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AB141517

BCTC, inhibitor of TRPV1

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(2 Publications)

MW 372.9 Da, Purity >98%. Potent inhibitor of TRPV1 (IC50 values are 35 and 6 nM for capsaicin and acid-induced activation respectively). Inhibits TRPM8 (IC50 = 0.8 μM). Reduces hyperalgesia in vivo..

View Alternative Names

Capsaicin receptor, DKFZp434K0220, Eag-related protein 1, Ether a go go related potassium channel protein, Ether-a-go-go-related gene potassium channel 1, Ether-a-go-go-related protein 1, H-ERG, KCNH2_HUMAN, Kv11.1, LQT 2, LTrpC-6, Long transient receptor potential channel 6, MGC2849, OTRPC1, Osm-9-like TRP channel 1, Potassium channel HERG, Potassium voltage gated channel subfamily H (eag related) member 2, Potassium voltage-gated channel subfamily H member 2, SQT1, Short form of the TRPM8 cationic channel, TRPM8_HUMAN, TRPV1_HUMAN, Transient receptor potential cation channel subfamily M member 8, Transient receptor potential cation channel subfamily V member 1, Trp-p8, VR 1, Vanilloid receptor 1, Vanilloid receptor subtype 1, Voltage gated potassium channel, subfamily H, member 2, Voltage-gated potassium channel subunit Kv11.1, eag homolog, hERG-1, transient receptor potential-p8

1 Images
Chemical Structure - BCTC, inhibitor of TRPV1 (AB141517)
  • Chemical Structure

Lab

Chemical Structure - BCTC, inhibitor of TRPV1 (AB141517)

2D chemical structure image of ab141517, BCTC, inhibitor of TRPV1

Key facts

CAS number

393514-24-4

Purity

>98%

Form

Solid

form

Molecular weight

372.9 Da

Molecular formula

C<sub>2</sub><sub>0</sub>H<sub>2</sub><sub>5</sub>ClN<sub>4</sub>O

PubChem

9929425

Nature

Synthetic

Solubility

Soluble in DMSO to 50 mM

Soluble in ethanol to 25 mM (with warming)

Biochemical name

Bctc

Biological description

Potent inhibitor of TRPV1 (IC50 values are 35 and 6 nM for capsaicin and acid-induced activation respectively). Inhibits TRPM8 (IC50 = 0.8 μM). Reduces hyperalgesia in vivo.

Canonical smiles

CC(C)(C)C1=CC=C(C=C1)NC(=O)N2CCN(CC2)C3=C(C=CC=N3)Cl

InChi

InChI=1S/C20H25ClN4O/c1-20(2,3)15-6-8-16(9-7-15)23-19(26)25-13-11-24(12-14-25)18-17(21)5-4-10-22-18/h4-10H,11-14H2,1-3H3,(H,23,26)

InChiKey

ROGUAPYLUCHQGK-UHFFFAOYSA-N

IUPAC Name

N-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl)piperazine-1-carboxamide

Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
Ambient
Appropriate long-term storage conditions
Ambient
Storage information
The product can be stored for up to 12 months

Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

TRPV1 also known as the transient receptor potential cation channel subfamily V member 1 is a non-selective cation channel with a molecular mass of approximately 95 kDa. TRPV1 is widely expressed in sensory neurons especially within the dorsal root and trigeminal ganglia. It serves as a molecular sensor for noxious heat and capsaicin the active component in chili peppers. TRPM8 another member of the transient receptor potential family often referred to as the cold and menthol receptor 1 has a role in sensing cold temperatures and menthol. It is mainly located in the trigeminal and dorsal root ganglia. On the other hand h-ERG the human ether-a-go-go-related gene potassium channel plays an important role in cardiac repolarization mainly expressed in the heart's cardiac tissue.
Biological function summary

These ion channels contribute to sensory perception and cellular signaling. TRPV1 directly participates in the detection of painful stimuli and is a single-channel entity. TRPM8 engages in cold sensation and like TRPV1 operates as an independent channel. H-ERG while distinct from TRPV1 and TRPM8 is essential for maintaining cardiac rhythm by contributing to the electrical activity through rapid potassium ion currents and it often exists as part of a larger protein complex.

Pathways

TRPV1 and TRPM8 engage in the sensory signal transduction pathway influencing the perception of temperature changes. TRPV1 can interact with several proteins like calmodulin that modulate its activity. TRPM8 similarly interfaces with signaling molecules including phosphatidylinositol 45-bisphosphate (PIP2). H-ERG is critical in the cardiac action potential pathway where it interacts with KCNE family proteins that affect cardiac conduction.

TRPV1 and TRPM8 are associated with pain and thermal sensitivity pathologies including chronic pain conditions. TRPV1 has connections with inflammatory proteins such as PKC contributing to its activation in pain pathways. H-ERG mutations or dysfunctions relate to cardiac conditions such as Long QT syndrome where abnormal ion channel activity can lead to arrhythmias. Furthermore h-ERG can be affected by other cardiac-related proteins like KCNQ1 impacting heart electrical stability.

Product protocols

Publications (2)

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APL bioengineering 7:016114 PubMed36968453

2023

Optimal low-intensity pulsed ultrasound stimulation for promoting anti-inflammatory effects in macrophages.

Applications

Unspecified application

Species

Unspecified reactive species

Francesco Iacoponi,Andrea Cafarelli,Francesco Fontana,Tiziano Pratellesi,Erik Dumont,Ivana Barravecchia,Debora Angeloni,Leonardo Ricotti

Annals of translational medicine 9:1470 PubMed34734022

2021

Cold-inducible RNA-binding protein migrates from the nucleus to the cytoplasm under cold stress in normal human bronchial epithelial cells via TRPM8-mediated mechanism.

Applications

Unspecified application

Species

Unspecified reactive species

Liang-Ping Mao,Yan Jiao,Jian-Hua Xiang,Xin-Wei Luo,Qian He,Dan-Hua Ran,Qing Xu,Chun-Hui Lang,Ling-Xiu Chen
View all publications

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