J, et al. The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase[J]. Biochemistry, 1996, 35(4): 1270-1273.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 270.2 |
Cas No. | 163451-81-8 |
Formula | C12H9F3N2O2 |
Synonyms | Flucyamide,HMR 1726,SU 20,Teriflunomide |
Solubility | ≤10.7mg/ml in DMSO;21.6mg/ml in dimethyl formamide |
Chemical Name | 2-cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-2Z-butenamide |
SDF | Download SDF |
Canonical SMILES | O=C(/C(C#N)=C(O)/C)NC1=CC=C(C(F)(F)F)C=C1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
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