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1161-94-0

中文名稱 PHENAMIL METHANESULFONATE
英文名稱 PHENAMIL METHANESULFONATE
CAS 1161-94-0
分子式 C13 H16 Cl N7 O4 S
分子量 401.8
MOL 文件 1161-94-0.mol
1161-94-0 結(jié)構(gòu)式 1161-94-0 結(jié)構(gòu)式

基本信息

中文別名
化合物 T23148
英文別名
MHPIZTURFVSLTJ-UHFFFAOYSA-N

物理化學(xué)性質(zhì)

儲(chǔ)存條件2-8°C
溶解度45%(w/v)aq2-羥丙基-β-環(huán)糊精:可溶2.5mg/mL
形態(tài)固體
顏色黃色
CAS 數(shù)據(jù)庫(kù)1161-94-0

安全數(shù)據(jù)

WGK Germany3

常見問(wèn)題列表

生物活性
Phenamil methanesulfonate 是 Amiloride (HY-B0285) 的類似物,一種更有效且不可逆的上皮鈉通道 (ENaC) 阻滯劑,IC50 為 400 nM。Phenamil methanesulfonate 也是 TRPP3 的競(jìng)爭(zhēng)性抑制劑,在 Ca2+ 攝取實(shí)驗(yàn)中,抑制 TRPP3 介導(dǎo)的 Ca2+ 轉(zhuǎn)運(yùn)的 IC50 為 140 nM。Phenamil methanesulfonate 是一種通過(guò)強(qiáng)烈激活 BMP 信號(hào)通路來(lái)促進(jìn)骨修復(fù)的小分子。Phenamil methanesulfonate 用于囊性纖維化肺疾病的相關(guān)研究。
靶點(diǎn)

TRPC3

140 nM (IC 50 )

體外研究

TRPP3, a member of the transient receptor potential (TRP) superfamily of cation channels, is a Ca 2+ -activated channel permeable to Ca 2+ , Na + , and K + . TRPP3 is implicated in regulation of pH-sensitive action potential in spinal cord neurons. Phenamil methanesulfonate (1 μM) decreases 45 Ca 2+ uptake in a radiotracer uptake assay. It inhibits TRPP3-mediated Ca 2+ transport with an IC 50 value of 0.28 μM in oocytes expressing TRPP3 or H2O-injected oocytes. Phenamil methanesulfonate is a more potent ENaC blocker than Amiloride, it inhibits the epithelial sodium channel (ENaC) with an IC 50 of 400 nM (Amiloride=776 nM).Phenamil methanesulfonate inhibits basal short-circuit currents with IC 50 values of 75 and 116 nM, respectively in both human and ovine bronchial epithelia cells.Phenamil methanesulfonate (0-20 μM; 14 days) elevates adipogenic gene expression, PPARγ, Fabp4, and lipoprotein lipase expression in a concentration-dependent manner ,and regulates adipogenesis in C3H10T1/2 cells.Phenamil methanesulfonate (0-20 μM; 7 or 14 days) modulates MC3T3-E1 osteoblastic differentiation, it increases Alkaline phosphatase (ALP) activity in MC3T3-E1 cells in a concentration-dependent manner.

RT-PCR

Cell Line: C3H10T1/2 cells
Concentration: 0 μM and 20 μM
Incubation Time: 14 days
Result: Increased PPARγ, Fabp4, and lipoprotein lipase (LPL) mRNA expression.
體內(nèi)研究

Phenamil methanesulfonate (subcutaneous injection; 15 or 30 mg/kg; 21 days; infusion rate of 1 ml/h) reduces chronic-hypoxia-induced pulmonary artery hypertension (PAH). Additionally, the mRNA level of SMA, SM22, Id3, and Trb3 from the lung sample are also decreased by Phenamil under hypoxia or normoxia in rats. However, phenamil has little effect on pulmonary vasculature under physiological conditions.

Animal Model: Male Sprague-Dawley rats
Dosage: 15 or 30 mg/kg
Administration: Subcutaneous injection; 15 or 30 mg/kg; 21 days; infusion rate of 1 ml/h
Result: Reduced hypoxia-induced pulmonary hypertension and vascular remodeling.
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