Tertiapin-Q trifluoroacetate salt

Modify Date: 2024-01-03 13:02:55

Tertiapin-Q trifluoroacetate salt structure	Common Name	Tertiapin-Q trifluoroacetate salt
	CAS Number	910044-56-3	Molecular Weight	2452.004
	Density	1.5±0.1 g/cm3	Boiling Point	N/A
	Molecular Formula	C₁₀₆H₁₇₅N₃₅O₂₄S₄	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of Tertiapin-Q trifluoroacetate salt

Tertiapin-Q is a highly selective blocker of GIRK1/4 heterodimer and ROMK1 (Kir1.1).

Name	Tertiapin-Q
Synonym	More Synonyms

Description	Tertiapin-Q is a highly selective blocker of GIRK1/4 heterodimer and ROMK1 (Kir1.1).
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel Research Areas >> Cardiovascular Disease Peptides
Target	Potassium channel[1]
In Vitro	Tertiapin-Q is a highly selective blocker of G protein-coupled inwardly rectifying potassium (GIRK1/4) heterodimer and renal outer medullary potassium channel (ROMK1, Kir1.1)[1]. Tertiapin-Q is a potent and selective blocker for Kir1.1 renal outer medullary potassium, Kir3.1-Kir3.4 channels and calcium activated large conductance potassium channels (big potassium channels). The somatostatin (SS-14)-activated current is almost completely blocked (93.2±2.9%, n=5; P<0.01) by preincubation with the G protein-coupled inwardly rectifying potassium (GIRK) channel blocker Tertiapin-Q (TPN-Q)[2].
In Vivo	Tertiapin-Q is a muscarinic acetylcholine receptor-operated K+ current (IK,Ach) blocker. After the cessation of rapid atrial pacing, the atrial effective refractory period (AERP) is unchanged during the experimental period in the rapid atrial pacing (RAP) rabbits (n=6). Bepridil (1 mg/kg, n=5 for each group), Amiodarone (10 mg/kg, n=5 for each group), Vernakalant (3 mg/kg, n=5 for each group), Ranolazine (10 mg/kg, n=6 for each group) or Tertiapin-Q (0.03 mg/kg, n=5 for each group) on the AERP in the control and RAP rabbits. Tertiapin-Q significantly prolongs the AERP at each pacing cycle length both in the control and RAP rabbits. The extents of prolonging effect of Tertiapin-Q on the AERP in the RAP rabbits are greater than those in the control animals[3].
Animal Admin	Rabbits[3] Male New Zealand White rabbits weighing 3.0-3.5 kg are used for this study. Effects of Vernakalant, Ranolazine and Tertiapin-Q on the atrial effective refractory period (AERP) in the control and rapid atrial pacing (RAP) rabbits. Vernakalant (left panels, 3 mg/kg, n=5 for each group), Ranolazine (middle panels; 10 mg/kg, n=6 for each group) or Tertiapin-Q (right panels; 0.03 mg/kg, n=5 for each group) is intravenously administered to the control or RAP rabbits. AERP is measured before and 10 min after the administration of each drug, which are shown in the lower panels.
References	[1]. Picton LD, et al. Mechanisms underlying the endogenous dopaminergic inhibition of spinal locomotor circuit function in Xenopus tadpoles. Sci Rep. 2016 Oct 20;6:35749. [2]. Günther T, et al. Research Resource: Real-Time Analysis of Somatostatin and Dopamine Receptor Signaling in Pituitary Cells Using a Fluorescence-Based Membrane Potential Assay. Mol Endocrinol. 2016 Apr;30(4):479-90. [3]. Chiba T, et al. Influences of rapid pacing-induced electrical remodeling on pharmacological manipulation of the atrial refractoriness in rabbits. J Pharmacol Sci. 2016 Mar;130(3):170-6.

Density	1.5±0.1 g/cm3
Molecular Formula	C₁₀₆H₁₇₅N₃₅O₂₄S₄
Molecular Weight	2452.004
Exact Mass	2450.243164
LogP	-9.12
Index of Refraction	1.693
Storage condition	2-8℃

N-{[(1R,4S,7S,10S,16S,19S,22S,25S,28S,31R,36R,39S,42S,45S,52R,55S)-52-[(L-Alanyl-L-leucyl)amino]-39,42-bis(4-aminobutyl)-28,55-bis(2-amino-2-oxoethyl)-4-(3-amino-3-oxopropyl)-16,22-di[(2S)-2-butanyl]-19-sec-butyl-25-(3-carbamimidamidopropyl)-7-(1H-imidazol-4-ylmethyl)-45-(1H-indol-3-ylmethyl)-3,6,9,15,18,21,24,27,30,38,41,44,47,53,56-pentadecaoxo-33,34,49,50-tetrathia-2,5,8,14,17,20,23,26,29,37,40,43,46,54,57-pentadecaazatricyclo[29.16.10.0

L-Lysinamide, N-[[(3S,6S,9R,12S,15S,18S,21R,26R,29S,32S,35S,38S,41S,46aS,49S,52R)-15,18-bis(4-aminobutyl)-32-[3-[(aminoiminomethyl)amino]propyl]-29,49-bis(2-amino-2-oxoethyl)-6-(3-amino-3-oxopropyl)-52-[[(2S)-2-[[(2S)-2-amino-1-oxopropyl]amino]-4-methyl-1-oxopentyl]amino]tetratetracontahydro-3-(1H-imidazol-4-ylmethyl)-12-(1H-indol-3-ylmethyl)-35,41-bis[(1S)-1-methylpropyl]-38-(1-methylpropyl)-1,4,7,10,13,16,19,27,30,33,36,39,42,48,51-pentad

DC Chemicals Limited
China
Product Name: Tertiapin-Q
Price: ￥Inquiry/1g
Purity: 98.9%
Stocking Period: 1 Day
Contact: Tony Cao

Zhejiang Hangyu API Co., Ltd
China
Product Name: Tertiapin Q
Price: $Inquiry/1kg
Purity: 99.0%
Stocking Period: 1 Day
Contact: Vinnie

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Tertiapin-Q trifluoroacetate salt

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Tertiapin-Q trifluoroacetate salt Biological Activity

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