In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
3-chloro-5-hydroxy BA is a GPR81 agonist.
GPR81 (HCA1) is a member of G-protein-coupled receptors (GPCRs). GPR81 is predominantly expressed on adipocytes and is activated by the endogenous ligands 2-hydroxypropanoate (lactate). Stimulation of GPR81 in adipose tissue lead to a decrease in the lipolysis of triglycerides by hormone-sensitive lipase, which resulted in reduced transport of fatty acids to the liver and a decrease in hepatic triglycerides .
In vitro: In the hGPR81 assay, 3-chloro-5-hydroxybenzoic acid showed the potency against GPR81 with an EC50 of 16 μM. The EC50 of 3-chloro-5-hydroxybenzoic acid against monkey GPR81, dog GPR81, rat GPR81, mouse GPR81, and hamster GPR81 was 17 μM, 67 μM, 7 μM, 22 μM and 27 μM, respectively . 3-chloro-5-hydroxy BA blocked basal ghrelin secretion by primary gastric mucosal cells .
In vivo: In mice, oral administration of 3-chloro-5-hydroxybenzoic acid at 30 mg/kg provided a Cmax of 67 μM at approximately 3-fold over the in vitro EC50 with an AUCinf of 54 h μM and a short t1/2 of 1.5 h, and the 100 mg/kg p.o dose attained a Cmax of 342 μM at greater than 15-fold over the observed in vitro EC50 .
. Dvorak C A, Liu C, Shelton J, et al. Identification of hydroxybenzoic acids as selective lactate receptor (GPR81) agonists with antilipolytic effects[J]. ACS medicinal chemistry letters, 2012, 3(8): 637-639.
. Engelstoft M S, Park W, Sakata I, et al. Seven transmembrane G protein-coupled receptor repertoire of gastric ghrelin cells[J]. Molecular metabolism, 2013, 2(4): 376-392.
|Storage||Store at -20°C|
|Synonyms||3-chloro-5-hydroxy BA,CHBA,GPR81 Agonist|
|Solubility||≥6.65mg/mL in DMSO|
|Chemical Name||3-chloro-5-hydroxy-benzoic acid|
|Shipping Condition||Evaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.|
|General tips||For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.|