Tertiapin-Q, Blocker of Kir Channels Tertiapin has been isolated from the venom of the Honeybee Apis mellifera. Tertiapin-Q is an oxidation-resistant mutant of the wild-type tertiapin where Methionine 13 has been replaced by a Glutamine. Tertiapin-Q blocks the inwardly rectifying Kir1.1 (ROMK1) and Kir3.1/3.4 (GIRK1/GIRK4 also known as IKACh) potassium channels with Kd values of around 2 nM and 8 nM respectively. Tertiapin-Q also inhibits calcium-activated large conductance BK potassium channels (KCa1.1) in a concentration and voltage-dependent manner (IC50 ~ 5 nM), in addition to inhibiting Kir3.1/3.2 (GIRK1/GIRK2) heteromultimer potassium channels with a Kd close to 270 nM. Tertiapin-Q can prevent dose-dependent acetylcholine(ACh)-induced atrioventricular blocks in mammalian hearts, as KCNJ3/KCNJ5 channels (also named I(KACh)), are activated by ACh found in mammalian myocytes. Tertiapin-Q technical information AA sequence: Ala-Leu-Cys3-Asn-Cys5-Asn-Arg-Ile-Ile-Ile-Pro-His-Gln-Cys14-Trp-Lys-Lys-Cys18-Gly-Lys-Lys-NH2 Disulfide bonds: Cys3-Cys14 and Cys5-Cys18 Length (aa): 21 Formula: C106H175N35O24S4 Molecular Weight: 2452 Da Appearance: White lyophilized solid Solubility: water and saline buffer CAS number: [252198-49-5] Source: Synthetic Purity rate: > 97 % http://www.smartox-biotech.com/en/potassium-channel/130-tertiapin-q

Smartox Biotechnology is specialized in supplying the life science research community with biological materials issued from animal's venoms. The company offers venom peptides for basic research and drug discovery solutions based on its venom collection and expertise.