1-Aminobenzotriazole (ABT) (Synonyms: ABT, 3-Aminobenzotriazole, 1-Benzotriazolylamine, NSC 114498, NSC 656987) |
Catalog No.GC14781
One-Click Copy Product Info
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1-Aminobenzotriazole (ABT)은 구강활성의 비특이성이고 불가역적인 세포색소 P450 (CYP) 억제제이다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1614-12-6
Sample solution is provided at 25 µL, 10mM.
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1-Aminobenzotriazole (ABT)은 구강활성의 비특이성이고 불가역적인 세포색소 P450 (CYP) 억제제이다. 1-Aminobenzotriazole (ABT)은 N-아세트릴전이효소 (NAT)의 기질이자 억제제이다[2].
체외 실험에서 1-Aminobenzotriazole (ABT) (1mM)을 이용하여 0-60분 동안 샌드위치에 배양된 인간 간세포 (SCHH)를 처리함으로써 CYP3A, CYP2C9, CYP2D6, CYP1A2의 세포내 활성을 현저하게 억제했다. CYP3A의 남은 활성도는 대조 그룹의 3%였고 CYP2C9, CYP2D6, CYP1A2의 남은 활성도는 5%에서 35% 사이에 유지했다[3].
체내 실험에서 SD 쥐에게 구강 투여하여 1-Aminobenzotriazole (0, 50, 100, 200, 300mg/kg)를 투여함으로써 MDZ의 간대사를 현저하게 억제했고 1'-OH MDZ 형성을 완전히 억제할 수는 없었다[4]. 3일 동안 수컷 쥐에게 구강 투여하여 1-Aminobenzotriazole (50mg/kg)를 투여함으로써 아크릴아미드 유도된 정원세포의 치명적 효과를 억제했다[5]. 1-Aminobenzotriazole (78mg/kg)를 투여하여 쥐에게 치료함으로써 기관무게와 사망률을 증가시키고 염증 유발 다발성 장기 부전 (MOF)에 대한 감도를 높였다[6].
References:
[1] de Montellano P R O. 1-Aminobenzotriazole: a mechanism-based cytochrome P450 inhibitor and probe of cytochrome P450 biology[J]. Medicinal chemistry, 2018, 8(3).
[2] Sun Q, Harper T W, Dierks E A, et al. 1-Aminobenzotriazole, a known cytochrome P450 inhibitor, is a substrate and inhibitor of N-acetyltransferase[J]. Drug metabolism and disposition, 2011, 39(9): 1674-1679.
[3] Kimoto E, Walsky R, Zhang H, et al. Differential modulation of cytochrome P450 activity and the effect of 1-aminobenzotriazole on hepatic transport in sandwich-cultured human hepatocytes[J]. Drug Metabolism and Disposition, 2012, 40(2): 407-411.
[4] Parrish K E, Mao J, Chen J, et al. In vitro and in vivo characterization of CYP inhibition by 1‐aminobenzotriazole in rats[J]. Biopharmaceutics & drug disposition, 2016, 37(4): 200-211.
[5] Adler I D, Baumgartner A, Gonda H, et al. 1-Aminobenzotriazole inhibits acrylamide-induced dominant lethal effects in spermatids of male mice[J]. Mutagenesis, 2000, 15(2): 133-136.
[6] Carcillo J, Kost C, Korzekwa K, et al. 1-aminobenzotriazole (ABT), the cytochrome P450 suicide inhibitor, sensitizes rats to zymosan induced-multiple organ failure184[J]. Pediatric Research, 1998, 43(4): 34-34.
| 세포 실험 [1]: | |
세포 라인 | 샌드위치에 배양된 인간 간세포(SCHH) |
제조 방법 | 샌드위치 배양된 인간 간세포 (SCHH)에 1-Aminobenzotriazole (1mM)을 0-60분 동안 사전 배양한 후 SCHH에 CYP1A2, CYP2C9, CYP2D6, CYP3A 전문화 기초 혼합물을 추가하고 추가로 30분 더 배양했습니다. |
반응 조건 | 1mM; 0-60분 동안 |
응용 분야 | CYP3A 활성의 표지로 사용되는 세포내 hydroxymidazolam 형성은 ABT와 사전 배양 후 거의 완전히 제거되었다 (대조 그룹의 3%). 1-Aminobenzotriazole 사전 배양을 60분 동안 진행하는 경우 CYP2C9, CYP2D6, CYP1A2의 남은 활성도는 5%에서 35% 사이에 유지했습니다. |
| 동물 실험 [2]: | |
동물 모형 | 수컷 Sprague-Dawley 쥐 |
제조 방법 | 쥐는 구강 투여 (2mg/kg)나 정맥 투여 (1mg/kg)의 미다졸람(MDZ) 2시간 전에 0, 50, 100, 200, 300mg/kg의 1-Aminobenzotriazole (물에 녹여)를 구강 투여했습니다. 1-Aminobenzotriazole 투여 전에 쥐는 12시간 동안 금식했고 MDZ 투여 후 10개의 시간점 (0.083, 0.25, 0.5, 1, 2, 4, 8, 12, 24, 36시간)에 경동맥을 통해 피를 채집했고 나트륨/칼륨 EDTA를 항응고제로 사용했습니다. 혈장 표본은 LC-MS/MS를 통하여 분석했습니다. |
제형 | 0, 50, 100, 200, 300mg/kg; p.o. |
응용 분야 | 1-Aminobenzotriazole은 MDZ의 산화적 대사를 현저하게 억제할 수 있지만 1'-OH MDZ 형성을 완전히 억제할 수는 없습니다. |
References: | |
| Cas No. | 1614-12-6 | SDF | |
| Synonyms | ABT, 3-Aminobenzotriazole, 1-Benzotriazolylamine, NSC 114498, NSC 656987 | ||
| Chemical Name | 1H-benzo[d][1,2,3]triazol-1-amine | ||
| Canonical SMILES | NN1N=NC2=CC=CC=C12 | ||
| Formula | C6H6N4 | M.Wt | 134.14 |
| Solubility | ≥ 6.7mg/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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 7.4549 mL | 37.2745 mL | 74.549 mL |
| 5 mM | 1.491 mL | 7.4549 mL | 14.9098 mL |
| 10 mM | 745.5 μL | 3.7274 mL | 7.4549 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >97.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 5 reference(s) in Google Scholar.)