Grouped product items

SKU

Size

Availability

Price

Qty

V127056-5mg

5mg

Available within 4-8 weeks(?)

$90.90

V127056-10mg

10mg

Available within 4-8 weeks(?)

$155.90

V127056-50mg

50mg

Available within 4-8 weeks(?)

$702.90

V127056-100mg

100mg

In stock

$1,263.90

V127056-250mg

250mg

In stock

$2,843.90

V127056-1g

In stock

$10,235.90

Basic Description

Synonyms	Ivacaftor\|873054-44-5\|VX-770\|Kalydeco\|Ivacaftor (VX-770)\|N-(2,4-di-tert-butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide\|VX 770\|ivacaftorum\|CHEBI:66901\|UNII-1Y740ILL1Z\|Ivacaftor-d18\|N-[2,4-Bis(tert-butyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxo-
Specifications & Purity	Moligand™, ≥98%
Biochemical and Physiological Mechanisms	Ivacaftor is a CFTR activator (IC50 of 43 ± 38 nM). In some cells Ivacaftor was shown to increase CFTR channel open probability in the F508del processing and the G551D gating mutations. In cultured human CF bronchial epithelia (HBE) expressing the F551D g
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads
Grade	Moligand™
Action Type	ACTIVATOR
Mechanism of action	Activator of CFTR
Note	5mg、50mg、10mg卖完停产，不再备货
Product Description	Ivacaftor (VX-770) is a potentiator of CFTR targeting G551D-CFTR and F508del-CFTR with EC50 of 100 nM and 25 nM, respectively. Is a CFTR activator

Product Properties

ALogP	5.6

Associated Targets

CTNNBIP1 Tbio Beta-catenin-interacting protein 1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CYP1A2 Tchem Cytochrome P450 1A2 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CYP2D6 Tclin Cytochrome P450 2D6 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CNR1 Tclin Cannabinoid receptor 1 0 Activities

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CYP2C19 Tchem Cytochrome P450 2C19 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

DRD1 Tclin D(1A) dopamine receptor 0 Activities

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DRD2 Tclin D(2) dopamine receptor 0 Activities

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CYP3A4 Tclin Cytochrome P450 3A4 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CFTR Tclin Cystic fibrosis transmembrane conductance regulator 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ESR1 Tclin Estrogen receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GABRA1 Tclin Gamma-aminobutyric acid receptor subunit alpha-1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

NR3C1 Tclin Glucocorticoid receptor 0 Activities

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CYP2C9 Tchem Cytochrome P450 2C9 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AVPR1A Tclin Vasopressin V1a receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HDAC6 Tclin Histone deacetylase 6 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HRH1 Tclin Histamine H1 receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SLC6A2 Tclin Sodium-dependent noradrenaline transporter 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SLC6A3 Tclin Sodium-dependent dopamine transporter 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SLC6A4 Tclin Sodium-dependent serotonin transporter 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PDE4D Tclin cAMP-specific 3',5'-cyclic phosphodiesterase 4D 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PDE3A Tclin cGMP-inhibited 3',5'-cyclic phosphodiesterase A 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PTGS1 Tclin Prostaglandin G/H synthase 1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PTGS2 Tclin Prostaglandin G/H synthase 2 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CACNA1C Tclin Voltage-dependent L-type calcium channel subunit alpha-1C 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

DRD3 Tclin D(3) dopamine receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CHRM3 Tclin Muscarinic acetylcholine receptor M3 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADRA2B Tclin Alpha-2B adrenergic receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CHRM2 Tclin Muscarinic acetylcholine receptor M2 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADRA2C Tclin Alpha-2C adrenergic receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR2A Tclin 5-hydroxytryptamine receptor 2A 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADORA2A Tclin Adenosine receptor A2a 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CHRM1 Tclin Muscarinic acetylcholine receptor M1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADRA2A Tclin Alpha-2A adrenergic receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADRB1 Tclin Beta-1 adrenergic receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADRA1A Tclin Alpha-1A adrenergic receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AR Tclin Androgen receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAOA Tclin Amine oxidase [flavin-containing] A 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR2C Tclin 5-hydroxytryptamine receptor 2C 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADORA1 Tclin Adenosine receptor A1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR1A Tclin 5-hydroxytryptamine receptor 1A 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADORA3 Tchem Adenosine receptor A3 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR3A Tclin 5-hydroxytryptamine receptor 3A 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR2B Tclin 5-hydroxytryptamine receptor 2B 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

OPRD1 Tclin Delta-type opioid receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

OPRK1 Tclin Kappa-type opioid receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

OPRM1 Tclin Mu-type opioid receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MLNR Tchem Motilin receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

IUPAC Name	N-(2,4-ditert-butyl-5-hydroxyphenyl)-4-oxo-1H-quinoline-3-carboxamide
INCHI	InChI=1S/C24H28N2O3/c1-23(2,3)16-11-17(24(4,5)6)20(27)12-19(16)26-22(29)15-13-25-18-10-8-7-9-14(18)21(15)28/h7-13,27H,1-6H3,(H,25,28)(H,26,29)
InChi Key	PURKAOJPTOLRMP-UHFFFAOYSA-N
Canonical SMILES	CC(C)(C)C1=CC(=C(C=C1NC(=O)C2=CNC3=CC=CC=C3C2=O)O)C(C)(C)C
Isomeric SMILES	CC(C)(C)C1=CC(=C(C=C1NC(=O)C2=CNC3=CC=CC=C3C2=O)O)C(C)(C)C
PubChem CID	16220172
Molecular Weight	392.49

Database links

PubChem CID	16220172
ChEBI	CHEBI:66901
CAS Registry No.	873054-44-5
Wikipedia	Ivacaftor
ChEMBL Ligand	CHEMBL2010601
DrugBank Ligand	DB08820
PEP	ivacaftor
RCSB PDB Ligand	VX7
Reactome Reaction	R-HSA-5679000, R-HSA-5678992
Reactome Drug	R-ALL-5678956
DrugCentral Ligand	4228

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section

5 results found

Lot Number	Certificate Type	Date	Item
G1530068	Certificate of Analysis	May 10, 2023	V127056
L2014259	Certificate of Analysis	Oct 15, 2022	V127056
K2218877	Certificate of Analysis	Aug 22, 2022	V127056
K2218907	Certificate of Analysis	Aug 22, 2022	V127056
K2218908	Certificate of Analysis	Aug 22, 2022	V127056

Chemical and Physical Properties

Solubility	DMSO 78 mg/mL Water <1 mg/mL Ethanol <1 mg/mL

Safety and Hazards(GHS)

Pictogram(s)	GHS08, GHS07
Signal	Warning
Hazard Statements	H315:Causes skin irritation H319:Causes serious eye irritation H335:May cause respiratory irritation H361:Suspected of damaging fertility or the unborn child
Precautionary Statements	P261:Avoid breathing dust/fume/gas/mist/vapors/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. P280:Wear protective gloves/protective clothing/eye protection/face protection. P302+P352:IF ON SKIN: wash with plenty of water. P321:Specific treatment (see ... on this label). P405:Store locked up. P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P271:Use only outdoors or in a well-ventilated area. P304+P340:IF INHALED: Remove person to fresh air and keep comfortable for breathing. P403+P233:Store in a well-ventilated place. Keep container tightly closed. P362+P364:Take off contaminated clothing and wash it before reuse. P203:Obtain, read and follow all safety instructions before use. P264+P265:Wash hands [and …] thoroughly after handling. Do not touch eyes. P318:if exposed or concerned, get medical advice. P337+P317:If eye irritation persists: Get medical help. P332+P317:If skin irritation occurs: Get medical help. P319:Get medical help if you feel unwell.

References

1. Van Goor F, Hadida S, Grootenhuis PD, Burton B, Cao D, Neuberger T, Turnbull A, Singh A, Joubran J, Hazlewood A et al.. (2009) Rescue of CF airway epithelial cell function in vitro by a CFTR potentiator, VX-770.. Proc Natl Acad Sci USA, 106 (44): (18825-30). [PMID:19846789]
2. Eckford PD, Li C, Ramjeesingh M, Bear CE. (2012) Cystic fibrosis transmembrane conductance regulator (CFTR) potentiator VX-770 (ivacaftor) opens the defective channel gate of mutant CFTR in a phosphorylation-dependent but ATP-independent manner.. J Biol Chem, 287 (44): (36639-49). [PMID:22942289]

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SKU	Size	Availability	Price
V127056-5mg	5mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$90.90
V127056-10mg	10mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$155.90
V127056-50mg	50mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$702.90
V127056-100mg	100mg	In stock	$1,263.90
V127056-250mg	250mg	In stock	$2,843.90
V127056-1g	1g	In stock	$10,235.90

Ivacaftor (VX-770) - ≥98%, high purity , CAS No.873054-44-5, Activator of CFTR

Basic Description

Product Properties

Associated Targets

CTNNBIP1 Tbio Beta-catenin-interacting protein 1 0 Activities

CYP1A2 Tchem Cytochrome P450 1A2 0 Activities

CYP2D6 Tclin Cytochrome P450 2D6 0 Activities

CNR1 Tclin Cannabinoid receptor 1 0 Activities

CYP2C19 Tchem Cytochrome P450 2C19 0 Activities

DRD1 Tclin D(1A) dopamine receptor 0 Activities

DRD2 Tclin D(2) dopamine receptor 0 Activities

CYP3A4 Tclin Cytochrome P450 3A4 0 Activities

CFTR Tclin Cystic fibrosis transmembrane conductance regulator 0 Activities

ESR1 Tclin Estrogen receptor 0 Activities

GABRA1 Tclin Gamma-aminobutyric acid receptor subunit alpha-1 0 Activities

NR3C1 Tclin Glucocorticoid receptor 0 Activities

CYP2C9 Tchem Cytochrome P450 2C9 0 Activities

AVPR1A Tclin Vasopressin V1a receptor 0 Activities

HDAC6 Tclin Histone deacetylase 6 0 Activities

HRH1 Tclin Histamine H1 receptor 0 Activities

SLC6A2 Tclin Sodium-dependent noradrenaline transporter 0 Activities

SLC6A3 Tclin Sodium-dependent dopamine transporter 0 Activities

SLC6A4 Tclin Sodium-dependent serotonin transporter 0 Activities

PDE4D Tclin cAMP-specific 3',5'-cyclic phosphodiesterase 4D 0 Activities

PDE3A Tclin cGMP-inhibited 3',5'-cyclic phosphodiesterase A 0 Activities

PTGS1 Tclin Prostaglandin G/H synthase 1 0 Activities

PTGS2 Tclin Prostaglandin G/H synthase 2 0 Activities

CACNA1C Tclin Voltage-dependent L-type calcium channel subunit alpha-1C 0 Activities

DRD3 Tclin D(3) dopamine receptor 0 Activities

CHRM3 Tclin Muscarinic acetylcholine receptor M3 0 Activities

ADRA2B Tclin Alpha-2B adrenergic receptor 0 Activities

CHRM2 Tclin Muscarinic acetylcholine receptor M2 0 Activities

ADRA2C Tclin Alpha-2C adrenergic receptor 0 Activities

HTR2A Tclin 5-hydroxytryptamine receptor 2A 0 Activities

ADORA2A Tclin Adenosine receptor A2a 0 Activities

CHRM1 Tclin Muscarinic acetylcholine receptor M1 0 Activities

ADRA2A Tclin Alpha-2A adrenergic receptor 0 Activities

ADRB1 Tclin Beta-1 adrenergic receptor 0 Activities

ADRA1A Tclin Alpha-1A adrenergic receptor 0 Activities

AR Tclin Androgen receptor 0 Activities

MAOA Tclin Amine oxidase [flavin-containing] A 0 Activities

HTR2C Tclin 5-hydroxytryptamine receptor 2C 0 Activities

ADORA1 Tclin Adenosine receptor A1 0 Activities

HTR1A Tclin 5-hydroxytryptamine receptor 1A 0 Activities

ADORA3 Tchem Adenosine receptor A3 0 Activities

HTR3A Tclin 5-hydroxytryptamine receptor 3A 0 Activities

HTR2B Tclin 5-hydroxytryptamine receptor 2B 0 Activities

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 0 Activities

OPRD1 Tclin Delta-type opioid receptor 0 Activities

OPRK1 Tclin Kappa-type opioid receptor 0 Activities

OPRM1 Tclin Mu-type opioid receptor 0 Activities

MLNR Tchem Motilin receptor 0 Activities

Names and Identifiers

Database links

Certificates

Certificate of Analysis(COA)

Chemical and Physical Properties

Safety and Hazards(GHS)

Related Documents

References

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