MedChemExpress LLC (MCE)

MedChemExpress - Model UK-383367 - 348622-88-8

UK-383367 is an orally available pro-collagen C-protease inhibitor (BMP-1) with an IC50 value of 44 nM. UK-383367 can reduce renal fibrosis and inflammation in chronic kidney disease (CKD) and may be used to study postoperative skin scarring[1][2][3].

UK-383367

MCE China：UK-383367

Brand：MedChemExpress (MCE)

Cat. No.HY-13102

CAS：348622-88-8

Purity：99.92%

Storage：Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

Description：UK-383367 is an orally available pro-collagen C-protease inhibitor (BMP-1) with an IC50 value of 44 nM. UK-383367 can reduce renal fibrosis and inflammation in chronic kidney disease (CKD) and may be used to study postoperative skin scarring.

In Vitro：UK-383367 (100-1000 nM, 24 h) inhibits the activity of NRK-49F cells[1]. UK-383367 (100-200 nM, 30 min) effectively suppresses the fibrotic response induced by TGF-β1 in mPTCs cells and shows a direct anti-fibrotic effect on renal cells in NRK-49F cells[1].

In Vivo：UK-383367 (5 mg/kg, intraperitoneal injection, once daily for seven days) improves tubulointerstitial fibrosis and inflammation in unilateral ureteral obstruction (UUO) chronic kidney disease (CKD) mice[1]. Pharmacokinetics of single intravenous and oral administration in rats and dogs[2] Animal Intravenous dose (mg/kg) Elimination half-life (h) Plasma clearance (mL/min•kg) Volume of distribution (1/kg) Oral dose (mg/kg) Cmax (ng/mL) Tmax (h) Oral bioavailability (%) Male rat 2.0 0.8 157 12.0 / / / / Male dog 0.5 1.5 35 4.6 2 110 0.5-1.5 13

References：

[1]. Mi Bai, et al. BMP1 inhibitor UK383,367 attenuates renal fibrosis and inflammation in CKD. Am J Physiol Renal Physiol. 2019 Dec 1;317(6):F1430-F1438. [Content Brief]

[2]. Allan GA, et al. Pharmacokinetics and metabolism of UK-383,367 in rats and dogs: a rationale for long-lived plasma radioactivity. Xenobiotica. 2006 May;36(5):399-418. [Content Brief]

[3]. Eugenia C Salcedo, et al. Global Protease Activity Profiling Identifies HER2-Driven Proteolysis in Breast Cancer. ACS Chem Biol. 2021 Apr 16;16(4):712-723. [Content Brief]

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