Tafamidis

A TTR kinetic stabilizer

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库存: 现货

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数量
5mg

￥762.00

610.00

- +
10mg

￥1300.00

1040.00

- +
25mg

￥2612.00

2090.00

- +
50mg

￥4425.00

3540.00

- +
100mg

￥7662.00

6130.00

- +
200mg

￥0.00

0.00

- +
500mg

￥0.00

0.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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货号: ajce59680
CAS: 594839-88-0
别名: 氯苯唑酸
分子式: C14H7Cl2NO3
分子量: 308.12
纯度: >98%
溶解度: DMSO: 37.5 mg/mL (121.71 mM); Water: < 0.1 mg/mL (insoluble)
储存: Store at -20°C
库存: 现货

Background

Tafamidis is a kinetic stabilizer of transthyretin (TTR) that prevents amyloidogenesis by wild-type and mutant TTRs.¹ It binds to TTR with negative cooperativity (K_d1 = 3 nM; K_d2 = 278 nM) to stabilize the TTR dimer-dimer interface and inhibit tetrameric dissociation. Tafamidis stabilizes wild-type and clinically significant V30M and V122I mutant TTR amyloidogenic homotetramers (EC₅₀s = 2.7-3.2 μM) under fibril-promoting, denaturing, and physiological conditions in vitro. It stabilizes TTR heterotetramers containing wild-type and mutant subunits ex vivo in human plasma derived from patients carrying V30M or V1221 mutations when used at a concentration of 7.2 μM. Formulations containing tafamidis have been used for the treatment of familial amyloid polyneuropathy.²

1.Bulawa, C.E., Connelly, S., Devit, M., et al.Tafamidis, a potent and selective transthyretin kinetic stabilizer that inhibits the amyloid cascadeProc. Natl. Acad. Sci. USA109(24)9629-9634(2012) 2.Scott, L.J.Tafamidis: A review of its use in familial amyloid polyneuropathyDrugs74(12)1371-1378(2014)