THR-123
THR-123 is an orally active ALK3 peptide agonist. THR-123 has a relatively weak binding to ALK2, but does not bind to ALK6. THR-123 suppresses inflammation, apoptosis and the epithelial-to-mesenchymal transition program and reverses established fibrosis in five mouse models of acute and chronic renal injury. THR-123 can be used for the study of kidney fibrosis.
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- Fòrmula: C83H124N22O27S2
- Peso molecular:1926.13
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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BMPR1A |
IL-6 |
IL-8 |
THR-123 (0-100 μM, 60 min) inhibits the expression of IL-6, IL-8 and ICAM-1 induced by TNF-α in a concentration-dependent manner in HK-2 cells[1].
THR-123 (250 μM) significantly inhibits TGF-β1, hypoxia, or cisplatin-induced cell apoptosis in HK-2 cells[1].
THR-123 (10 μM) restores the expression of E-cadherin inhibited by TGF-β1, reduces the expressions of CTGF and Snail1, and reverses the transformation of cell morphology into the mesenchymal form[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
THR-123 (5-15 mg/kg, p.o. or i.p., once daily for 5-7 days) inhibits interstitial volume expansion and collagen deposition in unilateral ureteral obstruction (UUO) model in mice[1].
THR-123 (5 mg/kg, p.o., once daily from 8 weeks to 16 weeks of age) does not alter the glomerular abnormalities, and significantly inhibits the tubular atrophy and interstitial fibrosis seen in COL4A3KO mice[1].
THR-123 (5 mg/kg, p.o., once daily for 3 months) inhibits the progression of fibrosis associated with advanced diabetic nephropathy in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nephrotoxic serum nephritis, NTN model established in CD1 mice[1]
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Dosage:5 mg/kg
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Administration:Oral administration (p.o.), once daily for 3 weeks
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Result:Significantly reversed the already formed renal fibrosis, and improve glomerular sclerosis, renal tubular atrophy and interstitial fibrosis.
Significantly reduced renal function indicators.
Inhibited epithelial-mesenchymal transition (EMT) and reduce the number of E-cadherin and FSP1 double-positive renal tubular cells.
Reduced macrophage infiltration and activate the BMP-Smad signaling pathway (p-Smad1/5).
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Animal Model:IRI model established in C57Bl/6 mice (8 weeks)[1]
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Dosage:5 mg/kg
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Administration:Oral administration (p.o.), once daily for 7 days
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Result:Significantly reduced the proportion of renal tubular necrosis and lowered the blood urea nitrogen level.
Reduced macrophage infiltration and alleviated cell apoptosis.
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Animal Model:UUO model established in CD1 mice (8-12 week)[1]
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Dosage:5 and 15 mg/kg (p.o.) or 5 mg/kg (i.p.)
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Administration:Oral administration (p.o.) or intraperitoneal injection (i.p.), once daily for 5-7 days
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Result:Inhibited interstitial volume expansion and collagen deposition. Reduced the expression of fibrosis markers (fibronectin and type I collagen).
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Animal Model:Alport syndrome model established in eight weeks-old COL4A3KO mice on C57Bl/6 background[1]
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Dosage:5 mg/kg
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Administration:Oral administration (p.o.), once daily from 8 weeks of age to 16 weeks of age
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Result:Improved glomerular sclerosis, tubular damage and interstitial fibrosis. Restored the expression of E-cadherin and reduce the fibroblast marker FSP1.
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Animal Model:Streptozotocin (HY-13753) induced Diabetic nephropathy, DN model established in male CD1 mice (8 week)[1]
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Dosage:5 mg/kg
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Administration:Oral administration (p.o.), once daily for 3 months
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Result:Reduced mesangial matrix expansion, macrophage infiltration and cell apoptosis.
Delayed the deterioration of renal function in combination of Captopril (HY-B0368).
Chemical Information
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Peso molecular 1926.13
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Fòrmula C83H124N22O27S2
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Sequence
Cys-Tyr-Phe-Asp-Asp-Ser-Ser-Asn-Val-Leu-Cys-Lys-Lys-Tyr-Arg-Ser (disulfide bridge: Cys1-Cys11)
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Sequence Shortening
CYFDDSSNVLCKKYRS (disulfide bridge: Cys1-Cys11)
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
THR-123 Related Classifications
HY-P11354 Related Classifications
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