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Talabostat

Talabostat

产品编号 T37861   CAS 149682-77-9

Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM.

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Talabostat Chemical Structure
Talabostat, CAS 149682-77-9
规格 价格/CNY 货期 数量
5 mg ¥ 931 待询
10 mg ¥ 1,381 待询
50 mg ¥ 5,269 待询

Talabostat 的其他形式现货产品:

Talabostat mesylate
其他形式的 Talabostat:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: Talabostat (T37861)
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参考文献
产品描述 Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM.
靶点活性 DPP4:< 4 nM (IC50), DPP4:0.18 nM (Ki), DPP8/9:1.5/0.76 nM (Ki), DPP8/9:4/11 nM (IC50), QPP:310 nM (IC50), FAP:560 nM (IC50)
体外活性 Talabostat 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[1]. 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[2]. 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[3].
体内活性 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[3]. 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[4].
分子量 214.07
分子式 C9H19BN2O3
CAS No. 149682-77-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: ≥ 40 mg/mL (186.85 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.6714 mL 23.3568 mL 46.7137 mL 116.7842 mL
5 mM 0.9343 mL 4.6714 mL 9.3427 mL 23.3568 mL
10 mM 0.4671 mL 2.3357 mL 4.6714 mL 11.6784 mL
20 mM 0.2336 mL 1.1678 mL 2.3357 mL 5.8392 mL
50 mM 0.0934 mL 0.4671 mL 0.9343 mL 2.3357 mL
100 mM 0.0467 mL 0.2336 mL 0.4671 mL 1.1678 mL

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TargetMol Library Books参考文献

1. Connolly BA, et al. Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potencyand in vivo efficacy and safety. J Med Chem. 2008 Oct 9;51(19):6005-13. 2. Okondo MC, et al. DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis. Nat Chem Biol. 2017 Jan;13(1):46-53. 3. Adams S, et al. PT-100, a small molecule dipeptidyl peptidase inhibitor, has potent antitumor effects and augments antibody-mediated cytotoxicity via a novel immune mechanism. Cancer Res. 2004 Aug 1;64(15):5471-80. 4. Egger C, et al. Effects of the fibroblast activation protein inhibitor, PT100, in a murine model of pulmonary fibrosis. Eur J Pharmacol. 2017 Aug 15;809:64-72.

TargetMol Library Books文献引用

1. Jin X, Liu D, Zhou X, et al.Entrectinib inhibits NLRP3 inflammasome and inflammatory diseases by directly targeting NEK7.Cell Reports Medicine.2023, 4(12).

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Keywords

Talabostat 149682-77-9 Inhibitor inhibitor inhibit

 

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