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首页-小分子抑制剂&激动剂-Immunology/Inflammation-Cyclooxygenase (COX)-PTUPB
PTUPB

Chemical Structure : PTUPB

CAS No.: 1287761-01-6

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PTUPB (COX-2/sEH inhibitor)

货号: PC-62501Not For Human Use, Lab Use Only.

PTUPB is a novel dual acting COX-2/sEH inhibitor with IC50 of 1.26 uM/0.9 nM, also is a potent AKR1C3 inhibitor with IC50 of 65 nM.

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5 mg ￥1580 In stock
10 mg ￥2480 In stock
25 mg ￥3980 In stock
50 mg ￥5980 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

PTUPB is a novel dual acting COX-2/sEH inhibitor with IC50 of 1.26 uM/0.9 nM, also is a potent AKR1C3 inhibitor with IC50 of 65 nM.
PTUPBdoes not inhibits COX-1 (IC50>100 uM).
PTUPB reduces kidney injury parameters, decreases inflammatory and oxidative stress markers in ZDF rats.
PTUPB exhibits more effective than the same dose of either COX-2 inhibitor (celecoxib) or sEH inhibitor (t-AUCB) alone, shows in vivo antiallodynic activity in vivo.
PTUPB also suppresses glioblastoma growth by targeting EGFR and hyaluronan mediated motility receptor, potentiates the antitumor efficacy of cisplatin.
PTUPB inhibits CRPC proliferation by suppressing the AKR1C3/AR/AR-V7 axis and is more effective and superior to indomethacin.
PTUPB shows much better efficacy than indomethacin in castration-relapsed VCaP xenograft, patient-derived xenograft (PDX) organoid, and cell models generated from advanced prostate cancer patients.

物理化学性质&存储条件

分子量 543.565
分子式 C26H24F3N5O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

4-(5-phenyl-3-{3-[3-(4-trifluoromethylphenyl)-ureido]-propyl}-pyrazol-1-yl)-benzenesulfonamide

参考文献

1. Joy C Yang, et al. Oncogene. 2023 Feb;42(9):693-707.

2. Li J, et al. Oncotarget. 2017 Sep 15;8(50):87353-87363.

3. Wang F, et al. Mol Cancer Ther. 2018 Feb;17(2):474-483.

4. Hwang SH, et al. J Med Chem. 2011 Apr 28;54(8):3037-50.

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