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A77 1726

A77 1726 ??? ???
?? ??:
163451-81-8
???:
A77 1726
???(??):
Flucyamide;A77 1726 (Teriflunomide);2-Butenamide, 2-cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-, (2Z)-;A 1726;HMR 1726;A77 1726;Teriflunomide(b);Teriflunomide (cGMP);Leflunomide Impurity B;Teriflunomide solution
CBNumber:
CB02486749
???:
C12H9F3N2O2
??? ??:
270.21
MOL ??:
163451-81-8.mol
MSDS ??:
SDS

A77 1726 ??

???
229-232°C
?? ?
410.8±45.0 °C(Predicted)
??
1.424±0.06 g/cm3(Predicted)
?? ??
-20°C
???
DMSO: ???5mg/mL, ??(??)
?? ?? (pKa)
5.20±0.50(Predicted)
??? ??
??
??
???? ????
?? ??(λmax)
203nm(MeOH)(lit.)
Merck
14,9165
???
???
InChIKey
UTNUDOFZCWSZMS-YFHOEESVSA-N
??
  • ?? ? ?? ??
  • ?? ? ???? ?? (GHS)
??? ?? Xn
?? ???? ?? 22
WGK ?? 3
HS ?? 2926.90.4801
????(GHS): GHS hazard pictograms
?? ?: Warning
??·?? ??:
?? ??·?? ?? ?? ?? ?? ?? ? ?? ?? P- ??
H225 ???? ?? ? ?? ??? ?? ?? 2 ?? GHS hazard pictograms P210,P233, P240, P241, P242, P243,P280, P303+ P361+P353, P370+P378,P403+P235, P501
H319 ?? ?? ??? ??? ?? ? ?? ?? ??? ?? ?? 2A ?? GHS hazard pictograms P264, P280, P305+P351+P338,P337+P313P
??????:
P210 ?·???·??·????? ????? - ?? ???.
P280 ????/???/???/?????? ?????.
P301+P312 ??? ???? ??? ????(??)? ??? ????.
P303+P361+P353 ??(?? ????)? ??? ??? ?? ??? ??? ????? ??? ?? ????/?????.
P305+P351+P338 ?? ??? ? ?? ?? ???? ????. ???? ?????? ?????. ?? ????.
NFPA 704
0
2 0

A77 1726 C??? ??, ??, ??

??

In September 2012, the US FDA approved teriflunomide (also referred to as HMR-1726) as a therapy for patients with relapsing forms of multiple sclerosis (MS). Teriflunomide is the second approved oral treatment option for MS, after Gilenya? which was approved in 2010. Teriflunomide, which is the active metabolite of leflunomide (a marketed drug for the treatment of rheumatoid and psoriatic arthritis), is a non?competitive and selective inhibitor of dihydroorotate dehydrogenase (DHODH), the rate-limiting enzyme in the de novo synthesis of pyrimidines. Although the net effect of inhibition of DHODH by teriflunomide and its therapeutic effect in MS are not clear, it is hypothesized that by inhibiting de novo pyrimidine synthesis, the effector functions of activated lymphocytes are suppressed, thus dampening the effect of an overactive immune system.

??? ??

White Solid

??

The active metabolite of Leflunomide, a potent disease-modifying antirheumatic drug used in the treatment of rheumatoid arthritis. LEF-M interferes with dendritic cell function.

??

ChEBI: An enamide obtained by formal condensation of the carboxy group of (2Z)-2-cyano-3-hydroxybut-2-enoic acid with the anilino group of 4-(trifluoromethyl)aniline. Used for the treatment of relapsing forms of multiple sclerosis and rheumatoid arthritis.

?? ??

Teriflunomide, marketed under the trade name Aubagio, is the active metabolite of leflunomide, an immunosuppressive disease-modifying antirheumatic drug, used in active moderate-to-severe rheumatoid arthritis and psoriatic arthritis. An analytical reference standard for use in LC/MS or GC/MS applications including clinical and diagnostic testing such as therapeutic drug monitoring assays.

A77 1726 ?? ?? ? ???

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A77 1726 ?? ??

???( 244)?? ??
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A77 1726 ?? ??:

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