| CAS NO: | 171235-71-5 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 2mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| Molecular Weight (MW) | 499.60 |
|---|---|
| Formula | C26H37N5O5 |
| CAS No. | 171235-71-5 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 99 mg/mL (198.2 mM) |
| Water: 60 mg/mL (120.1 mM) | |
| Ethanol: 99 mg/mL (198.2 mM) | |
| Other info | Chemical Name: N-[(2S)-1-[[(2S)-1-(2-Aminoethylamino)-1-oxopropan-2-yl]amino]-3-naphthalen-2-yl-1-oxopropan-2-yl]-N'-hydroxy-2-(2-methylpropyl)butanediamide InChi Key: AWNBSWDIOCXWJW-OWHMDLSXSA-N InChi Code: InChI=1S/C26H37N5O5/c1-16(2)12-21(15-23(32)31-36)25(34)30-22(26(35)29-17(3)24(33)28-11-10-27)14-18-8-9-19-6-4-5-7-20(19)13-18/h4-9,13,16-17,21-22,36H,10-12,14-15,27H2,1-3H3,(H,28,33)(H,29,35)(H,30,34)(H,31,32)/t17-,21?,22-/m0/s1 SMILES Code: O=C(N[C@@H](CC1=CC=C2C=CC=CC2=C1)C(N[C@@H](C)C(NCCN)=O)=O)C(CC(C)C)CC(NO)=O |
| Synonyms | TAPI-1; TAPI 1; TAPI |
| In Vitro | In vitro activity: TAPI-1 prevents unstimulated and PMA-induced release of the soluble forms of TNF-alpha, p60 TNFR, and IL-6R from the monocytic cell line, THP-1, and from human peripheral blood monocytes. TAPI also inhibits LPS-induced shedding of the p60 TNFR and TNF-alpha from monocytes. TAPI-1 inhibits TACE-dependent constitutive release of co-transfected APP(695). TAPI-1 attenuates Ang II-induced EGFR transactivation and cell proliferation in human HSC line LI90. TAPI-1 with the EGFR inhibitor AG1478 exhibits deactivated AREG/EGFR/ERK signaling pathway and reduces pro-inflammatory cytokines release in pSS salivary gland-derived epithelial cells. Cell Assay: Five thousand cells are seeded into each well of 96-well plates and their viability is assessed by CellTiter-Glo Luminescent Cell Viability assay. Upon serum deprivation for 24 h, the cells are treated with Ang II for 60 h with and without pretreatment with each inhibitor and antagonist. The assay substrates are then added to each well on the plate and the samples are evaluated using a luminometer. |
|---|---|
| In Vivo | Mice were treated with LPS (10 mg/kg, i.p.) and HK-2 cells were cultured with or without LPS (10 μg/ml) in the presence or absence of a type 1 TACE inhibitor (1 μM) or type 2 TACE inhibitor (10 μM). LPS treatment induced increased serum creatinine, TNFα, and urinary neutrophil gelatinase-associated lipocalin. Angiotensin II type 1 receptor, mitogen activated protein kinase (MAPK), and TACE increased, while angiotensin-converting enzyme-2 (ACE2) expression decreased in LPS-induced acute kidney injury and LPS-treated HK-2 cells. |
| Animal model | Mice |
| Formulation & Dosage | type 1 TACE inhibitor (1 μM) or type 2 TACE inhibitor (10 μM). |
| References | J Immunol. 1995 Dec 1;155(11):5198-205; Biochem J. 2001 Aug 1;357(Pt 3):787-94; Life Sci. 2014 Mar 3;97(2):137-44. |
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