Atrasentan
Based on 6 publication(s) in Google Scholar
Atrasentan (ABT-627) is an endothelin receptor antagonist with IC50 of 0.0551 nM for ETA.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.42%
- CAS No.: 173937-91-2
- Formule: C29H38N2O6
- Masse moléculaire:510.62
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) Atrasentan
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Activité biologique
IC50: 0.055 nM (ETA)
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
0.055 nM
Compound: 5; ABT-627; Xinlay
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Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane
Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane
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[PMID: 27266371] |
| MMQ | IC50 |
0.04 nM
Compound: 17v
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Inhibition of phosphoinositol hydrolysis of MMQ cells.
Inhibition of phosphoinositol hydrolysis of MMQ cells.
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[PMID: 8676339] |
| MMQ | IC50 |
0.31 nM
Compound: 17v
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Inhibitory activity against the Endothelin A receptor of rat MMQ cells
Inhibitory activity against the Endothelin A receptor of rat MMQ cells
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[PMID: 8676339] |
| MMQ | IC50 |
0.36 nM
Compound: 1
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Binding affinity against Endothelin A receptor in MMQ cells in rat
Binding affinity against Endothelin A receptor in MMQ cells in rat
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[PMID: 11689084] |
| Pituitary gland cell | IC50 |
0.4 nM
Compound: 13
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Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
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[PMID: 9022798] |
Atrasentan (ABT-627, 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 173937-91-2
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Appearance Solid
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Masse moléculaire 510.62
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Formule C29H38N2O6
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Color White to light yellow
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SMILES
OC([C@H]1[C@H](C2=CC=C(C=C2)OC)N(C[C@@H]1C3=CC=C(OCO4)C4=C3)CC(N(CCCC)CCCC)=O)=O
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Synonyms
ABT-627; (+)-A 127722; A-147627
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (6)
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Journal Impact Factor
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Most Recent
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Commun Biol
2022 Jul 28;5(1):750. PMID: 35902736 -
Eur J Pharmacol
Atrasentan alleviates high glucose-induced podocyte injury by the microRNA-21/forkhead box O1 axis. [Abstract]2019 Jun 5:852:142-150. PMID: 30876973 -
J Cell Mol Med
Crosstalk Between Gastric Cancer and Adjacent Mucosa Reveals EDN1-EDNRA-Mediated Regulation of Cancer Stemness and Immunomodulation Networks. [Abstract]2025 Apr;29(8):e70547. PMID: 40245183 -
Mol Immunol
Interactions between the complement and endothelin systems in normal pregnancy and following placental ischemia. [Abstract]2019 Oct:114:10-18. PMID: 31326653 -
J Vet Intern Med
The Association of Endothelin-1 Signaling with Bone Alkaline Phosphatase Expression and Protumorigenic Activities in Canine Osteosarcoma. [Abstract]2015 Nov;29(6):1584-94. PMID: 26426813
Atrasentan purchased from MedChemExpress. Usage Cited in: J Vet Intern Med. 2015 Nov;29(6):1584-94. [Abstract]
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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Atrasentan purchased from MedChemExpress. Usage Cited in: 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.
Solvant et solubilité
DMSO : 100 mg/mL (195.84 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (4.90 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.90 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (287 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Yuyama H, et al. Superiority of YM598 over atrasentan as a selective endothelin ETA receptor antagonist. Eur J Pharmacol. 2004 Sep 13;498(1-3):171-7. [Content Brief]
[2]. Banerjee S, et al. In vitro and in vivo molecular evidence for better therapeutic efficacy of ABT-627 and taxotere combination in prostate cancer. Cancer Res. 2007 Apr 15;67(8):3818-26. [Content Brief]
[3]. Weiss J, et al. Interaction potential of the endothelin-A receptor antagonist atrasentan with drug transporters and drug-metabolising enzymes assessed in vitro. Cancer Chemother Pharmacol. 2011 Oct;68(4):1093-8. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9584 mL | 9.7920 mL | 19.5840 mL | 48.9601 mL |
| 5 mM | 0.3917 mL | 1.9584 mL | 3.9168 mL | 9.7920 mL | |
| 10 mM | 0.1958 mL | 0.9792 mL | 1.9584 mL | 4.8960 mL | |
| 15 mM | 0.1306 mL | 0.6528 mL | 1.3056 mL | 3.2640 mL | |
| 20 mM | 0.0979 mL | 0.4896 mL | 0.9792 mL | 2.4480 mL | |
| 25 mM | 0.0783 mL | 0.3917 mL | 0.7834 mL | 1.9584 mL | |
| 30 mM | 0.0653 mL | 0.3264 mL | 0.6528 mL | 1.6320 mL | |
| 40 mM | 0.0490 mL | 0.2448 mL | 0.4896 mL | 1.2240 mL | |
| 50 mM | 0.0392 mL | 0.1958 mL | 0.3917 mL | 0.9792 mL | |
| 60 mM | 0.0326 mL | 0.1632 mL | 0.3264 mL | 0.8160 mL | |
| 80 mM | 0.0245 mL | 0.1224 mL | 0.2448 mL | 0.6120 mL | |
| 100 mM | 0.0196 mL | 0.0979 mL | 0.1958 mL | 0.4896 mL |
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