Puromycin aminonucleoside (Synonyms: 氨基核苷嘌呤霉素; NSC 3056)
Puromycin aminonucleoside (NSC 3056) 是一種氨基核苷類抗sheng素,為嘌呤霉素類似物。Puromycin aminonucleoside 誘導細胞凋亡 (apoptosis)。Puromycin aminonucleoside 可逆抑制二肽基肽酶 (dipeptidyl peptidase II) 和胞漿丙an酸氨基肽酶。Puromycin aminonucleoside 誘導細胞遷移小體的分泌。
生物活性
Puromycin aminonucleoside (NSC 3056) is the aminonucleoside portion of the antibiotic puromycin, and used in nephrosis animal models[1]. Puromycin aminonucleoside induces apoptosis[2]. Puromycin aminonucleoside is a reversible inhibitor of dipeptidyl peptidase II and cytosol alanyl aminopeptidase[3]. Puromycin aminonucleoside induces secretion of cell migrasome[4].
IC50 & Target
DPP-2
體外研究(In Vitro)
Puromycin aminonucleoside (NSC 3056) (30 μg/mL) markedly increases p53 protein levels in podocytes. Puromycin aminonucleoside (NSC 3056)-induced podocyte apoptosis is p53 dependent. Puromycin aminonucleoside (NSC 3056) induces podocyte apoptosis in a time-dependent manner[2]. The IC50 values for PMAT-expressing and vector-transfected cells are 48.9 and 122.1 μM, respectively, suggesting expression of PMAT-enhanced cell sensitivity to Puromycin aminonucleoside. Puromycin aminonucleoside (NSC 3056) (250 μM) is toxic to both PMAT-expressing and vector-transfected cells. Puromycin aminonucleoside (NSC 3056) uptake in PMAT-expressing cells is fourfold higher at pH 6.6 than that at pH 7.4[5].
體內(nèi)研究(In Vivo)
The number of podocytes per glomerulus is 95.5±17.6 in the control rats, 90.7 on Day 4 in Puromycin aminonucleoside (NSC 3056) (8 mg/100 g, i.v.)-treated nephrosis rats. The amount of nephrin per glomerulus in control rats is 1.02±0.11 fmol and those in Puromycin aminonucleoside (NSC 3056) nephrosis rats are reduced to 0.46±0.06 fmol and 0.35±0.04 fmol on Day 4 and Day 7. The nephrin amount per podocyte is significantly decreased association with the development of proteinuria in Puromycin aminonucleoside (NSC 3056) nephrosis rats[5]. Rats given Puromycin aminonucleoside (NSC 3056) (100 mg/kg, s.c.) gain less weight and their serum creatinine levels are higher than the control rats[7].
分子量:294.31
性狀:Solid
Formula:C12H18N6O3
CAS 號:58-60-6
中文名稱:氨基核苷嘌呤霉素;嘌呤霉素氨基核苷
運輸條件:Room temperature in continental US; may vary elsewhere.
儲存方式
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)
H2O : 40 mg/mL (135.91 mM; ultrasonic and warming and heat to 50°C)
DMSO : 25 mg/mL (84.94 mM; ultrasonic and warming and heat to 60°C)
濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
---|
1 mM | 3.3978 mL | 16.9889 mL | 33.9778 mL |
5 mM | 0.6796 mL | 3.3978 mL | 6.7956 mL |
10 mM | 0.3398 mL | 1.6989 mL | 3.3978 mL |
請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 儲存時,請在 6 個月內(nèi)使用,-20°C 儲存時,請在 1 個月內(nèi)使用。
以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
——為保證實驗結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當保存;體內(nèi)實驗的工作液,建議您現(xiàn)用現(xiàn)配,當天使用; 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
- 1.
請依序添加每種溶劑: PBS
Solubility: 12.5 mg/mL (42.47 mM); Clear solution; Need ultrasonic
- 2.
請依序添加每種溶劑: 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: ≥ 2.5 mg/mL (8.49 mM); Clear solution
- 3.
請依序添加每種溶劑: 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (8.49 mM); Clear solution
- 4.
請依序添加每種溶劑: 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (7.07 mM); Clear solution
- 5.
請依序添加每種溶劑: 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (7.07 mM); Clear solution
- 6.
請依序添加每種溶劑: 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (7.07 mM); Clear solution
- 7.
請依序添加每種溶劑: 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (7.07 mM); Clear solution
- 8.
請依序添加每種溶劑: 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (7.07 mM); Clear solution
- 9.
請依序添加每種溶劑: 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (7.07 mM); Clear solution
- 10.
請依序添加每種溶劑: 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (7.07 mM); Clear solution
參考文獻
[1]. Lacalle RA, et al. Cloning of the complete biosynthetic gene cluster for an aminonucleoside antibiotic, puromycin, and its regulated expression in heterologous hosts. EMBO J. 1992 Feb;11(2):785-92. [Content Brief]
[2]. Wada T, et al. Prevents podocyte apoptosis induced by puromycin aminonucleoside: role of p53 and Bcl-2-related family proteins. J Am Soc Nephrol. 2005 Sep;16(9):2615-25. [Content Brief]
[3]. Gong W, et al. Estrogen-related receptor-α mediates puromycin aminonucleoside-induced mesangial cell apoptosis and inflammatory injury. Am J Physiol Renal Physiol. 2019 May 1;316(5):F906-F913. [Content Brief]
[4]. Ying Liu, et al. Podocyte-Released Migrasomes in Urine Serve as an Indicator for Early Podocyte Injury. Kidney Dis (Basel). 2020 Nov;6(6):422-433. [Content Brief]
[5]. Xia L, et al. Podocyte-specific expression of organic cation transporter PMAT: implication in puromycin aminonucleosidenephrotoxicity. Am J Physiol Renal Physiol. 2009 Jun;296(6):F1307-13. [Content Brief]
[6]. Kawakami H, et al. Dynamics of absolute amount of nephrin in a single podocyte in puromycin aminonucleoside nephrosis rats calculated by quantitative glomerular proteomics approach with selected reaction monitoring mode. Nephrol Dial Transplant. 2012 Apr; [Content Brief]
[7]. Nosaka K, et al. An adenosine deaminase inhibitor prevents puromycin aminonucleoside nephrotoxicity. Free Radic Biol Med 1997 ;22 (4): 597-605. [Content Brief]
注:產(chǎn)品僅用于科研