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94345-47-8

CAS 94345-47-8
分子式 C21H28N4O2
分子量 368.47
MOL 文件 94345-47-8.mol
94345-47-8 結(jié)構(gòu)式 94345-47-8 結(jié)構(gòu)式
4-[7-(4-carbamimidoylphenoxy)heptoxy]benzenecarboximidamide價格(試劑級)
報(bào)價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2023/03/20HY-169184-[7-(4-carbamimidoylphenoxy)heptoxy]benzenecarboximidamide
Heptamidine
94345-47-85mg2100元
2023/03/20HY-169184-[7-(4-carbamimidoylphenoxy)heptoxy]benzenecarboximidamide
Heptamidine
94345-47-810mg3360元
2023/03/20HY-169184-[7-(4-carbamimidoylphenoxy)heptoxy]benzenecarboximidamide
Heptamidine
94345-47-850mg9750元

常見問題列表

生物活性
Heptamidine (SBi4211) 是一種強(qiáng)效的 Pentamidine-related 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 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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