SAR7334 is a TRPC6 inhibitor, and used for treat the fibrotic disorders, such as focal segmental glomerulosclerosis, skeletal muscle dysfunction. SAR7334 inhibited TRPC6, TRPC3 and TRPC7-mediated Ca(2+) influx into cells with IC50 s of 9.5, 282 and 226 nM, whereas TRPC4 and TRPC5-mediated Ca(2+) entry was not affected.
|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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO: ≥ 100 mg/mL|
Pharmacological Characterization of the Native Store-Operated Calcium Channels of Cortical Neurons from Embryonic Mouse Brain.
Chauvet S, et al. Front Pharmacol. 2016 Dec 12;7:486. PMID: 28018223.
Discovery and pharmacological characterization of a novel potent inhibitor of diacylglycerol-sensitive TRPC cation channels.
Maier T, et al. Br J Pharmacol. 2015 Jul;172(14):3650-60. PMID: 25847402.
S107 is a Type 1 ryanodine receptor (RyR1) stabilizer.
3,3’,5,5’-Tetramethylbenzidine(TMB) is a chromogenic substrate used in staining procedures in immunohistochemistry as well as being a visualising reagent used in enzyme-linked immunosorbent assays (ELISA).
Coelenterazine is the luciferin, the light-emitting molecule, used for monitoring reporter genes in BRET, ELISA and HTS techniques.
Fluorescein is a synthetic organic compound and dye.
SBI-0640756 is a first-in-class inhibitor that targets eIF4G1 and disrupts the eIF4F complex.
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