152684-53-2
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- CAS号:
- 152684-53-2
- 英文名:
- TLK117
- 英文别名:
- TER117;TLK117;TLK-117,TLK117;Glycine, L-γ-glutamyl-S-(phenylmethyl)-L-cysteinyl-2-phenyl-, (2R)-
- 中文名:
- 152684-53-2
- 中文别名:
- 化合物 T8424
- CBNumber:
- CB24796697
- 分子式:
- C23H27N3O6S
- 分子量:
- 473.54
- MOL File:
- 152684-53-2.mol
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152684-53-2化学性质
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沸点:
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832.7±65.0 °C(Predicted)
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密度:
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1.346±0.06 g/cm3(Predicted)
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酸度系数(pKa):
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2.21±0.10(Predicted)
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152684-53-2性质、用途与生产工艺
TLK197是TLK199的活性代谢物,选择性抑制谷胱甘肽S-转移酶P1-1 (Glutathione S-transferase P1–1 (GSTP1-1)),结合 GSTP的 Ki 值为0.4 μM。 TLK117还竞争性地抑制乙二醛酶I (glyoxalase I), Ki值为0.56 μM。
Ki: 0.4 μM, 0.56 μM (glyoxalase I)
TLK117 is the most specific GSTP inhibitor to date, with a binding affinity greater than GSH itself and a selectivity for GSTP over 50-fold greater than the GSTM and GSTA classes (K
i
=0.4 μM). TER 117 is developed as a GST P1-1 isoenzyme inhibitor to circumvent the indicated contribution of GST P1-1 to drug resistance of tumor cells. To facilitate the cellular uptake of TER 117, it is delivered as a diethyl ester (TER 117 DEE, also called TER 199). TER 117 is found to be a competitive inhibitor of both GST P1-1 and glyoxalase I.
Oropharyngeal administration of the GSTP inhibitor, TLK117, at a time when fibrosis is already apparent, attenuated bleomycin- and AdTGFβ-induced remodeling, α-SMA, caspase activation, FAS S-glutathionylation, and total protein S-glutathionylation. Four hours after administration of 50 mg/kg TLK117, GSTP activity is strongly decreased and remains decreased by about 60% for at least 24 hours.
152684-53-2
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更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/04/30 | HY-13634B | 152684-53-2 TLK117 | 152684-53-2 | 5mg | 1800元 |
2024/04/30 | HY-13634B | 152684-53-2 TLK117 | 152684-53-2 | 10mg | 2800元 |
152684-53-2, 152684-53-2 相关搜索:
- 化合物 T8424
- 152684-53-2
- TLK-117,TLK117
- Glycine, L-γ-glutamyl-S-(phenylmethyl)-L-cysteinyl-2-phenyl-, (2R)-
- TER117
- TLK117