Companies
MedChemExpress LLC (MCE)
Products
MedChemExpress - Model Apratastat - ...

MedChemExpress - Model Apratastat - 287405-51-0

Apratastat (TMI-005) is an orally active, non-selective and reversible TACE/MMPs inhibitor, can inhibit inhibit the release of TNF-α. Apratastat has the potential to overcome radiotherapy-resistance in non-small cell lung cancer (NSCLC)[1][2]. Apratastat is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Apratastat

MCE China：Apratastat

Brand：MedChemExpress (MCE)

Cat. No.HY-119307

CAS：287405-51-0

Synonyms：TMI-005

Purity：99.67%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

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

Description：Apratastat (TMI-005) is an orally active, non-selective and reversible TACE/MMPs inhibitor, can inhibit inhibit the release of TNF-α. Apratastat has the potential to overcome radiotherapy-resistance in non-small cell lung cancer (NSCLC). Apratastat is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

In Vitro：Apratastat (10 μM, 24 hours) inhibits expression of pro-inflammatory cytokines TNF-α and IL-6 in lung tissue samples[3]. Apratastat (10 μM, 24 hours) reduces ADAM17 activity and MCAM release in HUVEC[4].

In Vivo：Apratastat (10 mg/kg, i.p., administered twice at 4 and 16 hours post-induction) alleviats lung inflammation induced by Poly(I) (HY-119307) and SARS-CoV-2 RBD-S protein in C57BL/6 mice[3]. Apratastat (10 mg/kg, p.o., once daily for 14 days) exhibits anti-tumor and anti-angiogenic activity in the MC38 xenograft C57BL/6 mouse model[4].

IC50 & Target：MMP

References：

[1]. Shu C, et al. Pharmacokinetic-pharmacodynamic modeling of apratastat: a population-based approach. J Clin Pharmacol. 2011 Apr;51(4):472-81. [Content Brief]

[2]. Ieguchi K, et al. Savior or not: ADAM17 inhibitors overcome radiotherapy-resistance in non-small cell lung cancer. J Thorac Dis. 2016 Aug;8(8):E813-5. [Content Brief]

[3]. Lartey NL, et al. ADAM17/MMP inhibition prevents neutrophilia and lung injury in a mouse model of COVID-19. J Leukoc Biol. 2022 Jun;111(6):1147-1158. [Content Brief]

[4]. Stalin J, et al. Targeting of the NOX1/ADAM17 Enzymatic Complex Regulates Soluble MCAM-Dependent Pro-Tumorigenic Activity in Colorectal Cancer. Biomedicines. 2023 Nov 30;11(12):3185. [Content Brief]

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
•   The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects；
•   Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
•   It has a professional experimental center and strict quality control and verification system；
•   Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
•   The biological activity of the products has been verified by the experiments of customers in various countries；
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。