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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 |
備注: |
中文名稱2-氨基-5-[(5-硝基-2-噻唑基)硫代]-1,3,4-噻二唑中文同義詞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-胺英文名稱5-[(5-Nitro-2-thiazolyl)thio]-1,3,4thiadiazol-2-amine英文同義詞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號40045-50-9分子式C5H3N5O2S3分子量261.3EINECS號相關類別噻二唑;化工原料;定制產品;定制中心Mol文件40045-50-9.mol結構式2-氨基-5-[(5-硝基-2-噻唑基)硫代]-1,3,4-噻二唑性質熔點160°C(dec.)沸點549.8±42.0°C(Predicted)密度1.88±0.1g/cm3(Predicted)儲存條件StoreatRT溶解度DMSO:62.5mg/mL(239.19mM;需要超聲波)酸度系數(shù)(pKa)0.65±0.10(Predicted)形態(tài)淡黃色固體顏色淡黃色至琥珀色至深綠色2-氨基-5-[(5-硝基-2-噻唑基)硫代]-1,3,4-噻二唑用途與合成方法生物活性SU3327是一種有效的,選擇性的且具有底物競爭性的JNK抑Chemicalbook制劑,IC50為0.7μM。SU3327還以IC50值為239nM抑制JNK和JIP之間的蛋白相互作用。SU3327對p38α和Akt激酶的活性較低。靶點IC50:0.7μM(JNK);239nM(JNK-JIPinteractions)體外研究SU3327(compound9)isabletoinhibitTNF-αstimulatedphosphorylationofc-JuninHeLacells(EC50=6.23μM).SU3327(25nM)pretreatmentofhuman-derivedcerebralmicrovascularendothelialcells(hCMEC/D3)effectivelyreducesLPS-inducedpolymorphonuclearleukocytes(PMN)rolling/adhesiontohCMEC/D3,preventsactivationofAP-1,andsignificantlyreducesexpressionofVCAM-1.體內研究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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