2. NTU281

NTU281 is a potent transglutaminase-2 inhibitor. NTU281 can reduce the increases in serum creatinine and albuminuria in diabetic rats. NTU281 can also reduce glomerular collagen I accumulation, Hic-5 and α-SMA expression, and apoptosis. NTU281 can be used for researching glomerulosclerosis caused by diabetes.

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NTU281 Chemical Structure

NTU281 Chemical Structure

CAS No. : 815619-12-6

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Description

NTU281 is a potent transglutaminase-2 inhibitor. NTU281 can reduce the increases in serum creatinine and albuminuria in diabetic rats. NTU281 can also reduce glomerular collagen I accumulation, Hic-5 and α-SMA expression, and apoptosis. NTU281 can be used for researching glomerulosclerosis caused by diabetes[1][2].

In Vivo

NTU281 (2.5 μl/h of 50 mM; cannulate to deliver into kidneys) reduces glomerular collagen I overexpression as well as the increases in glomerular Hic-5 and α-SMA expression; also decreases serum creatinine, albuminuria, glomerulosclerosis and tubulointerstitial scarring in diabetic rats[1][2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Wistar Han rats [subjected to right uninephrectomy, then induced hyperglycemia by tail vein injection of streptozotocin (35 mg/kg in citrate buffer pH 4)][1]
Dosage: 2.5 μl/h of 50 mM
Administration: Cannulated to deliver into kidneys
Result: Reduced glomerular collagen I overexpression by ~50%; reduced the increases in glomerular Hic-5 expression; reduced diabetic nephropathy-induced α-SMA expression.
Animal Model: Male Wistar Han rats [subjected to right uninephrectomy, then induced hyperglycemia by tail vein injection of streptozotocin (35 mg/kg in citrate buffer pH 4)][2]
Dosage: Various concentration
Administration: Cannulated to deliver into kidneys
Result: Significantly reduced the increases in serum creatinine (-68%) and albuminuria (-80%) in diabetic rats during eight-month experimental period; reduced in glomerulosclerosis (-76.6%) and tubulointerstitial scarring (-68.2%) as a result of lowered accumulation of collagen I, III and IV; and reduced numbers of myofibroblasts present.
Molecular Weight

487.59

Formula

C25H31N2O6S+
CAS No.
SMILES

O=C(N[C@H](C(N[C@@H](CCC(C[S+](C)C)=O)C(O)=O)=O)CC1=CC=CC=C1)OCC2=CC=CC=C2
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Room temperature in continental US; may vary elsewhere.
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Keywords:

NTU281815619-12-6NTU 281NTU-281Inhibitorinhibitorinhibit

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