JPH203 (Nanvuranlat)

製品コードS8667 バッチS866702

化学情報

	Synonyms	KYT-0353, JPH-203SBECD	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₃H₁₉Cl₂N₃O₄
	分子量	472.32	CAS No.	1037592-40-7
Solubility (25°C)*	体外	DMSO	3 mg/mL (6.35 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <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	選択的L型アミノ酸トランスポーター1阻害剤であるNanvuranlat (JPH203, KYT-0353, JPH-203SBECD)は、ヒト結腸癌細胞 (HT-29)、ヒト口腔癌細胞 (YD-38) および白血病細胞において、ロイシン取り込み (IC50=0.06 µM) および細胞増殖 (IC50=4.1 µM) を劇的に阻害する。
in vitro	Nanvuranlat (JPH203) completely and slightly inhibited the L-Leucine uptake in YD-38 cells (IC50 value: 0.79 μM) and NHOKs (IC50 value: >100 μM), respectively. It inhibited HT-29 cell growth, generating an apparent IC50 of 4.1 μM, but the IC50 concentration (0.06 μM) needed to inhibit the L-Leucine uptake did not inhibit HT-29 cell growth, which represents a 68-fold difference in susceptibility. This compound activated the mitochondria-dependent apoptotic signaling pathway by upregulating pro-apoptotic factors, such as Bad, Bax, and Bak, and the active form of caspase-9, and downregulating anti-apoptotic factors, such as Bcl-2 and Bcl-xL in Saos2 human osteosarcoma cells. It can distinguish relative abundance between LAT1 and LAT2, and has high selectivity for LAT1. JPH203 was metabolically stable in mouse, rat, dog, monkey and human liver microsomal incubations. It induces both G2/M and G0/G1 cell cycle arrest, as well as reduced the S phase accompanied by altered expression of the proteins in cell cycle progression: cyclin D1, CDK4, and CDK6.
in vivo	Daily intravenous administration of JPH203 (12.5 and 25 mg/kg) significantly inhibited tumor growth in KKU-213 cholangiocarcinoma cell xenografts in the nude mice model in a dose-dependent manner with no statistically significant change in the animal’s body weight and with no differences in the histology and appearance of the internal organs compared with the control group. Thus, this compound shows anti-tumor efficacy in nude mice bearing human cholangiocarcinom (CCA) cell xenografts without general toxicity.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Saos2 human osteosarcoma cells
	濃度	100 µM
	反応時間	72 h
	実験の流れ	Colony formation assays are performed by seeding 300 cells/well into 6 well plates. After 24 h of growth, the cells are treated with 100 µM Nanvuranlat (JPH203) for 72 h. This compound is then removed and fresh medium is added. The cells are incubated for 10 days. Thereafter, medium is removed and the cells are washed with phosphate buffered saline (PBS) and fixed with 4% paraformaldehyde for 10 min at 4℃. Sequentially, the colonies are stained with 2% crystal violet for 10 min. Finally, colonies stained by crystal violet are washed with PBS and dried at room temperature, before imaged by a digital camera.
動物実験	動物モデル	Sprague-Dawley rats
	投薬量	0.9-1.0 mg/kg
	投与方法	i.v.

参考

https://pubmed.ncbi.nlm.nih.gov/24492461/
https://pubmed.ncbi.nlm.nih.gov/29200902/
https://pubmed.ncbi.nlm.nih.gov/21914964/

https://pubmed.ncbi.nlm.nih.gov/28347255/

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

LAT1-NRF2 axis controls sFlt-1/PlGF imbalance and oxidative stress in preeclampsia [ Nat Commun, 2025, 16(1):9112]	PubMed: 41087351
TXNIP mediates LAT1/SLC7A5 endocytosis to limit amino acid uptake in cells entering quiescence [ EMBO J, 2025, 10.1038/s44318-025-00608-9]	PubMed: 41116060
Amino acid transporter LAT1 (SLC7A5) promotes metabolic rewiring in TNBC progression through the L-Trp/QPRT/NAD+ pathway [ J Exp Clin Cancer Res, 2025, 44(1):190]	PubMed: 40611146
SLC7A5 is required for cancer cell growth under arginine-limited conditions [ Cell Rep, 2025, 44(1):115130]	PubMed: 39756034
Expression and Functional Evaluation of ABC and SLC Transporters in Human Choroid Plexus Papilloma (HIBCPP) Cells: A Human Blood-Cerebrospinal Fluid Barrier Model [ Pharm Res, 2025, 10.1007/s11095-025-03987-0]	PubMed: 41372689
Fragment-Based Screening Identifies Novel Non-Amino Acid Inhibitors of the Sodium-Coupled Neutral Amino Acid Transporter SNAT2 [ Pharm Res, 2025, 42(8):1285-1297]	PubMed: 40775108
Targeting LAT1 with JPH203 to reduce TNBC proliferation and reshape suppressive immune microenvironment by blocking essential amino acid uptake [ Amino Acids, 2025, 57(1):27]	PubMed: 40379991
BCAA mediated microbiota-liver-heart crosstalk regulates diabetic cardiomyopathy via FGF21 [ Microbiome, 2024, 12(1):157]	PubMed: 39182099
BCKDK Modification Enhances the Anticancer Efficacy of CAR-T Cells by Reprogramming Branched Chain Amino Acid Metabolism [ Mol Ther, 2024, S1525-0016(24)00319-8]	PubMed: 38734897
Oligonol®, an Oligomerized Polyphenol from Litchi chinensis, Enhances Branched-Chain Amino Acid Transportation and Catabolism to Alleviate Sarcopenia [ Int J Mol Sci, 2024, 25(21)11549]	PubMed: 39519101

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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