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Home / Proteins & Peptide / Proteins

u/omega-TRTX-Tap1a

SKU : BHP21300304

A Blocker of Voltage-Gated Na+ and T-Type Ca2+ Channels

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Mfr.No.	STT-600, STT-600_0.1 mg, STT-600_0.5 mg, STT-600_1 mg, STT-600_10 mg, STT-600_5 mg, STT-600_50 mcg
Description	A Blocker of Voltage-Gated Na+ and T-Type Ca2+ Channels
Reconstitution	Centrifuge the vial (10,000 x g for 5 minutes) before adding solvent to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Gently tap, tilt, and roll the vial to aid dissolution. Avoid vigorous vortexing; light vortexing for up to 3 seconds is acceptable if needed. The product is soluble in pure water at high micromolar concentrations (100 uM - 1 mM). For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in double-distilled water (ddH2O) at a concentration between 100-1000x of the final working concentration. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. Centrifuge all product preparations before use. It is recommended to prepare fresh solutions in working buffers just before use. Avoid multiple freeze-thaw cycles to maintain biological activity.
Molecular Formula	C174H258N52O55S7
Background	u/omega-TRTX-Tap1a (Tap1a) is a 35 amino acid peptidyl toxin originally isolated from the venom of the tarantula, Theraphosa apophysis. Tap1a inhibits voltage-gated sodium (NaV) and voltage-gated calcium (CaV)3 channels by inducing a hyperpolarizing shift in both voltage-dependent activation and steady state inactivation1. Tap1a specifically inhibits NaV1.7, NaV1.2, and CaV3.1 with nanomolar potency and NaV1.3, NaV1.6, NaV1.1, and CaV3.2 at low micromolar concentrations1. These ion channels participate in neuron polarization, transmission of somatosensory signals, as well as neuronal cell differentiation, death, and survival. Thus, they are involved in many diseases, including pain disorders, epilepsy, and age-related neurodegeneration.Spider peptides modulate an array of ion channels and receptor proteins. Knottins, which are a subtype of spider peptides, are also referred to as inhibitor cystine knot (ICK) peptides. ICK peptides harbor a disulfide-rich structural motif that forms a "knot", which confers high structural, thermal, and proteolytic stability. The modelled structure of Tap1a revealed an ICK fold typical of spider venom peptides, as well as a hydrophobic patch involved in the binding of spider venom peptides to CaV3 and NaV channels1.CaV3 are T-type, low voltage-gated calcium channels. Their electrophysiological properties include low voltage thresholds for activation and inactivation, rapid inactivation, and rebound bursting. These properties are responsible for the CaV3-mediated fine-tuned regulation of neuronal excitability in both the central nervous system (CNS) and peripheral nervous system (PNS)2.CaV3.1 is highly expressed in the brain amygdala, subthalamic nuclei, cerebellum, and thalamus. In contrast, CaV3.1 is only moderately expressed in the heart. CaV3.1 participates in neuron polarization, synaptic transmission, as well as neuronal cell differentiation, death, and survival. CaV3.1 was implicated in the process of age-related neurodegeneration, Parkinson's disease, and Alzheimer's disease3. Moreover, mutations in CaV3.1 have been shown to induce cerebellar ataxia. CaV3.2 channels are expressed in the thalamus where they play a role in the pathophysiology of epilepsy. In addition, the constitutive deletion of the CaV3.2 gene alleviates acute pain, inflammatory pain, and chronic visceral pain in mice4.NaV1.1-1.9 are voltage-gated sodium channels. They open upon depolarization of the membrane and inactivate rapidly before returning to the closed state upon membrane hyperpolarization. The rapid influx of Na+ ions is vital to the generation and propagation of action potential (AP) as well as the transmission of somatosensory signals.NaV1.7 is expressed in the PNS, dorsal root ganglia neurons, visceral sensory neurons, olfactory sensory neurons, trigeminal ganglia, and sympathetic neurons. NaV1.7 gain-of-function mutations have been identified in patients with various pain disorders, such as inherited erythromelalgia (IEM), paroxysmal extreme pain disorder (PEPD), small fiber neuropathy (SFN), and painful diabetic peripheral neuropathy5.NaV1.2 is abundantly expressed at the nodes of Ranvier and in the axon initial segment (AIS) during early development. NaV1.2 plays a dominant role in the initiation and propagation of APs. In mature neurons, NaV1.6 takes the role of AP initiation, and NaV1.2 merely augments APs. Pathogenic variants of NaV1.2 are common causes of neurodevelopmental disorders such as episodic ataxia, schizophrenia, autism spectrum disorder, and intellectual disability with and without seizures6.
Biological Activity	Nav1.1, Nav1.2, Nav1.3, Nav1.6, Nav1.7 and Cav3.1 blocker at nanomolar concentrations (IC50=81-301 nM). Surprisingly, selectively slows fast inactivation of Nav1.3. Also shows moderate inhibition of Cav3.2 (IC50=1233 nM)1.
Formulation	Lyophilized from double distilled water (ddH2O). May contain TFA as a residual counter ion.
Molecular Weight	4182.7 Da
Solubility	Centrifuge the vial before adding solvent (10,000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. The product is soluble in pure water at high micromolar concentrations (100 uM - 1 mM). For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in double-distilled water (ddH2O) at a concentration between 100-1000x of the final working concentration. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. Centrifuge all product preparations before use. It is recommended to prepare fresh solutions in working buffers just before use. Avoid multiple freeze-thaw cycles to maintain biological activity.
Source	Synthetic peptide
Accession Number	P0DQO3
Concentration	80 nM - 1 uM
Form	Lyophilized
Notes	Bioassay Tested: yes Steril endotoxin free: no Is Toxin: Yes
UNSPSC Code	12352202
Lead Time	1-2 Business Days
Modifications	Disulfide bonds location: Cys3-Cys18, Cys10-Cys23, Cys17-Cys30
Origin	Theraphosa apophysis (Goliath pinkfoot tarantula) (Pseudotheraphosa apophysis)

Synonyms	Mu/omega-TRTX-Tap1a, Mu/omega-theraphotoxin-Tap1a, Tap1a
Gene Id	CACNA1G, CACNA1H, SCN1A,SCN2A,SCN3A,SCN8A,SCN9A
Sequence	DDCLGMFSSCDPNNDKCCPNRKCSRKDQWCKYQLW-OH
Target	NaV channels and T-type Ca2+ channels

Country Of Origin	Israel/IL
Purity	>=98% (HPLC)
Storage	Storage After Reconstitution: The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles. Storage Before Reconstitution: The product is shipped as a lyophilized powder at room temperature. Upon receipt, store the product at -20°C. Protect from moisture. Storage of solutions: The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles.

Applications	Electrophysiology

Reference	Cardoso, F. C. et al. (2021) Pain 162, 569. Lory, P. et al. (2020) Pflugers Arch Eur. J. Physiol. 472, 831. Pan, C. et al. (2021) Curr. Med. Sci. 41, 680. Candelas, M. et al. (2019) Sci. Rep. 9, 3112. Dongol, Y. et al. (2019) Toxins 11, 626. Reynolds, C. et al. (2020) Eur. J. Paediatr. Neurol. 24, 117.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHP21300304-1	STT-600_0.1 mg	0.1 mg	$523		Add to Cart
BHP21300304-2	STT-600_0.5 mg	0.5 mg	$1078		Add to Cart
BHP21300304-3	STT-600_1 mg	1 mg	$1486		Add to Cart
BHP21300304-4	STT-600_10 mg	10 mg	$6551		Add to Cart
BHP21300304-5	STT-600_5 mg	5 mg	$4379		Add to Cart
BHP21300304-6	STT-600_50 mcg	50 mcg	$328		Add to Cart

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