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Home / Proteins & Peptide / Proteins

u-TRTX-Tsp1a

SKU : BHP21300303

Selective and potent inhibitor of Nav1.7 channels

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Mfr.No.	STT-500, STT-500_0.1 mg, STT-500_0.25 mg, STT-500_0.5 mg, STT-500_1 mg, STT-500_5 mg, STT-500_50 mcg
Description	Selective and potent inhibitor of Nav1.7 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	C148H221N41O39S6
Background	u-theraphotoxin-Tsp1a (Tsp1a) is a 28 amino acid peptidyl toxin originally isolated from the venom of the Thrixopelma spec. (Peru) spider venoM Tsp1a is a potent (IC50 = 10 nM) and highly specific inhibitor of NaV1.7 channels, with a selectivity of >100-fold over hNaV1.3?hNaV1.6 and hNaV1.8, 45-fold over hNaV1.1, and 24-fold over hNaV1.21.Tsp1a is a gating modifier toxin that inhibits hNaV1.7 by stabilizing the channel in its inactivated state, inducing a hyperpolarizing shift in the voltage-dependence of channel inactivation and slowing recovery from fast inactivation1.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. NMR studies revealed that Tsp1a adopts a classical knottin fold, and like many knottin peptides, it is exceptionally stable in human serum1.NaV1.7 is expressed in the PNS, dorsal root ganglia neurons, visceral sensory neurons, olfactory sensory neurons, trigeminal ganglia, and sympathetic neurons. Gain-of-function mutations in SCN9A, the gene encoding NaV1.7, 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 neuropathy. Nav 1.7 loss-of-function mutations lead to a congenital indifference to pain2,3. Tsp1a toxin was shown to reduce visceral hypersensitivity in a model of irritable bowel syndrome. This suggests that pharmacological inhibition of hNaV1.7 at peripheral sensory nerve endings might be a viable approach for eliciting analgesia in patients suffering from chronic visceral pain1.
Biological Activity	Tsp1a toxin is a highly specific and potent inhibitor of NaV1.7 channels, with a selectivity of >100-fold over hNaV1.3?hNaV1.6 and hNaV1.8, 45-fold over hNaV1.1, and 24-fold over hNaV1.21.
Formulation	Lyophilized from double distilled water (ddH2O). May contain TFA as a residual counter ion.
Molecular Weight	3391 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
Concentration	10 - 200 nM
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 between: Cys2-Cys16, Cys9-Cys21, Cys15-Cys28 Asn28 - C-terminal amidation
Origin	Thrixopelma spec. (Peru) spider

Synonyms	u-theraphotoxin-Tsp1a, Tsp1a, u-TRTX-Tsp1a, Mu-TRTX-Tsp1a
Gene Id	SCN9A
Sequence	YCQKFLWTCDSERPCCEGLVCRLWCKIN-NH2
Target	Nav 1.7

Country Of Origin	Israel/IL
Purity	>=97% (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	Jiang, Y. et al. (2021) ACS Pharmacol. Transl. Sci., 4, 1362. Dongol, Y. et al. (2019) Toxins 11, 626. Dib-Hajj, S.D. et al. (2007) Trends Neurosci., 30, 555.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHP21300303-1	STT-500_0.1 mg	0.1 mg	$295		Add to Cart
BHP21300303-2	STT-500_0.25 mg	0.25 mg	$593		Add to Cart
BHP21300303-3	STT-500_0.5 mg	0.5 mg	$1003		Add to Cart
BHP21300303-4	STT-500_1 mg	1 mg	$1625		Add to Cart
BHP21300303-5	STT-500_5 mg	5 mg	$5686		Add to Cart
BHP21300303-6	STT-500_50 mcg	50 mcg	$218		Add to Cart

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