MK6-83 is an agonist of the transient receptor potential channel ML3 (TRPML3). MK6-83 appears to be significantly more efficacious on fibroblast lysosomes isolated from R403C or V446L expressing cells than on those isolated from TRPML1-/- cells.
|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.
|Solubility||DMSO 4 mg/mL|
A small molecule restores function to TRPML1 mutant isoforms responsible for mucolipidosis type IV
Cheng-Chang Chen, et al. Nat Commun. 2014 Aug 14;5:4681. PMID: 25119295.
|Related TRP Channel Products|
MDR-652 is a potent and specific transient receptor potential vanilloid 1 (TRPV1) agonist with Ki of 11.4 nM and 23.8 nM for hTRPV1 and rTRPV1, respectively.
AC1903 is a specific inhibitor of TRPC5 channel.
Nonivamide (also called pelargonic acid vanillylamide or PAVA) can activate the TRPV1 receptor, thus, stimulate the firing rate of dopaminergic neurons in the ventral tegmental area of the brain and to increase the expression of the serotonin receptor gene HTR2A.
HC-067047 is a potent, selective inhibitor of hTRPV4.
Capsazepine is a specific vanilloid receptor antagonist; synthetic analog of capsaicin.
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