1. GPCR/G Protein
  2. Endothelin Receptor
  3. Atrasentan hydrochloride

Atrasentan hydrochloride (Synonyms: ABT-627 hydrochloride; (+)-A 127722 hydrochloride; A-147627 hydrochloride)

製品番号: HY-15403A 純度: 99.80%
取扱説明書

Atrasentan hydrochloride (ABT-627 hydrochloride) is an endothelin receptor antagonist with IC50 of 0.0551 nM for ETA.

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Atrasentan hydrochloride 構造式

Atrasentan hydrochloride 構造式

CAS 番号 : 195733-43-8

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1 mL in DMSO USD 260 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 216 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 360 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 1087 在庫あり
Estimated Time of Arrival: December 31
100 mg   お問い合わせ  
200 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 6 publication(s) in Google Scholar

Other Forms of Atrasentan hydrochloride:

Top Publications Citing Use of Products

    Atrasentan hydrochloride purchased from MCE. Usage Cited in: Department Veterinary Clinical Medicine. University of Illinois. 2015.

    Effects of ET-1 and ABT-627 on the expression levels of pAkt and Akt in serum starved Abrams and HMPOS cells. Increased phosphorylation of Akt in HMPOS cells treated with ET-1 and 10% FBS can be seen visually with darkening of the bands. Cells treated with ABT-627 and the combination of ABT-627 and ET-1 show decreased band weight.

    Atrasentan hydrochloride purchased from MCE. Usage Cited in: J Vet Intern Med. 2015 Nov;29(6):1584-94.

    In the HMPOS cell line, membranous cleavage of bone alkaline phosphatase is reduced following exposure to ABT-627 alone or in combination with endothelin-1.
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    製品説明

    Atrasentan hydrochloride (ABT-627 hydrochloride) is an endothelin receptor antagonist with IC50 of 0.0551 nM for ETA[1].

    IC50 & Target

    IC50: 0.055 nM (ETA)

    体外実験

    Atrasentan hydrochloride (ABT-627 hydrochloride) (0-50 μM) significantly inhibits LNCaP and C4-2b prostate cancer cell growth. ABT-627 in conbination with Taxotere elicits a significantly greater loss of viable prostate cancer cells relative to either agent alone and shows greater degree of down-regulation of the NF-κB DNA binding activity[2]. Atrasentan profoundly induces several CYPs and drug transporters (e.g. 12-fold induction of CYP3A4 at 50 μM). It is a moderate P-gp inhibitor (IC50 in P388/dx cells=15.1±1.6 μM) and a weak BCRP inhibitor (IC50 in MDCKII-BCRP cells=59.8±11 μM)[3].

    体内実験

    Atrasentan hydrochloride (ABT-627 hydrochloride) (3 mg/kg, p.o.) inhibits the pressor response induced by big endothelin-1 (1 nmol/kg) in pithed rats[1]. Aatrasentan (ABT-627, 10 mg/kg, i.p.) as well as Taxotere alone inhibited the C4-2b tumor growth within the bone environment to some extent in the SCID-hu model[2].

    臨床実験
    分子量

    547.08

    分子式

    C₂₉H₃₉ClN₂O₆

    CAS 番号

    195733-43-8

    SMILES

    O=C([[email protected]]1[[email protected]](C2=CC=C(OC)C=C2)N(CC(N(CCCC)CCCC)=O)C[[email protected]@H]1C3=CC=C(OCO4)C4=C3)O.Cl

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 33.3 mg/mL (60.87 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8279 mL 9.1394 mL 18.2789 mL
    5 mM 0.3656 mL 1.8279 mL 3.6558 mL
    10 mM 0.1828 mL 0.9139 mL 1.8279 mL
    *Please refer to the solubility information to select the appropriate solvent.
    体内:
    • 1.

      Add each solvent one by one:  0.5% CMC-Na/saline water

      Solubility: 0.75 mg/mL (1.37 mM); Clear solution; Need ultrasonic and warming

    *All of the co-solvents are provided by MCE.
    参考文献
    キナーゼ実験
    [2]

    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.

    MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

    細胞実験
    [2]

    All three prostate cancer cell lines (LNCaP, C4-2b, and PC-3 cells) are seeded at a density of 3 × 103 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 drug, 20 μL of MTT solution (5 mg/mL in PBS) are 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.

    MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

    動物実験
    [1]

    YM598 (0.3, 1, and 3 mg/kg), atrasentan (0.3, 1, and 3 mg/kg), or 0.5% methyl cellulose as vehicle is orally administered to rats with a dosing cannula. 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 cause 50% inhibition (ID50) of the big endothelin-1-induced increase in diastolic blood pressure is determined by linear regression analysis.

    MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

    参考文献
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    Keywords:

    AtrasentanABT-627(+)-A 127722A-147627ABT627ABT 627A147627A 147627Endothelin ReceptorInhibitorinhibitorinhibit

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    製品名:
    Atrasentan hydrochloride
    製品番号:
    HY-15403A
    数量:
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