MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)。

BI-4394

CAS No. : 1222173-37-6

產(chǎn)品活性：BI-4394 (MMP13-IN-3) is a potent, selective, and orally active MMP-13 inhibitor (IC₅₀=1 nM) for the potential treatment of osteoarthritis. BI-4394 is >1000 selective over other MMPs.

研究領(lǐng)域：Metabolic Enzyme/Protease

作用靶點(diǎn)：MMP

In Vitro: BI-4394 (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. BI-4394 inhibits MMP-2, MMP-9, MMP-10 and MMP-14 with IC₅₀s of 18, 8.9, 16 and 8.3 μM, respectively.

In Vivo: When dosed orally at 10 mg/kg or i.v. 1 mg/kg, BI-4394 (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 V_ss is quite low at 0.26 mL/mi/kg rat pharmacokinetic profile. BI-4394 has short terminal elimination half-life (t_1/2=0.47 h for rat (1 mg/kg, i.v.) and rat (10 mg/kg, orally), respectively).

相關(guān)產(chǎn)品：Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  Metabolism/Protease Compound Library  |  Differentiation Inducing Compound Library  |  Chemical Probe Library  |  Anti-Pancreatic Cancer Compound Library  |  Angiogenesis-Related Compound Library  |  Anti-Pulmonary Fibrosis Compound Library  |  Heterocyclic Compound Library  |  Pain-Related Compound Library  |  Membrane Protein-targeted Compound Library  |  Doxycycline calcium  |  Imidapril  |  Edaravone  |  BAY-7598  |  Doxycycline monohydrate  |  WAY-170523  |  Chondroitin sulfate  |  MMP-2 Inhibitor II  |  Threo-Chloramphenicol-d₆  |  cis-ACCP  |  Hydrangenol  |  Diethyl-pythiDC  |  TP0556351  |  MMP-2/9-IN-1  |  Mca-PLGL-Dpa-AR-NH2  |  o-Phenanthroline monohydrate  |  Apratastat  |  BPHA  |  Apigenin-7-glucuronide  |  Mca-P-Cha-G-Nva-HA-Dap(DNP)-NH2  |  PPNDS tetrasodium  |  ARP101  |  Astragaloside IV  |  Phosphoramidon Disodium  |  Cipemastat  |  Tubulin/MMP-IN-2  |  Ilomastat  |  PythiDC  |  MMP2-IN-3  |  Marimastat

熱門(mén)產(chǎn)品線(xiàn)：重組蛋白  |  化合物庫(kù)  |  天然產(chǎn)物  |  熒光染料  |  PROTAC  |  同位素標(biāo)記物  |  寡核苷酸  |  抗體  |  點(diǎn)擊化學(xué)

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry

品牌介紹:
•   MCE (MedChemExpress) 擁有200 多種*僅有化合物庫(kù)，我們致力于為*科研客戶(hù)提供前沿的高品質(zhì)小分子活性化合物；
•   50,000 多種高選擇性抑制劑、激動(dòng)劑涉及各熱門(mén)信號(hào)通路及疾病領(lǐng)；
•   產(chǎn)品種類(lèi)涵蓋各種重組蛋白，多肽，常用試劑盒 ，更有 PROTAC、ADC 等特色產(chǎn)品，廣泛應(yīng)用于新藥研發(fā)、生命科學(xué)等科研項(xiàng)目；
•   提供虛擬篩選，離子通道篩選，代謝組學(xué)分析檢測(cè)分析，藥物篩選等專(zhuān)業(yè)技術(shù)服務(wù)；
•   設(shè)有專(zhuān)業(yè)的實(shí)驗(yàn)中心和嚴(yán)格的質(zhì)控、驗(yàn)證體系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各項(xiàng)質(zhì)檢報(bào)告，確保產(chǎn)品的高純度、高品質(zhì)；
•   產(chǎn)品的生物活性多經(jīng)各國(guó)客戶(hù)實(shí)驗(yàn)驗(yàn)證；
•   Nature, Cell, Science 等多種頂級(jí)期刊及制藥 Patent 收錄了MCE客戶(hù)的科研成果；
•   專(zhuān)業(yè)團(tuán)隊(duì)跟蹤新的制藥及生命科學(xué)研究進(jìn)展，為您提供*新的活性化合物；
•   與世界各大制藥公司及*科研機(jī)構(gòu)建立了長(zhǎng)期的合作。