L1790

L-685,458

>96% (HPLC), solid

• 別名: (5S)-(t-ブトキシカルボニルアミノ)-6-フェニル-(4R)ヒドロキシ-(2R)ベンジルヘキサノイル)-L-leu-L-phe-アミド
• 実験式（ヒル表記法）: C₃₉H₅₂O₆N₄
• CAS番号: 292632-98-5
• 分子量: 672.85
• MDL番号: MFCD03093402
• UNSPSCコード: 12352200
• PubChem Substance ID: 329817393
• NACRES: NA.77

特性

• アッセイ: >96% (HPLC)
• 形状: solid
• 色: white
• 溶解性: DMSO: >10 mg/mL
• オーガナイザー: Merck & Co., Inc., Kenilworth, NJ, U.S.
• 保管温度: −20°C
• SMILES記法: O[C@@H]([C@H](CC1=CC=CC=C1)NC(OC(C)(C)C)=O)C[C@@H](CC2=CC=CC=C2)C(N[C@@H](CC(C)C)C(N[C@@H](CC3=CC=CC=C3)C(N)=O)=O)=O
• InChI: 1S/C39H52N4O6/c1-26(2)21-33(37(47)41-32(35(40)45)24-29-19-13-8-14-20-29)42-36(46)30(22-27-15-9-6-10-16-27)25-34(44)31(23-28-17-11-7-12-18-28)43-38(48)49-39(3,4)5/h6-20,26,30-34,44H,21-25H2,1-5H3,(H2,40,45)(H,41,47)(H,42,46)(H,43,48)/t30-,31+,32+,33+,34-/m1/s1
• InChI Key: MURCDOXDAHPNRQ-ZJKZPDEISA-N
• 遺伝子情報: human ... APH1A(51107) , APH1B(83464) , NCSTN(23385) , NOTCH1(4851) , NOTCH2(4853) , NOTCH3(4854) , NOTCH4(4855) , PSEN1(5663) , PSEN2(5664) , PSENEN(55851) ; mouse ... Aph1a(226548) , Aph1b(208117) , Ncstn(59287) , Notch1(18128) , Notch2(18129) , Notch3(18131) , Notch4(18132) , Psen1(19164) , Psen2(19165) , Psenen(66340) ; rat ... Aph1a(365872) , Aph1b(300802) , Ncstn(289231) , Notch1(25496) , Notch2(29492) , Notch3(56761) , Notch4(406162) , Psen1(29192) , Psen2(81751) , Psenen(292788)

詳細

アプリケーション

L-685,458 has been used to attenuate Notch signalling in ovary culture. It has also been used to analyze the specificity of the γ-secretase activity in brain tissue samples.

生物化学的／生理学的作用

L-685,458 mimics the transition state in aspartyl protease. It possesses an IC50 of 17nM with respect to inhibition of Aβ synthesis. It is known to block Notch (neurogenic locus notch homolog protein) signaling, which in turn reduces ERK (extracellular signal regulated kinase) phosphorylation by EGF (epidermal growth factor). L-685,458 targets the active site and substrate binding site of the enzyme.

L-685,458は、新規構造の強力かつ選択的なγ-セクレタ-ゼインヒビタ-であり、Aβ_1-42およびAβ_1-40のそれぞれの産生に対して同等の効力があります。

特徴および利点

This compound was developed by Merck & Co., Inc., Kenilworth, NJ, U.S.. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

法的情報

Merck & Co., Inc., Kenilworth, NJとのライセンスを受けて製造・販売しています。

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable
• 個人用保護具 (PPE): Eyeshields, Gloves, type N95 (US)