Product Description
Size: 10mg / 50mg
MW 372.9 Da, Purity >98%. Potent inhibitor of TRPV1 (IC 50 values are 35 and 6 nM for capsaicin and acid-induced activation respectively) . Inhibits TRPM8 (IC 50 = 0.8 μM). Reduces hyperalgesia in vivo. .
Key facts
CAS number:393514-24-4,
Purity:>98%,
Form:SolidSee storage information,
Molecular weight:372.9 Da,
Molecular formula:C20H25ClN4O,
PubChem:9929425,
Nature:Synthetic,
Solubility:Soluble in DMSO to 50 mMSoluble 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.
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Collaboration
Tony Tang
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