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Submit ReviewTalabostat mesylate is a potent DPP IV inhibitor (IC50 values are <4, 4, 11, 310 and 560 nM at DPP4, DPP8, DPP9, DPP7 and FAP, respectively). Activates the inflammasome sensor protein NLRP1b and selectively triggers pyroptosis in monocytes and macrophages. Induces immune-mediated tumor regression in multiple mouse models of cancer. Orally bioavailable.
分子量 | 310.18 |
公式 | C9H19BN2O3.CH3SO3H |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 150080-09-4 |
PubChem ID | 11522448 |
InChI Key | OXYYOEIGQRXGPI-WSZWBAFRSA-N |
Smiles | O=C([C@@H](N)C(C)C)N1CCC[C@H]1B(O)O.CS(O)(=O)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 31.02 | 100 | |
DMSO | 15.51 | 50 |
以下数据基于产品分子量 310.18。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 3.22 mL | 16.12 mL | 32.24 mL |
5 mM | 0.64 mL | 3.22 mL | 6.45 mL |
10 mM | 0.32 mL | 1.61 mL | 3.22 mL |
50 mM | 0.06 mL | 0.32 mL | 0.64 mL |
参考文献是支持产品生物活性的出版物。
Okondo et al (2017) DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis. Nat.Chem.Biol. 13 46 PMID: 27820798
Okondo et al (2018) Inhibition of Dpp8/9 activates the Nlrp1b inflammasome. Cell Chem.Biol. 25 262 PMID: 29396289
If you know of a relevant reference for Talabostat mesylate, please let us know.
关键词: Talabostat mesylate, Talabostat mesylate supplier, Potent, DPP, IV, inhibitors, inhibits, inflammasome, pyroptosis, Nlrp1b, BXCL701, DPP4, Val-boroPro, BXCL, 701, Dipeptidyl, Peptidase, (DPP-IV), Inflammasomes, 3719, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Talabostat mesylate 的部分引用包括:
Massimiliano et al (2022) PhAc-ALGP-Dox, a Novel Anticancer Prodrug with Targeted Activation and Improved Therapeutic Index. Mol Cancer Ther 21 568-581 PMID: 35149549
Daniel A et al (2022) A ubiquitin-independent proteasome pathway controls activation of the CARD8 inflammasome. J Biol Chem 298 102032 PMID: 35580636
Justin R et al (2022) M24B aminopeptidase inhibitors selectively activate the CARD8 inflammasome. Nat Chem Biol 18 565-574 PMID: 35165443
Orth-He et al (2023) Protein folding stress potentiates NLRP1 and CARD8 inflammasome activation. Cell Rep 42 111965 PMID: 36649711
Henrik et al (2020) The half-life of the bone-derived hormone osteocalcin is regulated through O-glycosylation in mice, but not in humans. Elife 9 PMID: 33284103
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