AC 4 is a photoswitchable TRPV1 channel blocker (IC50 = 3.1 μM). Acts as an antagonist in trans conformation during voltage gated activation. Also acts as an antagonist in the cis formation during capsaicin-induced TRPV1 currents. Switches conformation from cis to trans at 440 nm and trans to cis at 360 nm. Allows photoswitchable antagonist and an agonist to be applied at the same time.
| Molecular Weight | 514.56 |
| Formula | C26H25F3N4O2S |
| CAS Number | 1459809-09-6 |
| Solubility (25°C) | DMSO 51.46 mg/mL |
| 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 TRP Channel Products |
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N-oleoyl-glutamine is a PM20D1-regulated N-acyl amino acids (NAAs). |
| N-Oleoyl valine
N-Oleoyl valine is a N-acyl valine compound that acts as a TRPV3 receptor antagonist. |
| TAT-M2NX
TAT-M2NX (tatM2NX) is a TRPM2 inhibitor with specific neuroprotective activity in male mice. |
| SOR-C13
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| GsMTx4 TFA
GsMTx4 TFA is a spider venom peptide that selectively inhibits cation permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. In addition, GsMTx4 TFA blocks cation-selective stretch-activated channels (SACs) and attenuates lysophosphatidylcholine (LPC)-induced astrocytotoxicity and microglial cell reactivity. |
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