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仪器信息网试剂标物生化试剂生物分子 Talabostat mesilate

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爱必信(上海)生物科技有限公司

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Talabostat mesilate

价格：￥ 1686

品牌：爱必信

供货周期：一周

货号：abs812055

规格：≥98%

CAS：150080-09-4

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抑制剂描述：

产品名称：Talabostat mesilate

产品别名：见爱必信官网

英文别名：Talabostat mesilate

靶点：DPP4

CAS：150080-09-4

纯度：98% min

外观：见爱必信官网

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

Talabostat(PT-100; Val-boroPro)甲磺酸盐是一种有效的高效DPP4抑制剂，IC50为1 nM。

溶解性：DMSO: ≥ 40 mg/mL

体外研究：

Talabostat mesylate is a nonselective DPP-IV inhibitor, inhibiting DPP8/9, FAP, DPP2 and some other DASH family enzymes essentially as potently as it inhibits DPP-IV. Talabostat stimulates the immune system by triggering a proinflammatory form of cell death in monocytes and macrophages known as pyroptosis. The inhibition of two serine proteases, DPP8 and DPP9, activates the proprotein form of caspase-1 independent of the inflammasome adaptor ASC. Talabostat competitively inhibits the dipeptidyl peptidase (DPP) activity of FAP and CD26/DPP-IV, and there is a high-affinity interaction with the catalytic site due to the formation of a complex between Ser630/624 and the boron of talabostat.

体内研究：Talabostat can stimulate immune responses against tumors involving both the innate and adaptive branches of the immune system. In WEHI 164 fibrosarcoma and EL4 and A20/2J lymphoma models, PT-100 causes regression and rejection of tumors. The antitumor effect appears to involve tumor-specific CTL and protective immunological memory. Talabostat treatment of WEHI 164-inoculated mice increases mRNA expression of cytokines and chemokines known to promote T-cell priming and chemoattraction of T cells and innate effector cells. Talabostat treated mice show significant less fibrosis and FAP expression is reduced. Upon PT100 treatment, significant differences in the MMP-12, MIP-1α, and MCP-3 mRNA expression levels in the lungs are also observed. Treatment with PT100 in this murine model of pulmonary fibrosis has an anti-fibro-proliferative effect and increases macrophage activation.

产品信息订购：

产品货号	产品名称	规格	价格	大包装及货期
abs812055	Talabostat mesilate	10mg	1686.00	立即咨询
abs812055	Talabostat mesilate	50mg	7623.00	立即咨询

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