Talabostat (Val-boroPro, PT-100) Mesylate

製品コードS8455 バッチS845501

化学情報

	Synonyms	Val-boroPro	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₁₀H₂₃BN₂O₆S
	分子量	310.18	CAS No.	150080-09-4
Solubility (25°C)*	体外	DMSO	62 mg/mL (199.88 mM)
		Water	62 mg/mL (199.88 mM)
		Ethanol	62 mg/mL (199.88 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Talabostat (Val-boroPro, PT-100) は、DPP-IV、DPP8、DPP9、QPP、FAP、および PEP に対してそれぞれ <4 nM、4 nM、11 nM、310 nM、560 nM、および 390 nM の IC50 値を持つジペプチジルペプチダーゼ阻害剤です。これは抗腫瘍活性と造血刺激活性を持っています。
in vitro	In vitro, talabostat (PT-100) upregulates cytokines/chemokines in human bone marrow stromal cells. This compound induces monocytes and macrophage cell death, and its induction of pyroptosis requires caspase-1.
in vivo	Talabostat (PT-100) has been shown to produce potent antitumor effects when administered orally in multiple mouse tumor models. Val-boroPro mediates complete tumor regression via a novel mechanism that requires more rapid DC trafficking and subsequent acceleration of T cell priming. In tumor stroma, it can directly target FAP expressed by reactive fibroblasts. This compound stimulates innate and adaptive immune responses against tumors involving transcriptional upregulation of cytokines and chemokines. Val-boroPro is known to stimulate the transcriptional upregulation several cytokines, including IL-1β, IL-6, G-CSF, and CXCL1/KC, in both tumors and tumor-draining lymph nodes, and to increase the mouse serum protein levels of several of these cytokines, including G-CSF and CXCL1/KC.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	THP-1 macrophages
	濃度	0.1, 1, 10 μM
	反応時間	24 h
	実験の流れ	--
動物実験	動物モデル	C57BL/6 female mice
	投薬量	20 µg
	投与方法	by gavage

参考

https://pubmed.ncbi.nlm.nih.gov/16186403/
https://cancerres.aacrjournals.org/content/67/9_Supplement/1894
https://www.ncbi.nlm.nih.gov/pubmed/?term=23554941

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5477230/

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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