Apratastat
CAS No. : 287405-51-0
(Synonyms: TMI-005)
| Size | Price | Stock |
|---|---|---|
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| 5mg | $200 | In-stock |
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| Cat. No. : | HY-119307 |
| M.Wt: | 414.50 |
| Formula: | C17H22N2O6S2 |
| Purity: | >98 % |
| Solubility: | DMSO : 41.4 mg/mL (ultrasonic;warming) |
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. 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].
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