GLPG1837

製品コードS8698 バッチS869801

化学情報

	Synonyms	ABBV-974	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₆H₂₀N₄O₃S
	分子量	348.42	CAS No.	1654725-02-6
Solubility (25°C)*	体外	DMSO	69 mg/mL (198.03 mM)
		Ethanol	5 mg/mL (14.35 mM)
		Water	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	GLPG1837 (ABBV-974) is a novel CFTR potentiator with an EC50 value of 3 nM for F508del, showing enhanced efficacy on CFTR mutants harboring class III mutations compared to Ivacaftor.
in vitro	GLPG1837 has an attractive in vitro ADME profile, showing low Clint,unb in both microsomal and hepatocytes stability assays, good permeability, and no off-target inhibition of CYPs and the hERG channel^[1].
in vivo	The pharmacokinetic profile of GLPG1837 is attractive, showing a low Cl,unb and good F% in both rat and dog. The CL (L/h/kg) of GLPG1837 after intravenous injection of 1 mg/kg dose are 1.92 and 0.32 in rats and dogs, respectively. T_1/2 is 1.84 h in rats while 3 h in dogs. After 5 mg/kg p.o, the oral availability of GLPG1837 in rat is 67%. In dogs, F%>100^[1].

プロトコル(参考用のみ)

参考

[1] Van der Plas SE, et al. J Med Chem. 2018, 61(4):1425-1435.

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：

Molecular dynamics and functional characterization of I37R-CFTR lasso mutation provide insights into channel gating activity [ iScience, 2022, 25(1):103710]	PubMed: 35072004
In Vitro Rescue of the Bile Acid Transport Function of ABCB11 Variants by CFTR Potentiators [ Int J Mol Sci, 2022, 23(18)10758]	PubMed: 36142670
Pharmacological Responses of the G542X-CFTR to CFTR Modulators [ Front Mol Biosci, 2022, 9:921680]	PubMed: 35813815
Primary human nasal epithelial cells: biobanking in the context of precision medicine [ Biology, 2022, (182)-]	PubMed: None
Primary Human Nasal Epithelial Cells: Biobanking in the Context of Precision Medicine [ J Vis Exp, 2022, (182)]	PubMed: 35532277
Utilisation of CFTR orthologues to evaluate new therapies for cystic fibrosis [ University of Bristol, 2022, ]	PubMed: None
Nanomolar-potency 'co-potentiator' therapy for cystic fibrosis caused by a defined subset of minimal function CFTR mutants. [ Sci Rep, 2019, 9(1):17640]	PubMed: 31776420

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。