KI696|1799974-70-1|-陌孚医药/Medlife

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KI696

目录号: PL11820 纯度: ≥99%

CAS No. :1799974-70-1

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中文名称	KI696
英文名称	KI696
英文别名	KI696;(3s)-3-(7-Methoxy-1-Methyl-1h-Benzo[d][1,2,3]triazol-5-Yl)-3-(4-Methyl-3-(((R)-4-Methyl-1,1-Dioxido-3,4-Dihydro-2h-Benzo[b][1,4,5]oxathiazepin-2-Yl)methyl)phenyl)propanoic Acid;BDBM50180850;J3.605.567G;Q27462296;(8R)-6-[2-Methyl-5-[(S)-1-(1-methyl-7-methoxy-1H-benzotriazole-5-yl)-3-oxo-3-hydroxypropyl]benzyl]-8beta-methyl-7,8-dihydro-5-thia-6-aza-9-oxa-6H-benzocycloheptene 5,5-dioxide;(S)-3-(7-methoxy-1-
Cas No.	1799974-70-1
分子式	C₂₈H₃₀N₄O₆S
分子量	550.63
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	KI696 是一种干扰 Keap1/NRF2 相互作用的高亲和力探针。KI696 是有效、选择性的 KEAP1/NRF2 相互作用抑制剂。
生物活性	KI696 is a high affinity probe that disrupts the Keap1/NRF2 interaction. KI696 is a potent and selective inhibitor of the KEAP1/NRF2 interaction.
性状	Solid
IC50 & Target[1][2]	Target: Keap1-NRF2
体外研究(In Vitro)	KI696 (compound 7) exhibits very high affinity for the KEAP1 Kelch domain (ITC Kd=1.3 nM with the exception of the organic anion transporting polypeptide 1B1 (OATP1B1) (IC50=2.5 μM), the bile salt export pump BSEP (IC50=4.0 μM), and the phosphodiesterase PDE3A (IC50=10 μM), no significant cross-reactivity is observed. No cytotoxicity is observed towards BEAS-2B cells with KI696 at concentrations up to 10 μM. KI696 increases NRF2 Nuclear Translocation in Normal Human Bronchial Epithelial cells. KI696 increases mRNA expression of the NRF2-dependent genes NQO1 and GCLM in NHBE cells transfected with the non-targeting siRNA, while NRF2 gene silencing significantly decreases compound activity. KI696 increases NQO1 Activity in an NRF2-Dependent Manner. Treatment with tBHP clearly has a detrimental effect on cell health and appearance while
体内研究(In Vivo)	KI696 induces the expression of each of the Nqo1, Ho-1, Txnrd1, Srxn1, Gsta3, Gclc genes in a dose-dependent manner, with maximum increases over vehicle controls of 37-(Nqo1), 17-(Ho-1), 9-(Txnrd1), 28-(Srxn1), 15-(Gsta3) and 13-fold (Gclc) occurring at the 50 μmol/kg dose. EC 50 values are 44.0, 25.7, 42.6, 33.8, 28.4, and 44.1 μmol/kg, respectively, giving an average EC 50 value of 36.4±3.4 μmol/kg. KI696 attenuates ozone-Induced pulmonary inflammation. KI696 restores ozone-induced depletion of lung GSH levels. KI696 is administered to rats at 10, 35 and 50 μmol/kg by IV infusion, resulting in steady state compound concentrations in the blood of 407±44 nM, 946±50 nM and 1437±186 nM, respectively, over the 6 hour infusion period. Exposure to ozone 24 hours post-dose produces a significant depletion in lung levels of the anti-oxidant molecule, GSH, w
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Davies TG, et al. Monoacidic Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery. J Med Chem. 2016 Apr 28

溶解度数据	In Vitro: DMSO : 50 mg/mL (90.81 mM; Need ultrasonic)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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