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2-氨基-5-[(5-硝基-2-噻唑基)硫代]-1,3,4-噻二唑 |
| CAS No.: |
40045-50-9 |
| 分子式： |
C5H3N5O2S3 |
| 分子量： |
261.3046 |
| 备注： |
中文名称2-氨基-5-[(5-硝基-2-噻唑基)硫代]-1,3,4-噻二唑中文同义词2-氨基-5-[(5-硝基-2-噻唑基)硫代]-1,3,4-噻二唑;5-((5-硝基噻唑-2-基)硫基)-1,3,4-噻二唑-2-胺;化合物SU3327;5-[(5-硝基-1,3-噻唑-2-基)硫基]-1,3,4-噻二唑-2-胺英文名称5-[(5-Nitro-2-thiazolyl)thio]-1,3,4thiadiazol-2-amine英文同义词SU3327;5-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3,4-thiadiazol-2-amine;2-Amino-5-[(5-nitro-2-thiazolyl)thio]-1,3,4-thiadiazole;5-[(5-Nitro-2-thiazolyl)thio]-1,3,4thiadiazol-2-amine;JNKInhibitorXIII-CAS40045-50-9-Calbiochem;1,3,4-Thiadiazol-2-amine,5-[(5-nitro-2-thiazolyl)thio]-;Halicin;5-((5-Nitrothiazol-2-yl)thio)-1,3,4-thiadiazol-2-amineCAS号40045-50-9分子式C5H3N5O2S3分子量261.3EINECS号相关类别噻二唑;化工原料;定制产品;定制中心Mol文件40045-50-9.mol结构式2-氨基-5-[(5-硝基-2-噻唑基)硫代]-1,3,4-噻二唑性质熔点160°C(dec.)沸点549.8±42.0°C(Predicted)密度1.88±0.1g/cm3(Predicted)储存条件StoreatRT溶解度DMSO：62.5mg/mL（239.19mM；需要超声波）酸度系数(pKa)0.65±0.10(Predicted)形态淡黄色固体颜色淡黄色至琥珀色至深绿色2-氨基-5-[(5-硝基-2-噻唑基)硫代]-1,3,4-噻二唑用途与合成方法生物活性SU3327是一种有效的，选择性的且具有底物竞争性的JNK抑Chemicalbook制剂，IC50为0.7μM。SU3327还以IC50值为239nM抑制JNK和JIP之间的蛋白相互作用。SU3327对p38α和Akt激酶的活性较低。靶点IC50:0.7μM(JNK);239nM(JNK-JIPinteractions)体外研究SU3327(compound9)isabletoinhibitTNF-αstimulatedphosphorylationofc-JuninHeLacells(EC50=6.23μM).SU3327(25nM)pretreatmentofhuman-derivedcerebralmicrovascularendothelialcells(hCMEC/D3)effectivelyreducesLPS-inducedpolymorphonuclearleukocytes(PMN)rolling/adhesiontohCMEC/D3,preventsactivationofAP-1,andsignificantlyreducesexpressionofVCAM-1.体内研究SU3327(Compound9;25mg/kg;intraperitonealinjection;maleBKS.Cg-+Leprdb/+Leprdb/OlaHsddb/dbmice)treatmentpossessestheabilitytorestoreinsulinsensitivityinmicemodelsofdiabetes.SU3327(Compound9)hasfavorablemicrosomalandplasmastability(T1/2=27min).AnimalModel:MaleBKS.Cg-+Leprdb/+Leprdb/OlaHsddb/dbmice(11-week-old)injectedwithinsulinDosage:25mg/kgAdministration:IntraperitonealinjectionResult:Resultedinastatisticallysignificantreductioninbloodglucoselevels. |
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