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161374-55-6

中文名稱 SBi4211 dimethanesulfonate
英文名稱 SBi4211 dimethanesulfonate
CAS 161374-55-6
更新日期 2024/12/22 21:24:10
分子式 C22H32N4O5S
分子量 464.58
MOL 文件 161374-55-6.mol
161374-55-6 結(jié)構(gòu)式 161374-55-6 結(jié)構(gòu)式

基本信息

中文別名
化合物HEPTAMIDINE DIMETHANESULFONATE
英文別名
SBi4211 dimethanesulfonate
Heptamidine dimethanesulfote
Heptamidine dimethanesulfonate

物理化學(xué)性質(zhì)

儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO: 62.5 mg/mL (111.47 mM)
形態(tài)Solid
顏色Off-white to light yellow

安全數(shù)據(jù)

危險(xiǎn)性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H335
SBi4211 dimethanesulfonate價(jià)格(試劑級)
報(bào)價(jià)日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價(jià)格
2024/11/08HY-16918ASBi4211 dimethanesulfonate
Heptamidine dimethanesulfonate
161374-55-65mg1760元
2024/11/08HY-16918ASBi4211 dimethanesulfonate
Heptamidine dimethanesulfonate
161374-55-610mM * 1mLin DMSO2171元
2024/11/08HY-16918ASBi4211 dimethanesulfonate
Heptamidine dimethanesulfonate
161374-55-610mg2800元

常見問題列表

生物活性
Heptamidine dimethanesulfonate (SBi4211 dimethanesulfonate) 是一種強(qiáng)效的,與噴他脒 (HY-B0537) 有關(guān)的鈣結(jié)合蛋白 S100B 的抑制劑 (Kd=6.9 μM),選擇性地殺死表達(dá) S100B 的黑素瘤細(xì)胞。Heptamidine dimethanesulfonate 是研究強(qiáng)直性肌營養(yǎng)不良 (DM) 的有效工具。
靶點(diǎn)

Kd: 6.9 μM (calcium-binding protein S100B)

體外研究

Heptamidine is a Pentamidine-S100B complex, two molecules of pentamidine bind per monomer of S100B, which performs to be an inhibitor for S100B.Heptamidine (20 μM) does not decrease CUG levels?significantly when compares to Propamidine and Pentamidine, and exhibits cytotoxic at concentrations above 17.5 μM in HeLa cells expressing 960 CUG repeats.Heptamidine rescues mis-splicing of minigene reporters in a HeLa cell DM1 model with an EC 50 value of 15 μM.

體內(nèi)研究

Heptamidine (intraperitoneal injection; 20 or 30 mg/kg; 7 days) causes a dose-dependent reduction of exon 7a inclusion in HSA LR?mice, returning to wild type levels (6±1%) when at 20 mg/kg dose, the myotonia is reduced from grade 3 to grade 1 (occasional myotonic discharge) or grade 0 at both 20 or 30 mg/kg.

Animal Model: Homozygous?HSALR?transgenic mice in line 20b (FVB inbred background)?with a Myotonic dystrophy (DM) mouse model
Dosage: 20 or 30 mg/kg
Administration: Intraperitoneal injection; 7 days; once daily
Result: Reversed splicing defects and rescues myotonia in a DM mouse model.
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