calcium channel) 拮抗劑。Felodipine 通過選擇性作用于血管平滑肌,尤其是阻力血管來降低血壓。">
取消
清空記錄
歷史記錄
清空記錄
歷史記錄
產(chǎn)品中心
Felodipine 是一種二氫吡啶,是一種有效的血管選擇性鈣通道 (b>calcium channel) 拮抗劑。Felodipine 通過選擇性作用于血管平滑肌,尤其是阻力血管來降低血壓。Felodipine 是具有抗高血壓活性,可誘導(dǎo)自噬。Felodipine 可以跨越血腦屏障。
生物活性
Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier[1][2][3].
體外研究(In Vitro)
Felodipine, a dihydropyridine calcium antagonist, is the most potent in relaxing porcine coronary arteries (IC50=0.15 nM)[1].
Felodipine, an L-type calcium channel blocker, induces autophagy and clears diverse aggregate-prone, neurodegenerative disease-associated proteins [2].
Felodipine blocks the muscarinic receptor-mediated (carbachol) Ca2+-dependent contraction of guinea pig ileum longitudinal smooth muscle (GPILSM) with an IC50 of 1.45 nM[3].
分子量:384.25
性狀:Solid
Formula:C18H19Cl2NO4
CAS 號(hào):72509-76-3
中文名稱:非洛地平
運(yùn)輸條件:Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
溶解性數(shù)據(jù)
DMSO : 100 mg/mL (260.25 mM; Need ultrasonic)
濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
---|
1 mM | 2.6025 mL | 13.0124 mL | 26.0247 mL |
5 mM | 0.5205 mL | 2.6025 mL | 5.2049 mL |
10 mM | 0.2602 mL | 1.3012 mL | 2.6025 mL |
請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 儲(chǔ)存時(shí),請(qǐng)?jiān)?6 個(gè)月內(nèi)使用,-20°C 儲(chǔ)存時(shí),請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。
以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用; 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶
參考文獻(xiàn)
[1]. Johnson JD, et al. Calcium and calmodulin antagonists binding to calmodulin and relaxation of coronary segments. J Pharmacol Exp Ther. 1983;226(2):330-334. [Content Brief]
[2]. Siddiqi FH, et al. Felodipine induces autophagy in mouse brains with pharmacokinetics amenable to repurposing [published correction appears in Nat Commun. 2019 Jun 4;10(1):2530]. Nat Commun. 2019;10(1):1817. Published 2019 Apr 18. [Content Brief]
[3]. Yiu, S. and E.E. Knaus, Synthesis, biological evaluation, calcium channel antagonist activity, and anticonvulsant activity of felodipine coupled to a dihydropyridine-pyridinium salt redox chemical delivery system. J Med Chem, 1996. 39(23): p. 4576-82. [Content Brief]
Felodipine 是一種二氫吡啶,是一種有效的血管選擇性鈣通道 (b>calcium channel) 拮抗劑。Felodipine 通過選擇性作用于血管平滑肌,尤其是阻力血管來降低血壓。Felodipine 是具有抗高血壓活性,可誘導(dǎo)自噬。Felodipine 可以跨越血腦屏障。
生物活性
Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier[1][2][3].
體外研究(In Vitro)
Felodipine, a dihydropyridine calcium antagonist, is the most potent in relaxing porcine coronary arteries (IC50=0.15 nM)[1].
Felodipine, an L-type calcium channel blocker, induces autophagy and clears diverse aggregate-prone, neurodegenerative disease-associated proteins [2].
Felodipine blocks the muscarinic receptor-mediated (carbachol) Ca2+-dependent contraction of guinea pig ileum longitudinal smooth muscle (GPILSM) with an IC50 of 1.45 nM[3].
分子量:384.25
性狀:Solid
Formula:C18H19Cl2NO4
CAS 號(hào):72509-76-3
中文名稱:非洛地平
運(yùn)輸條件:Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
溶解性數(shù)據(jù)
DMSO : 100 mg/mL (260.25 mM; Need ultrasonic)
濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
---|
1 mM | 2.6025 mL | 13.0124 mL | 26.0247 mL |
5 mM | 0.5205 mL | 2.6025 mL | 5.2049 mL |
10 mM | 0.2602 mL | 1.3012 mL | 2.6025 mL |
請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 儲(chǔ)存時(shí),請(qǐng)?jiān)?6 個(gè)月內(nèi)使用,-20°C 儲(chǔ)存時(shí),請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。
以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用; 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶
參考文獻(xiàn)
[1]. Johnson JD, et al. Calcium and calmodulin antagonists binding to calmodulin and relaxation of coronary segments. J Pharmacol Exp Ther. 1983;226(2):330-334. [Content Brief]
[2]. Siddiqi FH, et al. Felodipine induces autophagy in mouse brains with pharmacokinetics amenable to repurposing [published correction appears in Nat Commun. 2019 Jun 4;10(1):2530]. Nat Commun. 2019;10(1):1817. Published 2019 Apr 18. [Content Brief]
[3]. Yiu, S. and E.E. Knaus, Synthesis, biological evaluation, calcium channel antagonist activity, and anticonvulsant activity of felodipine coupled to a dihydropyridine-pyridinium salt redox chemical delivery system. J Med Chem, 1996. 39(23): p. 4576-82. [Content Brief]