Atrasentan hydrochloride

规格	价格/CNY		数量
1 mg	￥ 428	现货
2 mg	￥ 617	现货
5 mg	￥ 947	现货
10 mg	￥ 1,390	现货
25 mg	￥ 2,820	现货
50 mg	￥ 3,970	现货
1 mL * 10 mM (in DMSO)	￥ 1,190	现货

规格

价格/CNY

货期

数量

1 mg

￥ 428

现货

2 mg

￥ 617

现货

5 mg

￥ 947

现货

10 mg

￥ 1,390

现货

25 mg

￥ 2,820

现货

50 mg

￥ 3,970

现货

1 mL * 10 mM (in DMSO)

￥ 1,190

现货

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: 0.4 mg/mL (0.73 mM), when pH is adjusted to 4 with HCl. Sonication and heating to 60℃ are recommended.

DMSO: 30 mg/mL (54.84 mM)

0.1 M HCL: < 1 mg/mL (insoluble), when pH is adjusted to 1 with HCl. Sonication and heating to 60℃ are recommended.

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8279 mL	9.1394 mL	18.2789 mL	45.6972 mL
	5 mM	0.3656 mL	1.8279 mL	3.6558 mL	9.1394 mL
	10 mM	0.1828 mL	0.9139 mL	1.8279 mL	4.5697 mL
	20 mM	0.0914 mL	0.457 mL	0.9139 mL	2.2849 mL
	50 mM	0.0366 mL	0.1828 mL	0.3656 mL	0.9139 mL

产品描述	Atrasentan hydrochloride (ABT-627 hydrochloride) is an antagonist of the endothelin receptor(IC50 = 55.1 μM for ETA).
靶点活性	ETA:55.1 μM
体外活性	Atrasentan（0-50 μM）显著抑制LNCaP和C4-2b前列腺癌细胞生长。ABT-627与Taxotere联合使用，相比单独使用任一药物，可显著降低前列腺癌活细胞的数量，并更大程度地下调NF-κB DNA结合活性[2]。Atrasentan显著诱导多种CYPs和药物转运体的表达。它是一种中等强度的P-gp抑制剂（IC50：15.1 μM，在P388/dx细胞中）和一种弱BCRP抑制剂（IC50：59.8 μM，在MDCKII-BCRP细胞中）[3]。
体内活性	Atrasentan（3 mg/kg, p.o.）通过抑制大型内皮素-1（1 nmol/kg）诱导的加压反应，在去髓大鼠中显示出效果[1]。此外，Atrasentan（10 mg/kg, i.p.）在SCID-hu模型中对C4-2b肿瘤在骨环境中的生长有一定程度的抑制作用[2]。
激酶实验	Cells are incubated and treated with Atrasentan. They are then washed twice with PBS and lysed in ice-cold lysis buffer [20 mM Tris (pH 7.4), 150 mM NaCl, 1% Triton X-100, 1 mM EDTA, 1 mM EGTA, 2.5 mM sodium PPi, 1 mM β-glycerophosphate, 1 mM sodium orthovanadate, 1 μg/mL leupeptin, and 1 mM PMSF]. The extracts are centrifuged to remove cellular debris, and the protein content of the supernatants is determined using the bicinchoninic acid (BCA) protein assay reagent. Proteins (150 μg) are incubated with gentle rocking at 4°C overnight with immobilized Akt antibody cross-linked to agarose hydrazide beads. After the Akt is selectively immunoprecipitated from the cell lysates, the immunoprecipitated products are washed twice with lysis buffer and twice with kinase assay buffer [25 mM Tris (pH 7.5), 10 mM MgCl2, 5 mM β-glycerol phosphate, 0.1 mM sodium orthovanadate, 2 mM DTT] and then resuspended in 40 μL of kinase assay buffer containing 200 μM ATP and 1 μg GSK-3α/β fusion protein. The kinase assay reaction is allowed to proceed at 30°C for 30 min and stopped by the addition of Lamelli SDS sample buffer. Reaction products are resolved by 10% SDS-PAGE, followed by Western blotting with antiphosphorylated GSK-3α/β antibody. For analysis of the total amount of Akt, 40 μg of protein from the lysate samples are resolved by 10% SDS-PAGE, followed by Western blotting with anti-Akt antibody [2].
细胞实验	All three prostate cancer cell lines (LNCaP, C4-2b, and PC-3 cells) are seeded at a density of 3 × 10^3 cells per well in 96-well microtiter culture plates. After overnight incubation, the medium is removed and replaced with a fresh medium containing different concentrations of ABT-627 (0-50 μM) diluted from a 10-mM stock. After 72 h of incubation with the drug, 20 μL of MTT solution (5 mg/mL in PBS) is added to each well and incubated further for 2 h. Upon termination, the supernatant is aspirated and the MTT formazan formed by metabolically viable cells is dissolved in isopropanol (100 μL). The plates are mixed for 30 min on a gyratory shaker, and the absorbance is measured at 595 nm on a plate reader [2].
动物实验	YM598 (0.3, 1, and 3 mg/kg), atrasentan (0.3, 1, and 3 mg/kg), or 0.5% methylcellulose as vehicle is orally administered to rats with a dosing cannula. The dosing volume of the test substances and vehicle is set at 5 mL/kg. Approximately 20 min after administration of compounds, the rats are anesthetized with sodium pentobarbital, and then pithed and ventilated 30 min after dosing. Approximately 1 h after oral administration of compounds, big endothelin-1 (1 nmol/kg) is intravenously administered, and blood pressure is measured. In these two experiments, the dose of test compound that causes 50% inhibition (ID50) of the big endothelin-1-induced increase in diastolic blood pressure is determined by linear regression analysis [1].

别名	(+)-A 127722 hydrochloride, ABT-627 hydrochloride, 盐酸阿曲生坦, A-147627 hydrochloride
分子量	547.08
分子式	C29H39ClN2O6
CAS No.	195733-43-8

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