产品名称

英文名称：ONX-0914 (PR-957)

同义词

PR-957;ONX 0914;ONX0914;PR957;PR 957;N-[2-(4-Morpholinyl)acetyl]-L-alanyl-O-methyl-N-[(1S)-2-[(2R)-2-methyl-2-oxiranyl]-2-oxo-1-(phenylmethyl)ethyl]-L-tyrosinamide、PR-957;ONX 0914;ONX0914;PR957;PR 957;N-[2-(4-Morpholinyl)acetyl]-L-alanyl-O-methyl-N-[(1S)-2-[(2R)-2-methyl-2-oxiranyl]-2-oxo-1-(phenylmethyl)ethyl]-L-tyrosinamide

产品性质

CAS编号：960374-59-8

分子式：C31H40N4O7

分子量：580.67

PubChem编号：23642227

别名：PR-957;ONX 0914;ONX0914;PR957;PR 957;N-[2-(4-Morpholinyl)acetyl]-L-alanyl-O-methyl-N-[(1S)-2-[(2R)-2-methyl-2-oxiranyl]-2-oxo-1-(phenylmethyl)ethyl]-L-tyrosinamide

英文别名：PR-957;ONX 0914;ONX0914;PR957;PR 957;N-[2-(4-Morpholinyl)acetyl]-L-alanyl-O-methyl-N-[(1S)-2-[(2R)-2-methyl-2-oxiranyl]-2-oxo-1-(phenylmethyl)ethyl]-L-tyrosinamide

规格或纯度：≥98%

英文名称：ONX-0914 (PR-957)

生化机理：DescriptionIC50 Value ~10 nM [1]ONX-0914 (PR-957) is a potent and selectiveimmunoproteasome inhibitor with minimal cross-reactivity for the constitutive proteasome.in vitro PR-957 blocked presentation of LMP7-specific, MHC-I-restricted antigens in vitro and in vivo. Selective inhibition of LMP7 by PR-957 blocked production of interleukin-23 (IL-23) by activated monocytes and interferon-gamma and IL-2 by T cells [1].in vivo In mouse models of rheumatoid arthritis and lupus, ONX-0914 treatment reverses signs of disease and results in reductions in cellular infiltration, cytokine production and autoantibody levels at well-tolerated doses. The maximum tolerated dose (MTD) of ONX-0914 in mice to be 30 mg/kg body weight. IFN-g release is inhibited by ~60% at LMP7-selective concentrations of ONX-0914 and by ~90% at higher concentrations. Production of IL-2 is also inhibited by ~50% [1].Toxicity N/AClinical trial N/A

储存温度：-20°C储存

运输条件：超低温冰袋运输

备注：5mg、25mg卖完停产，不再备货

产品介绍：ONX-0914 (PR-957)是一种有效的，选择性的immunoproteasome（免疫蛋白酶体）抑制剂，具有最低的交叉反应性。ONX-0914 (PR-957) is a potent and selective immunoproteasome inhibitor with minimal cross-reactivity for the constitutive proteasome.

IUPAC Name：(2S)-3-(4-methoxyphenyl)-N-[(2S)-1-[(2R)-2-methyloxiran-2-yl]-1-oxo-3-phenylpropan-2-yl]-2-[[(2S)-2-[(2-morpholin-4-ylacetyl)amino]propanoyl]amino]propanamide

INCHI：InChI=1S/C31H40N4O7/c1-21(32-27(36)19-35-13-15-41-16-14-35)29(38)34-26(18-23-9-11-24(40-3)12-10-23)30(39)33-25(28(37)31(2)20-42-31)17-22-7-5-4-6-8-22/h4-12,21,25-26H,13-20H2,1-3H3,(H,32,36)(H,33,39)(H,34,38)/t21-,25-,26-,31+/m0/s1

InChi Key：WQAVPPWWLLVGFK-VTNASVEKSA-N

Canonical SMILES：CC(C(=O)NC(CC1=CC=C(C=C1)OC)C(=O)NC(CC2=CC=CC=C2)C(=O)C3(CO3)C)NC(=O)CN4CCOCC4

Isomeric SMILES：C[C@@H](C(=O)N[C@@H](CC1=CC=C(C=C1)OC)C(=O)N[C@@H](CC2=CC=CC=C2)C(=O)[C@]3(CO3)C)NC(=O)CN4CCOCC4

PubChem CID：23642227

MeSH Entry Terms：(S)-3-(4-methoxyphenyl)-N-((S)-1-((S)-2-methyloxiran-2-yl)-1-oxo-3-phenylpropan-2-yl)-2-((S)-2-(2-morpholinoacetamido)propanamido)propanamide;ONX 0914;PR-957

溶解性：DMSO 100 mg/mL (172.21 mM);Water <1 mg/mL (<1 mM);Ethanol 100 mg/mL (172.21 mM)

产品包装