Vocacapsaicin (CA-008), a prodrug of capsaicin, is the first (first-in-class) non-opioid TRPV1 agonist. Vocacapsaicin can provide lasting pain relief.
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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|
GDC-6599 is a first-in-class, orally effective TRPA1 inhibitor for studies related to chronic cough and asthma.
Acetaldehyde is a TRP anchor protein 1 (TRPA1) agonist that is converted to non-toxic acetic acid by acetaldehyde dehydrogenase (ALDH).
|Adenosine 5′-diphosphoribose sodium
Adenosine 5′-diphosphoribose sodium is a metabolite of nicotinamide adenine nucleotides (NAD+), as well as a potent intracellular Ca2+-permeable cation TRPM2 channel activator, and enhances autophagy.
JNJ-28583113 is a brain-permeable TRPM2 antagonist and blocks phosphorylation of GSK3α and β subunits by inhibiting TRPM2. In addition, JNJ-28583113 inhibits cytokine release from microglia in response to pro-inflammatory stimuli. It has the function of protecting cells from oxidative stress-induced cell death.
L-R4W2 TFA is a potent antagonist of vanilloid receptor 1 (VR1, TRPV1), with an IC50 of 0.1 μM. L-R4W2 TFA may act as a potent analgesic.
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