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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-PPAR-TPST-1120
TPST-1120

Chemical Structure : TPST-1120

CAS No.: 1616372-41-8

TPST-1120 (Amezalpat, TPST1120)

货号: PC-24111Not For Human Use, Lab Use Only.

Amezalpat (TPST-1120, TPST1120) is potent, selective and orally bioavailable inhibitor of peroxisome proliferator-activated receptor α (PPARα) with IC50 of 0.04 uM (human PPARα), >250-fold selectivity over the other PPAR isoforms (PPAR β/δ and γ).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

Amezalpat (TPST-1120, TPST1120) is potent, selective and orally bioavailable inhibitor of peroxisome proliferator-activated receptor α (PPARα) with IC50 of 0.04 uM (human PPARα), >250-fold selectivity over the other PPAR isoforms (PPAR β/δ and γ).
TPST-1120 exhibits potent anti-tumor immune responses and significant tumor regression in syngeneic models of breast, lung, colon, pancreatic and melanoma in addition to xenograft models of CLL, AML, pancreatic and melanoma cancers as a monotherapy or in combination with chemotherapy.
Combination of TPST-1120 plus anti-PD-1 therapy resulted in synergistic tumor reduction and durable antitumor immunity in multiple syngeneic mouse models.

物理化学性质&存储条件

分子量 555.72
分子式 C34H41N3O4
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

2-(3'-(3-(1-(4-(tert-butyl)benzyl)-4-ethyl-5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)propyl)-4-ethoxy-[1,1'-biphenyl]-3-yl)acetic acid

参考文献

1. Patent WO2014099503 A1.

2. Chan C. Whiting, et al. Cancer Res (2019) 79 (13_Supplement): 3606.

3. Mark Yarchoan, et al. Cancer Res Commun. 2024 Apr 18;4(4):1100-1110.

4. US Patent No.676,754 B2. Triazolone compounds and uses thereof; 2017.

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