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HsTX1[R14A]

SKU : BHP21300222

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Mfr.No.	STH-310, STH-310_0.1 mg, STH-310_0.5 mg, STH-310_1 mg, STH-310_50 mcg
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	C146H239N51O46S9
Background	HsTX1(R14A) is an analogue of HsTX1, a 34-residue peptide toxin originally derived from the venom of the scorpion Heterometrus spinifer1,2. In this analogue, arginine at position 14 is substituted with alanine, resulting in a potent and selective blocker of voltage-gated potassium channels (KV1.3), with an IC50 of 45 ± 3 pM. HsTX1(R14A) exhibits more than 2,000-fold selectivity for KV1.3 over KV1.11. The HsTX1(R14A) toxin has been shown to be highly resistant to proteolysis and stable in plasma1. This resistance, stabilized by four disulfide bridges, is superior to that of ShK analogues, including the clinical candidate ShK-186, which contains only three disulfide bridges3. Pharmacokinetic studies indicate that both intravenous and subcutaneous applications are viable for the delivery of this potent peptide4. Additionally, HsTX1(R14A) has shown efficacy in a model of rheumatoid arthritis, suggesting its potential as a therapeutic agent for effector memory T cells (TEM) cell-mediated autoimmune diseases5. Its high stability and bioavailability make HsTX1(R14A) toxin an excellent candidate for further development as a therapeutic lead and as a probe for therapeutic applications6. KV1.3 upregulation is implicated in various autoimmune and neuroinflammatory diseases, including rheumatoid arthritis, psoriasis, multiple sclerosis, and type I diabetes. While the therapeutic potential of KV1.3 blockade has been well-characterized in autoimmune diseases driven by effector memory T cells, emerging evidence suggests that KV1.3 also plays a role in diseases involving T helper cells, macrophages, microglia, and class-switched B cells3. This expanded understanding of KV1.3's role in various cell types and diseases further highlights the potential therapeutic value of HsTX1(R14A) and similar KV1.3 blockers.
Biological Activity	HsTX1(R14A) is a potent and selective blocker of Kv1.3 voltage-gated K+ channels1.
Formulation	Lyophilized from double distilled water (ddH2O). May contain TFA as a residual counter ion.
Molecular Weight	3733.4 Da
Source	Synthetic peptide
Accession Number	P59867
Concentration	0.05 0.5 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: Cys3-Cys24, Cys9-Cys29, Cys13-Cys31 and Cys19-Cys34 Cys34 = C-terminal amidation
Origin	Heterometrus spinifer (Asia giant forest scorpion) (Malaysian black scorpion)

Synonyms	Potassium channel toxin alpha-KTx 6.3 analogue
Gene Id	KCNA3
Sequence	ASCRTPKDCADPCAKETGCPYGKCMNRKCKCNRC -NH2
Target	KV1.3

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	Rashid, M.H. et al. (2014) Sci. Rep., 4, 4509. Lebrun, B. et al. (1997) Biochem. J. 328, 321. Tajti, G. et al. (2020), Biochem. Pharmacol., 181, 114146. Bergmann, R. et al. (2017) Sci. Rep., 7, 3756. Tanner M.R. et al. (2017) Clin. Immunol., 180, 45. Wai D.C.C. et al. (2022) Bioconj. Chem., 33, 2197. Rashid M.H. et al. (2014) Sci Rep., 4, 4509.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHP21300222-1	STH-310_0.1 mg	0.1 mg	$475		Add to Cart
BHP21300222-2	STH-310_0.5 mg	0.5 mg	$973		Add to Cart
BHP21300222-3	STH-310_1 mg	1 mg	$1475		Add to Cart
BHP21300222-4	STH-310_50 mcg	50 mcg	$375		Add to Cart

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