SML0485

Azamulin

≥98% (HPLC), powder, pleuromutilin antibiotic

• 別名: (5-Amino-1H-1,2,4-triazol-3-yl)thio]acetic acid (3aS,4R,5S,6R,8R,9R,9aR,10R)-6-ethyldecahydro-5-hydroxy-4,6,9,10-tetramethyl-1-oxo-3a,9-propano-3aH-cyclopentacycloocten-8-yl ester;, 14-O-(5-(2-Amino1,3,4-triazolyl)thioacetyl)dihydromutilin, Antibiotic TDM 85-530
• 実験式（ヒル表記法）: C₂₄H₃₈N₄O₄S
• CAS番号: 76530-44-4
• 分子量: 478.65
• MDL番号: MFCD00865055
• UNSPSCコード: 12161501
• PubChem Substance ID: 329825436
• NACRES: NA.77

特性

• product name: Azamulin, ≥98% (HPLC)
• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• 形状: powder
• 色: white to beige
• 溶解性: DMSO: 10 mg/mL (clear solution)
• 輸送温度: wet ice
• 保管温度: −20°C
• SMILES記法: CC[C@]1(C)C[C@@H](OC(=O)CSc2nnc(N)[nH]2)[C@]3(C)[C@H](C)CC[C@]4(CCC(=O)[C@@H]34)[C@@H](C)[C@@H]1O
• InChI: 1S/C24H38N4O4S/c1-6-22(4)11-16(32-17(30)12-33-21-26-20(25)27-28-21)23(5)13(2)7-9-24(14(3)19(22)31)10-8-15(29)18(23)24/h13-14,16,18-19,31H,6-12H2,1-5H3,(H3,25,26,27,28)/t13-,14+,16-,18+,19+,22-,23+,24+/m1/s1
• InChI Key: FMHQJXGMLMSMLC-WBUYAQKGSA-N

詳細

詳細

Azamulin isolated from fungus Pleurotus mutilis is a diterpene antibiotic. It is related to pleuromutilin being its synthetic azole derivative.

アプリケーション

Azamulin has been used as a selective CYP3A4 inhibitor to pretreat primary hepatocyte cells and in prostate cancer cell lines LNCaP and MDAPCa2b.

生物化学的／生理学的作用

Azamulin is a derivative of the antibiotic pleuromutilin. The compound is a very specific inhibitor of the CYP3A family (IC₅₀ = 0.03-0.24 μM). Azamulin is 15 and 13 fold more active against CYP3A4 compared to CYP3A5 or CYP3A7, respectively, and is at least 100 fold selective over other CYP isoforms, with the exception of CYP2J2 (approximately 50-fold).

安全性情報

• ピクトグラム: GHS07
• シグナルワード: Warning
• 危険有害性情報: H315,H319,H335
• 注意書き: P261 - P264 - P271 - P280 - P302 + P352 - P305 + P351 + P338
• 危険有害性の分類: Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
• ターゲットの組織: Respiratory system
• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable