数量	カタログ番号	注文内容	Qty/Pk	価格
			96-Well Plate

数量	カタログ番号	注文内容	Qty/Pk	価格
	48-602MAG	Buffer Detection Kit for Magnetic Beads	1 Kit

530541 Sigma-AldrichCFTR Potentiator, VX-770 - CAS 873054-44-5 - Calbiochem

A cell-permeable, potentiator of CFTR that directly, reversibly, and allosterically binds to WT and G551D mutant forms (~ 10 µM) and increases the open probability to restore lung function.

CFTR Potentiator, VX-770 - CAS 873054-44-5 - Calbiochem: のSDS（安全データシート）、CoA（試験成績書）およびCoQ（品質証明書）、カタログなど製品関連の技術資料を入手いただけます。

(M)SDS
参考資料
Data Sheet

同義語: Cystic Fibrosis Transmembrane Conductance Regulator Potentiator, VX 770, Ivacaftor, Kalydeco, N-(5-Hydroxy-2,4-bis(2-methyl-2-propanyl)phenyl]-4-oxo-1,4-dihydro-3-quinolinecarboxamide

Primary Target: WT and G551D mutant forms of cell surface CFTR

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概要

Replacement Information

主要スペック表

CAS #	Empirical Formula
873054-44-5	C₂₄H₂₈N₂O₃

価格＆在庫状況

カタログ番号	在庫状況	包装	Qty/Pk	価格	数量
5.30541.0001	在庫状況検索中… — 現在国内在庫なし現在国内在庫有り販売中止在庫僅少現在国内在庫あり在庫を照会するにはログインしてください現在国内在庫有り現在国内在庫なし現在国内在庫有り Remaining : Will advise Remaining : Will advise 注文対象外お問合せください Contact Customer Service お問合せくださいお問合せください	ｶﾞﾗｽﾋﾞﾝ	10 mg	価格を検索中… 価格が見つかりません Minimum Quantity needs to be mulitiple of Maximum Quantity is 弊社照会詳細を表示　値引 () — 弊社照会納入価格を閲覧するにはログインしてください	在庫状況を照会 —	お気に入り/ショッピングリストに追加お気に入り/ショッピングリストに追加お気に入りに追加されました

Description
Overview	A cell-permeable, orally bioavailable dihydroquinoline-carboxamide compound that acts as a potentiator of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) by directly binding to WT and G551D mutant forms in an allosteric and reversible manner (~ 10 µM) and increases the open probability to restore lung function. Enhances cAMP/PKA-signaling mediated gating activity of both WT and G551D mutants and its potentiation activity is dependent upon the phosphorylated status of CFTR. Does not compete for binding to the canonical ATP-binding catalytic site; but the rate of flux through CFTR increase by 1.5 to 2 fold when ATP concentrations are increased. Shown to increase Cl^- secretion by about 10 fold in cultured human CF bronchial epethelia (HBE) carrying G551D/F508del mutations and increases forskolin-stimulated transepethial current (IT; EC₅₀ = 236 nM) far more effectively than genistein (EC₅₀ = 16 µM). Displays favorable pharmacokinetic properties with t_1/2= 12 h. Please note that the molecular weight for this compound is batch-specific due to variable water content.
Catalogue Number	530541
Brand Family	Calbiochem®
Synonyms	Cystic Fibrosis Transmembrane Conductance Regulator Potentiator, VX 770, Ivacaftor, Kalydeco, N-(5-Hydroxy-2,4-bis(2-methyl-2-propanyl)phenyl]-4-oxo-1,4-dihydro-3-quinolinecarboxamide

References
References	Namkung, W., et al. 2013. Mol. Pharmacol. 84, 384. Eckford, P.D.W., et al. 2012. J. Biol. Chem. 287, 36639. Van Goor, F., et al 2009. Proc. Natl. Acad. Sci. USA 106, 18825.

Product Information
CAS number	873054-44-5
Form	Off-white powder
Hill Formula	C₂₄H₂₈N₂O₃
Chemical formula	C₂₄H₂₈N₂O₃
Reversible	Y
Structure formula Image
Quality Level	MQ100

Applications

Biological Information
Primary Target	WT and G551D mutant forms of cell surface CFTR
Purity	≥98% by HPLC

Physicochemical Information
Cell permeable	Y

Dimensions

Materials Information

Toxicological Information

Safety Information according to GHS

Safety Information

Product Usage Statements

Storage and Shipping Information
Ship Code	Ambient Temperature Only
Toxicity	Standard Handling
Storage	+2°C to +8°C
Protect from Light	Protect from light
Do not freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Packaging Information
Packaged under inert gas	Packaged under inert gas

Transport Information

Supplemental Information

Specifications

Global Trade Item Number
カタログ番号	GTIN
5.30541.0001	04055977260908

Documentation

CFTR Potentiator, VX-770 - CAS 873054-44-5 - Calbiochem (M)SDS

タイトル
英語版製品安全データシート（(M)SDS）

参考資料

参考資料の概要
Namkung, W., et al. 2013. Mol. Pharmacol. 84, 384. Eckford, P.D.W., et al. 2012. J. Biol. Chem. 287, 36639. Van Goor, F., et al 2009. Proc. Natl. Acad. Sci. USA 106, 18825.

データシート

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision	13-June-2014 JSW
Synonyms	Cystic Fibrosis Transmembrane Conductance Regulator Potentiator, VX 770, Ivacaftor, Kalydeco, N-(5-Hydroxy-2,4-bis(2-methyl-2-propanyl)phenyl]-4-oxo-1,4-dihydro-3-quinolinecarboxamide
Description	A cell-permeable, orally bioavailable dihydroquinoline-carboxamide compound that acts as a potentiator of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) by directly binding to WT and G551D mutant forms in an allosteric and reversible manner (~ 10 µM) and increases the open probability to restore lung function. Enhances cAMP/PKA-signaling mediated gating activity of both WT and G551D mutants and its potentiation activity is dependent upon the phosphorylated status of CFTR. Does not compete for binding to the canonical ATP-binding catalytic site; but the rate of flux through CFTR increase by 1.5 to 2 fold when ATP concentrations are increased. Shown to increase Cl^- secretion by about 10 fold in cultured human CF bronchial epethelia (HBE) carrying G551D/F508del mutations and increases forskolin-stimulated transepethial current (IT; EC₅₀ = 236 nM) far more effectively than genistein (EC₅₀ = 16 µM). Displays favorable pharmacokinetic properties with t_1/2= 12 h.
Form	Off-white powder
Intert gas (Yes/No)	Packaged under inert gas
CAS number	873054-44-5
Chemical formula	C₂₄H₂₈N₂O₃
Structure formula
Purity	≥98% by HPLC
Solubility	DMSO (100 mg/ml)
Storage	Protect from light +2°C to +8°C
Do Not Freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity	Standard Handling
References	Namkung, W., et al. 2013. Mol. Pharmacol. 84, 384. Eckford, P.D.W., et al. 2012. J. Biol. Chem. 287, 36639. Van Goor, F., et al 2009. Proc. Natl. Acad. Sci. USA 106, 18825.

カテゴリー

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Inducers

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