{"id":43163,"date":"2023-06-15T18:18:41","date_gmt":"2023-06-15T10:18:41","guid":{"rendered":"https:\/\/biopioneer.com.tw\/?p=43163"},"modified":"2025-11-20T10:46:56","modified_gmt":"2025-11-20T02:46:56","slug":"tak-242-tlr-4-%e4%bf%a1%e8%99%9f%e6%8a%91%e5%88%b6%e5%8a%91cas243984-11-4-apexbio%e8%b2%a8%e8%99%9fa3850","status":"publish","type":"post","link":"https:\/\/biopioneer.com.tw\/?p=43163","title":{"rendered":"TAK-242 TLR 4 \u4fe1\u865f\u6291\u5236\u5291CAS#243984-11-4 APExBIO\u8ca8\u865fA3850"},"content":{"rendered":"

TAK-242 TLR 4 \u4fe1\u865f\u6291\u5236\u5291CAS#243984-11-4 APExBIO\u8ca8\u865fA3850<\/span><\/span><\/a><\/span><\/strong><\/p>\n

TLR 4 signaling inhibitor<\/p>\n

TAK-242\u7522\u54c1\u4ecb\u7d39<\/span><\/strong><\/span><\/p>\n

IC50\uff1aTAK-242 \u7684 IC50 \u70ba 1.1 \u81f3 11 nM\uff0c\u53ef\u6291\u5236 RAW264.7 \u7d30\u80de\u548c\u5c0f\u9f20\u8179\u819c\u5de8\u566c\u7d30\u80de( peritoneal macrophages)\u4e2d LPS \u8a98\u5c0e\u7684 NO \u7522\u751f\u3001\u816b\u7624\u58de\u6b7b\u56e0\u5b50-\u03b1 (tumor necrosis factor-alpha)\u548c\u767d\u7d30\u80de\u4ecb\u7d20 ( interleukin, IL)-6 [1]\u3002Toll \u662f Toll \u6a23\u53d7\u9ad4 (TLR) \u5bb6\u65cf\u7684\u4e00\u54e1\uff0c\u88ab\u78ba\u5b9a\u70ba\u9ed1\u8179\u679c\u8805\u80da\u80ce( Drosophila melanogaster)\u80cc\u8179\u6975\u6027\u767c\u80b2(embryonic dorsoventral polarity)\u6240\u5fc5\u9700\u7684\u57fa\u56e0\u7522\u7269\u3002\u6b64\u5916\uff0c\u9084\u767c\u73fe\u5b83\u5728\u84bc\u8805\u7684\u6297\u771f\u83cc\u53cd\u61c9(antifungal response)\u4e2d\u8d77\u8457\u95dc\u9375\u4f5c\u7528\u3002 TAK-242 (resatorvid) \u662f\u4e00\u7a2e\u74b0\u5df1\u70ef\u884d\u751f\u7269(cyclohexene derivative)\uff0c\u88ab\u8a8d\u70ba\u662f\u4e00\u7a2e\u9078\u64c7\u6027\u6291\u5236 TLR4 \u4fe1\u865f\u50b3\u5c0e\u7684\u65b0\u578b\u5c0f\u5206\u5b50\u5316\u5408\u7269\u3002\u9ad4\u5916(In vitro)\uff1a\u5148\u524d\u7684\u9ad4\u5916\u7814\u7a76\u8868\u660e\uff0cTAK-242 \u53ef\u4ee5\u901a\u904e\u4f7f\u7528\u5171\u514d\u75ab\u6c89\u6fb1\u65b9\u6cd5\u8207 TLR4 \u7684\u7d30\u80de\u5167\u7d50\u69cb\u57df\u7d50\u5408\u4f86\u6291\u5236\u8102\u591a\u91a3\u8a98\u5c0e\u7684\u708e\u75c7\u4ecb\u8cea\u7684\u7522\u751f\u3002\u5728 10 \u7a2e\u4e0d\u540c\u7684\u4eba\u985e TLR \u4e2d\uff0cTAK-242 \u9078\u64c7\u6027\u5730\u7d50\u5408 TLR4\u3002\u9019\u4e9b\u767c\u73fe\u8868\u660e\uff0cTAK-242 \u53ef\u4ee5\u9078\u64c7\u6027\u5730\u7d50\u5408 TLR4 \u4e26\u7834\u58de TLR4 \u8207\u929c\u63a5\u5206\u5b50\u7684\u76f8\u4e92\u4f5c\u7528\uff0c\u5f9e\u800c\u6291\u5236 TLR4 \u4fe1\u865f\u8f49\u5c0e\u53ca\u5176\u4e0b\u6e38\u4fe1\u865f\u8f49\u5c0e [2]\u3002\u9ad4\u5167(In vivo)\uff1a\u81e8\u5e8a\u524d\u52d5\u7269\u7814\u7a76\u8868\u660e\uff0c\u6025\u6027\u675f\u7e1b\u61c9\u6fc0\u66b4\u9732\u53ef\u4e0a\u8abf\u5927\u9f20 mRNA \u548c\u86cb\u767d\u8cea\u6c34\u5e73\u7684 TLR-4 \u8868\u9054\u3002 TAK-242 \u9810\u61c9\u6fc0\u7d66\u85e5\u53ef\u9632\u6b62\u5927\u9f20\u5927\u8166\u984d\u8449\u76ae\u5c64\u4e2d\u6f5b\u5728\u6709\u5bb3\u7684\u708e\u75c7\u548c\u6c27\u5316\/\u4e9e\u785d\u5316\u4ecb\u8cea\u7684\u7a4d\u7d2f\u3002\u9019\u4e9b\u767c\u73fe\u8868\u660e\uff0c\u4f7f\u7528 TAK-242 \u6216\u5176\u4ed6 TLR-4 \u4fe1\u865f\u901a\u8def\u6291\u5236\u5316\u5408\u7269\u53ef\u88ab\u8996\u70ba\u4e00\u7a2e\u6f5b\u5728\u7684\u6cbb\u7642\u8f14\u52a9\u7b56\u7565\uff0c\u4ee5\u9650\u5236\u5728\u61c9\u6fc0\u66b4\u9732\u5f8c\u548c\u8207\u61c9\u6fc0\u76f8\u95dc\u7684\u795e\u7d93\u7cbe\u795e\u75be\u75c5\u4e2d\u767c\u751f\u7684\u708e\u75c7\u904e\u7a0b [3]\u3002<\/p>\n

<\/p>\n

<\/p>\n

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\"COA\u6587\u4ef6_\u5de5\u4f5c\u5340\u57df<\/a><\/p>\n

<\/p>\n\n\n\n\n\n\n\n\n\n\n\n\n\n\n
Physical Appearance<\/td>\nA solid<\/td>\n<\/tr>\n
Storage<\/td>\nStore at -20\u00b0C<\/td>\n<\/tr>\n
M.Wt<\/td>\n361.82<\/td>\n<\/tr>\n
Cas No.<\/td>\n243984-11-4<\/td>\n<\/tr>\n
Formula<\/td>\nC15<\/sub>H17<\/sub>ClFNO4<\/sub>S<\/td>\n<\/tr>\n
Synonyms<\/td>\nResatorvid;TAK242;TAK 242;CLI-095<\/td>\n<\/tr>\n
Solubility<\/td>\ninsoluble in H2O; \u2265100.6 mg\/mL in EtOH; \u226518.09 mg\/mL in DMSO<\/td>\n<\/tr>\n
Chemical Name<\/td>\nethyl (6R)-6-[(2-chloro-4-fluorophenyl)sulfamoyl]cyclohexene-1-carboxylate<\/td>\n<\/tr>\n
SDF<\/td>\nDownload SDF<\/a><\/td>\n<\/tr>\n
Canonical SMILES<\/td>\nCCOC(=O)C1=CCCCC1S(=O)(=O)NC2=C(C=C(C=C2)F)Cl<\/td>\n<\/tr>\n
Shipping Condition<\/td>\nSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.<\/td>\n<\/tr>\n
General tips<\/td>\nFor obtaining a higher solubility, please warm the tube at 37\u00b0C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon.<\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n

APExBIO\u53f0\u7063\u4ee3\u7406\u5546<\/a><\/span><\/strong><\/span><\/p>\n

https:\/\/www.apexbt.com<\/a><\/span><\/p>\n

APExBIO\u63d0\u4f9b\u512a\u8cea\u7684\u80dc\u80bd\u548c\u751f\u7269\u5206\u6790\u8a66\u5291\uff0c\u5ee3\u6cdb\u7522\u54c1\u7dda\u5982Protease\u3001Chromatin\/Epigenetics\u8868\u89c0\u907a\u50b3\u5b78\u3001MAPK Signal\u3001DNA Damege\/DNA repair\u3001\u7d30\u80de\u51cb\u4ea1\u3001\u816b\u7624\u751f\u7269\u5b78\u3001Stem cell\u7b49\u7814\u7a76\u9818\u57df\uff0c \u9084\u63d0\u4f9b\u5b9a\u5236\u7684\u670d\u52d9\uff0c\u5305\u62ec\u591a\u80bd\u5408\u6210\uff0c\u6297\u9ad4\u7684\u751f\u7522\u548c\u6aa2\u6e2c\u7684\u767c\u5c55\u3002\u7522\u54c1\u7ddaDNA\/RNA prep kit\u3001Drug Screening panel\u3001Bioactive peptides\u3001Growth factors\u3001Biotinylation Reagents\u3001tag peptides\u3001amino Acids\u3001Growth factors\u7b49\u3002APExBIO\u7522\u54c1\u8cea\u91cf\u90fd\u4f34\u96a8\u8457\u8b49\u66f8\u7684\u5206\u6790\uff0c\u9ad8\u6548\u6db2\u76f8\u8272\u8b5c\uff0c\u8cea\u8b5c\uff0c\u548cHMNR\u6578\u64da\u3002>>\u66f4\u591aAPExBio\u5546\u54c1<\/span><\/strong><\/em><\/span><\/a><\/p>\n

\"\"\u86cb\u767d\u6291\u5236\u5291\/\u7de9\u885d\u6db2\u6210\u5206<\/span><\/strong><\/span><\/p>\n