Tariquidar (Synonyms: XR9576) |
Catalog No.GC15570
One-Click Copy Product Info
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Tariquidar는 P-glycoprotein(P-gp)에 대한 강력하고 선택적인 억제제로 KD 값은 5.1 nM이다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 206873-63-4
Sample solution is provided at 25 µL, 10mM.
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Tariquidar는 P-glycoprotein(P-gp)에 대한 강력하고 선택적인 억제제로 KD 값은 5.1 nM이다. Tariquidar는 ATPase 활성을 차단해서 ABC 수송체 ABCB1을 억제하고 IC50 값은 223 ± 8 nM이다[2]. Tariquidar는 다제내성 세포 모델에서 세포 증식을 억제하기 위해 일반적으로 사용되고 있다[3].
체외 실험에서 33.34 µM Tariquidar를 2일간 처리하면 MRC5 세포 생존율을 현저하게 억제하였다[4]. 0.3 µM Tariquidar를 72시간 처리하면 HEK/MRP7 세포에서 MRP7 mRNA 수준에는 영향을 주지 않으면서 MRP7 단백질 발현을 현저하게 감소시켰고 택솔에 대한 세포 민감성을 증가시켰다[5]. 1.5 μM Tariquidar로 2시간 전처리한 후 1 μM 아르미실린을 처리하면 MDA-MB-231 세포에 대한 살해 효과가 현저하게 강화되었다[6].
체내 실험에서 2일마다 복강내 주입으로 13 mg/kg Tariquidar를 18일간 투여하면 Astragaloside IV(ASIV, 20 mg/kg/일, 복강주사)의 실험적 자가면역성 뇌척수염(EAE) 쥐에 대한 효능을 증강시켰고 임상 증상 감소, 발병률 저하, 중추신경계(CNS) 염증 침윤 감소 및 탈수초 정도 완화로 나타났다[7]. 수컷 Sprague Dawley 쥐에 7.5 mg/kg Tariquidar를 2시간 동안 단일 정주 투여하면 뇌와 척수에서 P-gp에 의한 앙댕스충 배출을 억제하였다[8].
References:
[1] Weidner L D, Fung K L, Kannan P, et al. Tariquidar is an inhibitor and not a substrate of human and mouse P-glycoprotein[J]. Drug Metabolism and Disposition, 2016, 44(2): 275-282.
[2] Kühnle M, Egger M, Müller C, et al. Potent and selective inhibitors of breast cancer resistance protein (ABCG2) derived from the p-glycoprotein (ABCB1) modulator tariquidar[J]. J Med Chem, 2009, 52(4): 1190-7.
[3] Mistry P, Stewart A J, Dangerfield W, et al. In vitro and in vivo reversal of P-glycoprotein-mediated multidrug resistance by a novel potent modulator, XR9576[J]. Cancer research, 2001, 61(2): 749-758.
[4] Parsons A J, Cohen T, Schwarz T M, et al. Valspodar limits human cytomegalovirus infection and dissemination[J]. Antiviral research, 2021, 193: 105124.
[5] Sun Y L, Chen J J, Kumar P, et al. Reversal of MRP7 (ABCC10)-mediated multidrug resistance by tariquidar[J]. PloS one, 2013, 8(2): e55576.
[6] Jadhao M, Tsai E M, Yang H C, et al. The long-term DEHP exposure confers multidrug resistance of triple-negative breast cancer cells through ABC transporters and intracellular ROS[J]. Antioxidants, 2021, 10(6): 949.
[7] Zhang W, Liu M, Yang L, et al. P-glycoprotein inhibitor tariquidar potentiates efficacy of astragaloside IV in experimental autoimmune encephalomyelitis mice[J]. Molecules, 2019, 24(3): 561.
[8] Chiang M, Back H, Lee J B, et al. Pharmacokinetic Modeling of the Effect of Tariquidar on Ondansetron Disposition into the Central Nervous System[J]. Pharmaceutical research, 2024, 41(7): 1401-1411.
| 세포 실험 [1]: | |
세포 라인 | MRC5 세포 |
제조 방법 | MRC5 세포는 10 % 태아소혈청, 1 mM HEPES, 100 U/ml 페니실린 및 100 μg/ml 스트렙토마이신이 보충된 DMEM 배지에서 배양하고 37 °C, 5 % CO₂ 환경에 두었습니다. 1×10⁴ 개의 MRC5 세포를 96-웰 판에 접종해서 밤새 접착시킨 후 Tariquidar(0.26, 0.52, 1.04, 2.08, 4.16, 8.32, 16.67, 33.34 μM)로 2일간 처리한 후 570 nm 흡광도를 측정하였습니다. |
반응 조건 | 0.26, 0.52, 1.04, 2.08, 4.16, 8.32, 16.67 및 33.34μM; 48 시간 동안 |
응용 분야 | 33.34 μM Tariquidar는 MRC5 세포의 생존율을 현저하게 억제하였습니다. |
| 동물 실험 [2]: | |
동물 모형 | 암컷 C57BL/6 쥐 |
제조 방법 | 암컷 C57BL/6 쥐(18–22 g, 6주령)를 실온(22 ± 1 °C), 12 시간 명암 주기 환경에 사육하고 사료와 물을 자유롭게 섭취하게 하였습니다. MOG₃₅₋₅₅을 피하 접종해서 EAE를 유도하였습니다. MOG₃₅₋₅₅ 면역 1일 전부터 18일간 매일 복강내 ASIV(20 mg/kg)를 투여하였고 ASIV 투여 30 분 전에 18일간 격일로 복강내 Tariquidar(13 mg/kg)를 투여하였습니다. |
제형 | 13mg/kg; 18일 동안 이틀에 한 번씩; i.p. |
응용 분야 | Tariquidar 처리는 EAE 쥐에서 ASIV의 효능을 강화시켜 임상 증상이 완화되고 발병률이 감소하고 CNS의 염증 침윤이 경감되었습니다. |
References: | |
| Cas No. | 206873-63-4 | SDF | |
| Synonyms | XR9576 | ||
| Chemical Name | N-[2-[[4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]phenyl]carbamoyl]-4,5-dimethoxyphenyl]quinoline-3-carboxamide | ||
| Canonical SMILES | COC1=C(C=C2CN(CCC2=C1)CCC3=CC=C(C=C3)NC(=O)C4=CC(=C(C=C4NC(=O)C5=CC6=CC=CC=C6N=C5)OC)OC)OC | ||
| Formula | C38H38N4O6 | M.Wt | 646.73 |
| Solubility | ≥ 16.168mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.5462 mL | 7.7312 mL | 15.4624 mL |
| 5 mM | 309.2 μL | 1.5462 mL | 3.0925 mL |
| 10 mM | 154.6 μL | 773.1 μL | 1.5462 mL |
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Quality Control & SDS
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- Purity: >98.50% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)