α-Conotoxin MII TFA, a natural product isolated from the sea snail Conus magus, can effectively inhibit the α3β2 subunit of the nAChR receptor, with an IC50 value of 0.5 nM. In addition, α-Conotoxin MII TFA can effectively inhibit the activity of β3-containing neuro-nicotinic receptor.
Molecular Weight | 1710.94 (free base) |
Formula | C67H103N23O22S4.xC2HF3O2 |
CAS Number | 175735-93-0 (free base) |
Form | Solid |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
Related AChR/AChE Products |
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Tacrine
Tacrine is a potent acetylcholinesterse (AChE) inhibitor (IC50=109 nM), also acting as a CYP1A2 substrate agent. |
THRX-160209
THRX-160209 is a potent antagonist at the M(2) muscarinic acetylcholine (ACh) receptor subtype that was designed using a multivalent strategy, simultaneously targeting the orthosteric site and a nearby site known to bind allosteric ligands. |
Catestatin
Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. |
α-Conotoxin MII
α-Conotoxin MII (α-CTxMII), a 16-amino acid peptide from the venom of the marine snail Conus magus, potently blocks nicotinic acetylcholine receptors (nAChRs) composed of α3β2 subunits, with an IC50 of 0.5 nM. |
COG 133 TFA
COG 133 TFA is a fragment of Apolipoprotein E (APOE) peptide. |
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