• 產(chǎn)品描述： BI-4394 （MMP13-IN-3） 是一種有效的選擇性口服活性 MMP-13 抑制劑（IC50=1 nM）的潛在治療骨關(guān)節(jié)炎.BI-4394 比其他 MMP 具有 >1000 選擇性

• 靶點(diǎn)： MMP-13:1 nM (IC50);MMP-14:8.3 μM (IC50);MMP-9:8.9 μM (IC50);MMP-10:16 μM (IC50);MMP-2:18 μM (IC50);MMP

• 體外研究：
  MMP13-IN-3 (Compound 15) is potent in a full-length MMP-13 collagen degradation assay (11 nM) and is able to inhibit degradation of bovine nasal cartilage with an IC50 of 31 nM. MMP13-IN-3 inhibits MMP-2, MMP-9, MMP-10 and MMP-14 with IC50s of 18, 8.9, 16 and 8.3 μM, respectively.

• 體內(nèi)研究：
  When dosed orally at 10 mg/kg or i.v. 1 mg/kg, MMP13-IN-3 (Compound 15) reaches micromolar plasma levels (AUC=1109±64 nM h/mL), displays modest clearance (CL=34 mL/min/kg), and shows acceptable bioavailability (39%). The Vss is quite low at 0.26 mL/mi/kg rat pharmacokinetic profile. MMP13-IN-3 has short terminal elimination half-life (t1/2=0.47 h for rat (1 mg/kg, i.v.) and rat (10 mg/kg, orally), respectively). Animal Model:Srapgue Dally Rats Dosage:10 mg/kg (oral gavage); 1 mg/kg (i.v.) Administration:Dosed orally (10 mg/kg); i.v. (1 mg/kg)(Pharmacokinetic Analysis)Result:T1/2=0.47 h for rat (1 mg/kg, i.v.) and rat (10 mg/kg, orally) , respectively.

• 參考文獻(xiàn)：
  1. Taylor SJ, et al. Fragment-based discovery of indole inhibitors of matrix metalloproteinase-13. J Med Chem. 2011 Dec 8;54(23):8174-87.
  2. Ruminski PG, et al. Discovery of N-(4-Fluoro-3-methoxybenzyl)-6-(2-(((2S,5R)-5-(hydroxymethyl)-1,4-dioxan-2-yl)methyl)-2H-tetrazol-5-yl)-2-methylpyrimidine-4-carboxamide. A Highly Selective and Orally Bioavailable Matrix Metalloproteinase-13 Inhibitor for the Potential Treatment of Osteoarthritis. J Med Chem. 2016 Jan 14;59(1):313-27.

• 溶解性： Soluble  in  DMSO

• 保存條件： -20℃

• 配置溶液濃度參考：
  

  	1mg	5mg	10mg
  1 mM	2.24 ml	11.199 ml	22.398 ml
  5 mM	0.448 ml	2.24 ml	4.48 ml
  10 mM	0.224 ml	1.12 ml	2.24 ml
  50 mM	0.045 ml	0.224 ml	0.448 ml

• 注意：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

輸入產(chǎn)品批號(hào)：

本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *