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12

抑制剂 & 化合物

9

天然产物

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Cat. No. Product Name Target Signaling Pathways
T15385 Glibornuride

Potassium Channel Membrane transporter/Ion channel
Glibornuride 是对 ATP 敏感的 K+通道 (KATP 通道) 阻滞剂,pKi 为 5.75。Glibornuride 显示抗糖尿病活性。
T15781 LP-935509

Serine/threonin kinase; AAK1 (AP2 associated kinase 1) Cell Cycle/Checkpoint; Metabolism; Neuroscience
LP-935509 是一种选择性的、具有脑渗透的、小分子的衔接蛋白-2 相关激酶1 (AAK1) ATP 竞争性抑制剂,其 IC50=3.3 nM,Ki=0.9 nM。它是一种 BIKE 的有效抑制剂 (IC50=14 nM) 和中度的 GAK 抑制剂 (IC50=320 nM)。它能够逆转 SNL 手术后的疼痛。
T5983 o-Phenanthroline

1,10-菲罗啉,1,10-Phenanthroline

MMP; Others Others; Proteases/Proteasome
o-Phenanthroline (1,10-Phenanthroline) 是一种金属螯合剂,能够与 Fe2+形成红色螯合物,在 510 nm 处最大吸收,可防止链脲佐菌素诱导染色体畸变。它也是一种MMP 的抑制剂。
T61166 α-Glucosidase-IN-16

α-Glucosidase-IN-16 is a highly effective and orally bioavailable inhibitor of α-glucosidase, displaying a remarkable IC50 value of 3.28 μM. This compound demonstrates the ability to significantly decrease blood glucose levels in diabetic rats induced by Streptozotocin. Notably, α-Glucosidase-IN-16 also exhibits noteworthy antidiabetic activity [1].
T35809 C20 Sphingomyelin (d18:1/20:0)

C20 Sphingomyelin is a naturally occurring sphingolipid. Levels of C20 sphingomyelin are upregulated in the hippocampus of rats with diabetes induced by streptozotocin and in human plasma where it is positively correlated with insulin resistance in obese humans. C20 sphingomyelin is also upregulated in the liver of a mouse model of Niemann-Pick type C1 disease, a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder. The plasma concentration of C20 sphingomyelin is decreased in m...
T3689L Ruboxistaurin mesylate

LY-333531,LY333531,LY 333531,LY-333531 Mesylate

Ruboxistaurin is a PKC beta inhibitor. Ruboxistaurin reduces oxidative stress and attenuates left ventricular hypertrophy and dysfunction in rats with streptozotocin-induced diabetes. Ruboxistaurin attenuates diabetic nephropathy via modulation of TGF-β1/
T69990 Ruboxistaurin mesylate monohydrate

Ruboxistaurin mesylate monohydrate is a PKC beta inhibitor potentially for the treatment of diabetic nephropathy and diabetic macular edema. Ruboxistaurin attenuates diabetic nephropathy via modulation of TGF-β1/Smad and GRAP pathways. Ruboxistaurin reduces oxidative stress and attenuates left ventricular hypertrophy and dysfunction in rats with streptozotocin-induced diabetes. Ruboxistaurin inhibits retinal neovascularization via suppression of phosphorylation of ERK1/2 and Akt.
T78612 APPA

Apoptosis Apoptosis
APPA为一种醛糖还原酶抑制剂,能够抑制大鼠多元醇途径,有效预防细胞凋亡及链脲佐菌素引发的糖尿病症状,显示出对糖尿病肾病(DN)研究的应用潜力。
T78066 BBT

Calcium Channel Membrane transporter/Ion channel; Metabolism
BBT是一种增强剂,用于改善受损的葡萄糖刺激胰岛素分泌(GSIS)。该化合物展现出抗高血糖的活性,并能在2型糖尿病模型中,对β细胞起到保护作用,抵御细胞因子或链脲佐菌素(STZ)引起的细胞死亡。BBT的作用机制涉及通过cAMP/PKA及持久(L型)电压依赖性Ca2+通道/CaMK2通路。
T71328 Theobromine-d6

Theobromine-d6 is intended for use as an internal standard for the quantification of theobromine by GC- or LC-MS. Theobromine is a methylxanthine alkaloid and derivative of caffeine that has been found in cocoa beans and has diverse biological activities. It is an adenosine A1 receptor antagonist. Theobromine increases AMPK phosphorylation and inhibits adipocyte differentiation, ERK and JNK phosphorylation, and IL-6 and TNF-α production in 3T3-L1 preadipocytes cultured in differentiation medium....
T71981 Gliclazide-d4

Gliclazide-d4 is intended for use as an internal standard for the quantification of gliclazide by GC- or LC-MS. Gliclazide is a sulfonylurea and an inhibitor of pancreatic β-cell ATP-sensitive potassium (KATP) channels. It is selective for pancreatic β-cell over cardiac and arterial smooth muscle cell KATP channels. Gliclazide (5 μM) increases insulin-induced glucose uptake and glucose transporter 4 (GLUT4) translocation to the plasma membrane in a differentiated 3T3L1 adipocyte model of insulin...
T83688 R 715 TFA

[Ac-Lys-[D-βNal7,Ile8]des-Arg9]-BK,Ac-Lys-Arg-Pro-Pro-Gly-Phe-Ser-D2Nal-Ile-OH

R 715是一种布拉迪肾上腺素B1受体拮抗剂。它抑制在表达布拉迪肾上腺素B1受体的孤立人类脐带中由布拉迪肾上腺素引发的收缩(pA2 = 8.49)。R 715(200、400及600 µg/kg)通过尾部闪烁测试减少了由链脲佐菌素(STZ)诱导的糖尿病神经病变小鼠模型中尾部撤回的潜伏期。它还在以髓磷脂少突胶质细胞糖蛋白(MOG)(35-55)(MOG35-55)抗原肽诱导的实验性自体免疫性脑炎(EAE)小鼠模型中,通过每天1 mg/kg的剂量减少了后肢无力和瘫痪的发病率,改善对称步态,并减少脊髓炎症灶点数、神经元脱髓鞘以及病灶单核细胞侵袭。R 715(0.01 nmol/动物,脑室内)能在自发性高血压大鼠中降低平均动脉血压并增加心率。

化合物

Glibornuride
Cat.No: T15385
Synonym:
Target: Potassium Channel
LP-935509
Cat.No: T15781
Synonym:
Target: Serine/threonin kinase, AAK1 (AP2 associated kinase 1)
o-Phenanthroline
Cat.No: T5983
Synonym: 1,10-菲罗啉,1,10-Phenanthroline
Target: MMP, Others
α-Glucosidase-IN-16
Cat.No: T61166
Synonym:
Target:
C20 Sphingomyelin (d18:1/20:0)
Cat.No: T35809
Synonym:
Target:
Ruboxistaurin mesylate
Cat.No: T3689L
Synonym: LY-333531,LY333531,LY 333531,LY-333531 Mesylate
Target:
Ruboxistaurin mesylate monohydrate
Cat.No: T69990
Synonym:
Target:
APPA
Cat.No: T78612
Synonym:
Target: Apoptosis
BBT
Cat.No: T78066
Synonym:
Target: Calcium Channel
Theobromine-d6
Cat.No: T71328
Synonym:
Target:
Gliclazide-d4
Cat.No: T71981
Synonym:
Target:
R 715 TFA
Cat.No: T83688
Synonym: [Ac-Lys-[D-βNal7,Ile8]des-Arg9]-BK,Ac-Lys-Arg-Pro-Pro-Gly-Phe-Ser-D2Nal-Ile-OH
Target:
Cat. No. Product Name Target Signaling Pathways
T1507 Streptozocin

STZ,Streptozotocin,链脲佐菌素,NSC-85998,链脲菌素,U 9889

DNA Alkylator/Crosslinker; DNA Alkylation; DNA/RNA Synthesis; Antibacterial; Antibiotic; Autophagy Autophagy; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology
Streptozocin (NSC-85998) 是一种抗生素,可诱导 DNA 甲基化。Streptozocin 对产生胰岛素的胰岛 B 细胞具有毒性,常用于构建 1 型糖尿病的动物模型。该产品在溶液中不稳定,建议现配现用。
T14046 Anandamide

花生四烯酸乙醇胺,(5Z,8Z,11Z,14Z)-N-(2-Hydroxyethyl)icosa-5,8,11,14-tetraenamide

Cannabinoid Receptor; Endogenous Metabolite GPCR/G Protein; Metabolism
Anandamide ((5Z,8Z,11Z,14Z)-N-(2-Hydroxyethyl)icosa-5,8,11,14-tetraenamide) 是一种免疫调节剂,通过大麻素受体 CB1 和 CB2 起作用,还通过中枢神经系统中的其他靶点起作用,如 GPR18/GPR55。
TN1308 6-Hydroxyflavanone

Others; Lipoxygenase; COX; GABA Receptor Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience; Others
6-Hydroxyflavanone 是从菖蒲叶中提取分离,通过靶向环氧合酶-2(COX-2),5-脂氧合酶(5-LOX)以及阿片类药物和 GABA-A 受体从而具有抗炎和抗神经性疼痛活性。6-Hydroxyflavanone 在链脲佐菌素诱导的糖尿病神经病变模型中具有抗伤害感受特性。
TN4138 Globularin

Others Others
Globularin has hypoglycaemic and hypolipidemic activities in normal and streptozotocin-induced diabetic rats.
TN3735 Cycloart-23-ene-3,25-diol

Antifection Microbiology/Virology
Cycloart-23-ene-3,25-diol has anti-inflammatory activity, it has protective activity against streptozotocin induced toxicity. Cycloart-23-ene-3,25-diol treatment can decrease liver malondialdehyde but increase superoxidase dismutase and reduced glutathion
T15949 Mahanimbine

AChE Neuroscience
Mahanimbine 存在于Murraya koenigii 的根、叶和茎中,是从Murraya koenigii 中的提取的一种具有口服活性的生物碱。Mahanimbine 具有乙酰胆碱酯酶抑制活性,可抑制了高脂肪饮食(HFD)引起的小鼠代谢并发症的发展,对科尼氏分枝杆菌叶对链脲佐菌素诱导的糖尿病大鼠胰腺β细胞组织病理学变化有作用。
T80007 Stevisalioside A

Phosphatase Metabolism
Stevisalioside A (Compound 2),一种从甜叶菊根提取的化合物,展现出抗糖尿病的口服活性。该化合物有效抑制PTP1B,IC50为526.8 μM,并能降低Stevisalioside A引起的高血糖小鼠血糖水平,改善餐后血糖峰值及口服葡萄糖和胰岛素耐量测试结果。
T83916 Cytogenin

Cytogenin(一种源自S. eurocidicum的香豆素衍生物)具有多种生物活性。在每日给药25 mg/kg剂量下,能减轻Ehrlich鼠自发性腺癌模型的肿瘤重量。在体内,Cytogenin(每日30和100 mg/kg)可减少链脲佐菌素诱导的体重下降和血浆葡萄糖水平上升,以及小鼠糖尿病模型中巨噬细胞胰腺浸润。同时,在每日100 mg/kg的剂量下,能降低小鼠巨噬细胞中zymosan和LPS诱导的一氧化氮产生,及LPS诱导的Il-6水平增加。
TN4997 Serpentine

IGF-1R Tyrosine Kinase/Adaptors
Serpentine 是一种玫瑰花根中的生物碱,可用作胰岛素增敏剂,以协助胰岛素降低血糖。Serpentine 可激活 AMPK 磷酸化,从而刺激C2C12细胞对葡萄糖的摄取。Serpentine 可增加了肌肉组织中GSK-3β mRNA的表达,从而增强葡萄糖摄取。Serpentine 显著增加胰高血糖素分泌和肝糖异生。在高脂肪饮食/链脲佐菌素(HFD/STZ)诱导的糖尿病小鼠中,Serpentine 显著延长了胰岛素的降血糖时间,显著降低了外源性胰岛素的使用,抑制了内源性胰岛素的分泌。

天然产物

Streptozocin
Cat.No: T1507
Synonym: STZ,Streptozotocin,链脲佐菌素,NSC-85998,链脲菌素,U 9889
Target: DNA Alkylator/Crosslinker, DNA Alkylation, DNA/RNA Synthesis, Antibacterial, Antibiotic, Autophagy
Anandamide
Cat.No: T14046
Synonym: 花生四烯酸乙醇胺,(5Z,8Z,11Z,14Z)-N-(2-Hydroxyethyl)icosa-5,8,11,14-tetraenamide
Target: Cannabinoid Receptor, Endogenous Metabolite
6-Hydroxyflavanone
Cat.No: TN1308
Synonym:
Target: Others, Lipoxygenase, COX, GABA Receptor
Globularin
Cat.No: TN4138
Synonym:
Target: Others
Cycloart-23-ene-3,25-diol
Cat.No: TN3735
Synonym:
Target: Antifection
Mahanimbine
Cat.No: T15949
Synonym:
Target: AChE
Stevisalioside A
Cat.No: T80007
Synonym:
Target: Phosphatase
Cytogenin
Cat.No: T83916
Synonym:
Target:
Serpentine
Cat.No: TN4997
Synonym:
Target: IGF-1R
TargetMol Loading
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