OD1

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OD1, a potent Nav1.7 channel activator

OD1 is a scorpion peptide that has been isolated initially from the venom of the scorpion Odonthobuthus doriae. OD1 potently inhibits fast inactivation of mammalian channels Nav1.7 (EC50 4.5 nM), Nav1.4 (EC50 10 ± 2 nM) and Nav1.6 (EC50 47 ± 10 nM). OD1 also blocks fast inactivation of the para/tipE insect channel (EC50 80 nM). OD1 weakly affects mammalian Nav1.3 and Nav1.5 (EC50 > 1 μM) and does not affect Nav1.2 and Nav1.8. OD1 induces spontaneous pain when injected in animal in association with our without Veratridine and can be used to test the analgesic effects of Nav1.7 blockers in-vivo.

OD1 bioassay results figure

A, C, Time course of the modulating effect of OD1 #ODX001 (50 nM) on hNav1.7 current.  The current was elicited by a 50 ms-depolarizing pulse to -25 mV (estimated V1/2) or to -10 mV from a holding potential of -90 mV. Inter-sweep period was 10 s. Current amplitudes were plotted against time. Black bar indicates toxin application. B, D, Representative recording traces of Nav1.7 current in control condition (black) and after the effect of OD1 #ODX001 had stabilized (red). The inactivation kinetics of current was fitted with the standard mono-exponential function. E, Families of hNav1.7 current traces in control and in the presence of 50 nM OD1 #ODX001. Currents were evoked by depolarizing pulses from -60 mV to 40 mV, while the cell was hold at -90 mV. F, Amplitude-voltage relationships obtained from E.

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Description

AA sequence:   GVRDAYIADDKNCVYTCASNGYCNTECTKNGAESGYCQWIGRYGNACWCIKLPDEVPIRIPGKCR-NH2
Disulfide bonds:   C13-C64 ; C17-C37 ; C23-C47 ; C27-C49
Length (aa): 65
Formula:  C308H466N90O95S8
Appearance: White lyophilized solid
CAS number: Not available
Molecular Weight: 7206.20 Da
Source: Synthetic
Counterion: TFA salts
Solubility: Water or saline buffer, 5 mg/mL maximum (recommendation)
Purity: >95%

OD1, the first toxin isolated from the venom of the scorpion
Odonthobuthus doriae

Potent Modulation of the Voltage-Gated Sodium Channel Nav1.7 by OD1

Chemical Engineering and Structural and Pharmacological Characterization of the α‑Scorpion Toxin OD1

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    OD1

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