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 a selective endothelin A receptor antagonist with an 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 a selective endothelin A receptor antagonist with an 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[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.) inhibits 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 : ≥ 100 mg/mL (182.79 mM)

    H2O : 12.5 mg/mL (22.85 mM; Need ultrasonic)

    *"≥" 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

    • 2.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

    • 4.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    参考文献
    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 NSC 10816, 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
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