Pargyline

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Chemical Structure| 555-57-7 同义名 : 优降宁
CAS号 : 555-57-7
货号 : A735949
分子式 : C11H13N
纯度 : 98%
分子量 : 159.228
MDL号 : MFCD00008576
存储条件:

Pure form Inert atmosphere,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(659.43 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Pargyline is an irreversible monoamine oxidase (MAO) inhibitor with Kis of 13 μM and 0.5 μM for MAO-A and MAO-B, respectively. Pargyline (0.5-2 mM; 24-120 hours) treatment inhibits the proliferation of LNCaP-LN3 cells in a time- and dose-dependent manner. Pargyline (0.5-2 mM; 24-48 hours) treatment decreases S phase and increases the G1 phase in the cells in a dose-dependent manner. Pargyline (0.5 mM; 24 hours) treatment increases the apoptotic cells. Pargyline (2 mM; 48 hours treatment induces an increase of cytochrome c and a decrease of caspase-3 in the cells, but does not lead to a change of BCL-2 expression[2]. Pargyline (10 mg/kg; iv) treatment induces a moderate (about 20 mm Hg) but persistent (48 h) decrease of systolic blood pressure in unanesthetized adult spontaneously hypertensive rats (SHR) but not in normotensive rats. A low dose of Pargyline (200 μg; icv) injected directly into the brain lowered arterial pressure. The hypotensive action of Pargylline in SHR appears to be the consequence of Norepinephrine accumulating at an inhibitory α-adrenoceptor in brain[3]. Oral pargyline treatment protected transplanted beta cells in diabetic mice, thus leading to disease reversal. Furthermore, pargyline prevented or delayed diabetes onset in several mouse models for T1D(Type 1 diabetes)[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

6.28mL

1.26mL

0.63mL

31.40mL

6.28mL

3.14mL

62.80mL

12.56mL

6.28mL

参考文献

[1]Bianchi P, et al. A new hypertrophic mechanism of serotonin in cardiac myocytes: receptor-independent ROS generation. FASEB J. 2005 Apr;19(6):641-3.

[2]Lee HT, Choi MR, Doh MS, Jung KH, Chai YG. Effects of the monoamine oxidase inhibitors pargyline and tranylcypromine on cellular proliferation in human prostate cancer cells. Oncol Rep. 2013 Oct;30(4):1587-92

[3]Fuentes JA, Ordaz A, Neff NH. Central mediation of the antihypertensive effect of pargyline in spontaneously hypertensive rats. Eur J Pharmacol. 1979 Jul 15;57(1):21-7

[4]Cai EP, Ishikawa Y, Zhang W, Leite NC, Li J, Hou S, Kiaf B, Hollister-Lock J, Yilmaz NK, Schiffer CA, Melton DA, Kissler S, Yi P. Genome-scale in vivo CRISPR screen identifies RNLS as a target for beta cell protection in type 1 diabetes. Nat Metab. 2020 Sep;2(9):934-945