ML SA1 is a activator of TRPML channels (TRPML1, 2 and 3); does not activate TRPM2, TRPV2, TRPV3, TRPC6 or TRPA1 channels. Induces TRPML-mediated Ca2+ release from lysosomes; activity corrects trafficking defects and reduces cholesterol accumulation in Niemann-Pick type C macrophages.
|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 5.25 mg/mL|
Degradation of TRPML1 in Neurons Reduces Neuron Survival in Transient Global Cerebral Ischemia
Yang Wang, et al. Oxid Med Cell Longev. 2018 Dec 18;2018:4612727. PMID: 30662583.
Antagonist functional selectivity: 5-HT2A serotonin receptor antagonists differentially regulate 5-HT2A receptor protein level in vivo.
Yadav, et al. J Pharmacol Exp Ther. 2011;339: 99. PMID: 21737536.
|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.
MK6-83 is an agonist of the transient receptor potential channel ML3 (TRPML3).
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.
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