2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  3. PPAR
  4. PPARα/δ antagonist-1

PPARα/δ antagonist-1 是一种具有口服活性的、高选择性的 PPARα/δ 双重拮抗剂，其对于人源 PPARα 和 PPARδ 的 IC50 分别为 0.113 和 0.025 μM。PPARα/δ antagonist-1 展现了优异的体外活性谱以及在小鼠肿瘤模型中的初步疗效。PPARα/δ antagonist-1 可用于癌症 (黑色素瘤转移、卵巢癌) 相关研究。

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PPARα/δ antagonist-1

PPARα/δ antagonist-1 Chemical Structure

CAS No. : 1673590-38-9

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PPARα/δ antagonist-1 相关抗体

Top Publications Citing Use of Products

查看 PPAR 亚型特异性产品:

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PPARα PPARβ/δ PPARγ PPAR PPARδ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PPARα/δ antagonist-1 is an orally active, highly selective dual antagonist of PPARα/δ, with IC50 values of 0.113 μM and 0.025 μM against human PPARα and PPARδ, respectively. PPARα/δ antagonist-1 exhibits an excellent in vitro activity profile and preliminary efficacy in mouse tumor models. PPARα/δ antagonist-1 can be used in studies related to cancers (melanoma metastasis, ovarian cancer)[1].

IC50 & Target[1]

PPARα

0.113 μM (IC50)

PPARδ

0.025 μM (IC50)

体外研究
(In Vitro)

PPARα/δ antagonist-1 (Compound 11) 对小鼠 PPARα 和 PPARδ 的效力 (IC₅₀ 分别为 1.28 μM 和 0.96 μM) 低于人源[1]。
PPARα/δ antagonist-1 (1-10 μM) 对核受体及大部分 CYP 表现出极低的脱靶活性，CYP3A4 诱导潜力低，在最高 30 μM 的浓度下不会降低 CHO 细胞活力，且在 10 μM 时 hERG 活性可忽略不计[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

PPARα/δ antagonist-1 相关抗体:
体内研究
(In Vivo)

PPARα/δ antagonist-1 (Compound 11) (10-30 mg/kg, p.o., 每日两次共 21-28 天) 在小鼠 B16F10 黑色素瘤肺转移模型和 SKOV-3 卵巢癌异种移植模型中展现出显著的抗肿瘤活性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female C57Bl/6 mice, 6-7 weeks old,[1]
Dosage: 10 and 30 mg/kg
Administration: p.o., twice daily for 21 and 28 days
Result: Significantly reduced the number of tumor nodules formed in the lungs of mice after intravenous injection of B16F10 cells.
Significantly inhibited the growth of SKOV-3 tumors in nude mice.
分子量

619.61

Formula

C34H29F4N3O4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

PPARα/δ antagonist-1 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PPARα/δ antagonist-11673590-38-9PPARPeroxisome proliferator-activated receptorsmouse PPAR isoformsovarian cancerhuman PPARαPPARδperoxisome proliferator-activated receptor alphaCHO cellPPARαmelanoma metastasishuman PPARδperoxisome proliferator-activated receptor deltaInhibitorinhibitorinhibit

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