JTT-551

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

JTT-551 (JTT551, JTT 551) 是一种新型有效的选择性蛋白酪氨酸磷酸酶 1B (PTP1B) 抑制剂，Ki 为 0.22 uM。

JTT-551 (JTT551, JTT 551) is a novel potent, selective inhibitor of protein tyrosine phosphatase 1B (PTP1B) with Ki of 0.22 uM, displays >45-fold and >136-fold selectivity over TCPTP, CD45 and LAR; JTT-551 exhibits clear selectivity against the other PTPs, increases the insulin-stimulated glucose uptake in L6 cells; enhances the IR phosphorylation of liver and reduces the glucose level in ob/ob mice , also shows a hypoglycaemic effect without an acceleration of body weight gain in db/db mice.Diabetes Phase 1 Discontinued.

JTT 551 is selective a protein tyrosine phosphatase 1B (PTP1B) inhibitor, with Kis of 0.22 μM and 9.3 μM for PTP1B and TCPTP (T-cell protein tyrosine phosphatase), respectively. JTT 551 shows low affinity at CD45 PTP (CD45) and leucocyte common antigen-related (LAR) PTP with Kis of both >30 μM. Furthermore, JTT-551 (10 and 30 μM) enhances the insulin-induced deoxyglucose uptake in a dosedependent manner.

JTT 551 (3 mg/kg, 30 mg/kg, p.o.) dose-dependently decreases blood glucose level on Days 7, 14 and 28 in db/db Mice. JTT 551 also significantly reduces triglyceride (TG) level at 30 mg/kg on Day 7 but does not alter insulin and total cholesterol (TC) levels.

JTT551 | JTT 551

Metabolic Enzyme/Protease

Protein Phosphatase/PTP

Protein Phosphatase/PTP

Metabolic Disease

Diabetes

776309-04-7

605.86

C34H43N3O3S2

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (165.06 mM)

CCCC(CCC)C1=CC=C(C=C1)OCC2=CC=C(C=C2)C3=CSC(=N3)CN(CC4=NC=C(S4)C(C)(C)C)CC(=O)O

N-((5-(tert-butyl)thiazol-2-yl)methyl)-N-((4-(4-((4-(heptan-4-yl)phenoxy)methyl)phenyl)thiazol-2-yl)methyl)glycine

(-20℃)

With Ice Pack

≥ 2 years