(Syn. : TPN Q)
TERTIAPIN Q | Product ID | L8406-500UG |
| Name | TERTIAPIN Q |
| Molecular formula | C106H175N35O24S4 |
| Description |
A 21 amino-acids peptide with 2 disulfide bridges , synthetic, initially isolated from the venom of the European honey bee Apis mellifera. |
| Biological activity | 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 Tertiapin-Q is an oxidation-resistant mutant of the wild-type tertiapin where Methionine 13 has been replaced by a Glutamine.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. |
Packaging and Prices
| Packaging | Price (€) | Quantité | Buy Now |
|---|---|---|---|
| 1 Unité(s) | 120.00 | ||
| 5 Unité(s) | 480.00 | ||
| For quotation of big quantities, please Contact us | |||
Product Technical Documents
 | Safety Data Sheet Available on request, please Contact us Ref. SDS_L8406-500UG : unit price : free of charge |
Chemical and Physical Properties
| Product code | L8406-500UG | Molecular weight | 2452 Da |
| Product name | TERTIAPIN Q | Physical form | White lyophilized solid |
| CAS No. | 252198-49-5 | Melting point | |
| RTECS | NA | Solubility | water and saline buffer |
| UNIPROT | P56587 | Optical Activity | |
| PubChem SID | |||
| PubChem CID | 90479782 | ||
| Purity | > 98 % | ||
| Toxicity(LD50) | No Data | ||
| Chemical Name | |||
| Storage & Reconstitution Recommandations |
Stable at room temperature, store preferably at 4°C |
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| Savety Recommandations | |||
Bibliographic References
| Product code | L8406-500UG |
| Product name | TERTIAPIN Q |
- 1. Felix, J. P.,et al. (2006) Characterization of Kir1.1 channels with the use of a radiolabeled derivative of tertiapin,Biochemistry. ;
2. Jin, W., et al. (1999) Mechanisms of inward-rectifier K+ channel inhibition by tertiapin-Q, Biochemistry.  ;
3. Jin, W., and Lu, Z. (1999) Synthesis of a stable form of tertiapin: a high-affinity inhibitor for inward-rectifier K+ channels, Biochemistry. ;
4. Kanjhan, R., C et al. (2005) Tertiapin-Q blocks recombinant and native large conductance K+ channels in a use-dependent manner, J Pharmacol Exp Ther. ;
5. Kitamura, H., et al. (2000) Tertiapin potently and selectively blocks muscarinic K(+) channels in rabbit cardiac myocytes, J Pharmacol Exp Ther. ;
6. Ramu, Y., et al. (2001) Titration of tertiapin-Q inhibition of ROMK1 channels by extracellular protons, Biochemistry.
Links
| Product code | L8406-500UG |
| Product name | TERTIAPIN Q |
| External Links |
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