Hm1a
Product ID L8436-100UG 
Name Hm1a 
Molecular formula C170H239N47O54S6
Description
A 35 amino-acids peptide with 3 disulfide bridges , synthetic, initially isolated from the venom of the Togo starbust baboon spider Heteroscodra maculata.
Biological activity

Hm1a is a gating modifier toxin that principally inhibits inactivation of the mammalian voltage-gated sodium channel Nav1.1/SCN1A. When tested against human Nav1.1/SCN1A-Nav1.8/SCN10A alpha subunits heterologously expressed in Xenopus oocytes, the toxin inhibits inactivation of Nav1.1 (EC(50)=38 nM), with substantially weaker effects on Nav1.2/SCN2A (EC(50)=236 nM) and Nav1.3/SCN3A (EC(50)=220 nM). The toxin inhibits several subtypes of voltage-gated potassium channels with significantly lower potency than its effects on Nav1.1/SCN1A (PubMed:27281198). It is a moderately potent blocker of Kv2.1/KCNB1, Kv2.2/KCNB2, Kv4.1/KCND1, Kv4.2/KCND2 and Kv4.3/KCND3 and has little effect on Kv1.1/KCNA1, Kv1.2/KCNA2, Kv1.3/KCNA3, Kv1.4/KCNA4, Kv1.5/KCNA5, Kv1.6/KCNA6 and Kv3.4/KCNC4. IC50 is 280 nM on Kv4.1/KCND1, whereas percentage of current inhibition are 23% on Kv2.1/KCNB1 at 100 nM, 19.7% on Kv2.2/KCNB2 at 100 nM (and 51% at 300 nM), 39% on Kv4.2/KCND2 at 300 nM, and 43% on Kv4.3/KCND3 at 300 nM. It does not inhibit Nav1.4/SCN4A, Nav1.5/SCN5A, Nav1.6/SCN8A, Nav1.7/SCN9A, and Nav1.8/SCN10A at concentrations up to 1 µM.

 Packaging and Prices

Packaging Price (€) Quantité Buy Now
1 Unité(s) 160.00

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5 Unité(s) 640.00

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For quotation of big quantities, please Contact us
 Product Technical Documents
Safety Data Sheet Available on request, please Contact us
Ref. SDS_L8436-100UG : unit price : free of charge
 Chemical and Physical Properties
Product code L8436-100UG  Molecular weight 3997.46 Da
Product name Hm1a  Physical form White lyophilized solid
CAS No. NA Melting point
RTECS NA Solubility water and saline buffer
UNIPROT P60992 Optical Activity
PubChem SID    
PubChem CID NA    
Purity > 98 %    
Toxicity(LD50) No Data    
Chemical Name    
Storage & Reconstitution
Recommandations

Stable at room temperature, store preferably at 4°C


 
Savety Recommandations  
 Bibliographic References
Product code L8436-100UG 
Product name Hm1a 

- "1. Escoubas P, Diochot S, Célérier ML, Nakajima T, Lazdunski M (July 2002). ""Novel tarantula toxins for subtypes of voltage-dependent potassium channels in the Kv2 and Kv4 subfamilies"". Molecular Pharmacology. 62 (1): 48–57. ;
2. Osteen, Jeremiah D.; Herzig, Volker; Gilchrist, John; Emrick, Joshua J.; Zhang, Chuchu; Wang, Xidao; Castro, Joel; Garcia-Caraballo, Sonia; Grundy, Luke (June 2016). ""Selective spider toxins reveal a role for the Nav1.1 channel in mechanical pain"". Nature. 534 (7608): 494–499. ;
3. Osteen, Jeremiah D.; Sampson, Kevin; Iyer, Vivek; Julius, David; Bosmans, Frank (2017-06-12). ""Pharmacology of the Nav1.1 domain IV voltage sensor reveals coupling between inactivation gating processes"". Proceedings of the National Academy of Sciences : 201621263. ;
4. Shiau YS, Huang PT, Liou HH, Liaw YC, Shiau YY, Lou KL (October 2003). ""Structural basis of binding and inhibition of novel tarantula toxins in mammalian voltage-dependent potassium channels"". Chemical Research in Toxicology. 16 (10): 1217–25."
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