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1-PHENYL-3,3-BIS(PYRIDIN-4-YLMETHYL)INDOLIN-2-ONE DIHYDROCHLORIDE

Name: 1-PHENYL-3,3-BIS(PYRIDIN-4-YLMETHYL)INDOLIN-2-ONE DIHYDROCHLORIDE
Brand: 2A Biotech
SKU: 2A-0109625

CAS Number105431-72-9

Synonymslinopiridine; Dup 996; Linopirdine

Molecular FormulaC26H21O1N3

Molecular Weight391.47

Purity96+%

Density1.255 g/cm3

Boiling Point655.9ºC at 760 mmHg

EINECS0

MSDSChinese English

Cat. No.: 2A-0109625 Purity: 96+%

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Quality Control of [ 105431-72-9 ] Purity: 96+% SDS Specification MoL

Chemical & Physical Properties
CAS Number	105431-72-9
Catalog No.	2A-0109625
Chinese Name	利诺吡啶 (DUP996)
Synonyms	linopiridine; Dup 996; Linopirdine
Molecular Formula	C26H21O1N3
Molecular Weight	391.47
Purity	96+
Density	1.255 g/cm3
Boiling Point	655.9ºC at 760 mmHg
Storage Condition	2-8°C, sealed, dry
Application	Linopirdine (DuP 996) is an orally active, selective inhibitor of M-type K+ currents (IM; Kv7; KCNQ Channels) with an IC50 of 2.4 μM. Linopirdine is a TRPV1 activator. Linopirdine is a recognized cogn
EINECS	0
HTC	2933790090
UN(IATA)	0
MDL Number	MFCD00867216
SMILES	O=C1N(c2ccccc2)c2ccccc2C1(Cc1ccncc1)Cc1ccncc1
InChI	InChI=1S/C26H21N3O/c30-25-26(18-20-10-14-27-15-11-20,19-21-12-16-28-17-13-21)23-8-4-5-9-24(23)29(25)22-6-2-1-3-7-22/h1-17H,18-19H2
InChI Key	YEJCDKJIEMIWRQ-UHFFFAOYSA-N
MSDS	msds/109625_1_105431_72_9.pdf
Bioactivity	Linopirdine (DuP 996) is an orally active, selective M-type K+ current (IM; Kv7; KCNQ Channels) inhibitor with an IC50 of 2.4 μM. Linopirdine is a TRPV1 agonist. Linopirdine, a putative cognition enhancing drug, increases acetylcholine release in rat brain tissue[1][2][3]. Related Catalog Signaling Pathways >> Membrane Transporter/Ion Channel >> TRP Channel Research Areas >> Neurological Disease Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel Target IC50: 2.4 μM (M-type K+ current)[1] In Vitro Linopirdine (DuP 996) inhibits IC (measured as a medium afterhyperpolarization tail current, ImAHP) with an IC50 of 16.3 μM. Linopirdine (100 μM) weakly inhibits the K+ leak current, IL, the transient outward current, IA, the delayed rectifier, IK, and the slow component of IAHP, by 28, 37, 36 and 52 percent, respectively. The mixed Na+/K+ inward rectifying current, IQ, is essentially unaffected by Linopirdine (IC50>300 μM)[1]. Linopirdine acts as an agonist of TRPV1 (transient receptor potential vanilloid type 1)[3]. In Vivo Linopirdine (DuP 996; i.v.; 0.1-6 mg/kg; increasing doses) transiently (10-15 min) and dose-dependently increases MAP by up to 15%[2]. Animal Model: Male Sprague-Dawley rats (300-350 g)[2] Dosage: 0.1, 0.5, 1, 3, 6 mg/kg Administration: 5 intravenous bolus injections of increasing doses Result: Transiently and dose-dependently increases MAP by up to 15%. References [1]. Schnee ME, et al. Selectivity of linopirdine (DuP 996), a neurotransmitter release enhancer, in blocking voltage-dependent and calcium-activated potassium currents in hippocampal neurons. J Pharmacol Exp Ther. 1998 Aug;286(2):709-17. [2]. Nassoiy SP, et al. Kv7 voltage-activated potassium channel inhibitors reduce fluid resuscitation requirements afterhemorrhagic shock in rats. J Biomed Sci. 2017 Jan 17;24(1):8. [3]. Neacsu C, et al. The M-channel blocker linopirdine is an agonist of the capsaicin receptor TRPV1. J Pharmacol Sci. 2010;114(3):332-40. Chemical & Physical Properties Density 1.255 g/cm3 Boiling Point 655.9ºC at 760 mmHg Molecular Formula C26H21N3O Molecular Weight 391.46400 Flash Point 350.5ºC Exact Mass 391.16800 PSA 46.09000 LogP 4.94310 Vapour Pressure 4.45E-17mmHg at 25°C Index of Refraction 1.669 InChIKey YEJCDKJIEMIWRQ-UHFFFAOYSA-N SMILES O=C1N(c2ccccc2)c2ccccc2C1(Cc1ccncc1)Cc1ccncc1
Use of	Linopirdine (DuP 996) is an orally active, selective M-type K+ current (IM; Kv7; KCNQ Channels) inhibitor with an IC50 of 2.4 μM. Linopirdine is a TRPV1 agonist. Linopirdine, a putative cognition enhancing drug, increases acetylcholine release in rat brain tissue[1][2][3]. Properties Articles40 Name 1-phenyl-3,3-bis(pyridin-4-ylmethyl)indol-2-one Synonym More Synonyms Linopirdine(DuP-996) Biological Activity Description Linopirdine (DuP 996) is an orally active, selective M-type K+ current (IM; Kv7; KCNQ Channels) inhibitor with an IC50 of 2.4 μM. Linopirdine is a TRPV1 agonist. Linopirdine, a putative cognition enhancing drug, increases acetylcholine release in rat brain tissue[1][2][3]. Related Catalog Signaling Pathways >> Membrane Transporter/Ion Channel >> TRP Channel Research Areas >> Neurological Disease Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel IC50: 2.4 μM (M-type K+ current)[1] In Vitro Linopirdine (DuP 996) inhibits IC (measured as a medium afterhyperpolarization tail current, ImAHP) with an IC50 of 16.3 μM. Linopirdine (100 μM) weakly inhibits the K+ leak current, IL, the transient outward current, IA, the delayed rectifier, IK, and the slow component of IAHP, by 28, 37, 36 and 52 percent, respectively. The mixed Na+/K+ inward rectifying current, IQ, is essentially unaffected by Linopirdine (IC50>300 μM)[1]. Linopirdine acts as an agonist of TRPV1 (transient receptor potential vanilloid type 1)[3]. References [1]. Schnee ME, et al. Selectivity of linopirdine (DuP 996), a neurotransmitter release enhancer, in blocking voltage-dependent and calcium-activated potassium currents in hippocampal neurons. J Pharmacol Exp Ther. 1998 Aug;286(2):709-17. [2]. Nassoiy SP, et al. Kv7 voltage-activated potassium channel inhibitors reduce fluid resuscitation requirements afterhemorrhagic shock in rats. J Biomed Sci. 2017 Jan 17;24(1):8. [3]. Neacsu C, et al. The M-channel blocker linopirdine is an agonist of the capsaicin receptor TRPV1. J Pharmacol Sci. 2010;114(3):332-40. Chemical & Physical Properties Molecular Formula C26H21N3O Exact Mass 391.16800 PSA 46.09000 LogP 4.94310 Index of Refraction 1.669 InChIKey YEJCDKJIEMIWRQ-UHFFFAOYSA-N
Tax Rebate	9.0%
Supervision	None MFN tariff: 9.0% Ordinary tariff: 20.0%
Transport Info	Product name: Summary 2933790090. other lactams. VAT:17.0%. Tax rebate rate:9.0%. . MFN tariff:9.0%. General tariff:20.0%

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1-PHENYL-3,3-BIS(PYRIDIN-4-YLMETHYL)INDOLIN-2-ONE DIHYDROCHLORIDE

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