An agonist of GPR81
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3-chloro-5-hydroxy BA

Item No. 16795

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-chloro-5-hydroxy-benzoic acid
CAS Number
53984-36-4
Synonyms
  • 3-chloro-5-hydroxy Benzoic Acid
  • CHBA
  • GPR81 Agonist
Molecular Formula
C7H5ClO3
Formula Weight
172.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 50 mg/mlDMSO: 50 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 30 mg/ml
λmax
210, 305 nm
SMILES
ClC1=CC(O)=CC(C(O)=O)=C1
InChi Code
InChI=1S/C7H5ClO3/c8-5-1-4(7(10)11)2-6(9)3-5/h1-3,9H,(H,10,11)
InChi Key
RJOLIYHZZKAIET-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    25 mg

    $40

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    50 mg

    $68

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    100 mg

    $123

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    500 mg

    $525

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    Cayman Chemical
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    Product Description

    GPR81, also known as hydroxycarboxylic acid receptor 1 (HCAR1), is a recently de-orphanized receptor that is activated by lactic acid (EC50 ~ 1.5 mM) but not by other hydroxycarboxylic acids.1,2 3-chloro-5-hydroxy BA is an agonist of GPR81 (EC50 = 16 µM) that is inactive against the related GPR109a (HCAR2) receptor.3 It is similarly effective at GPR81 receptors from a variety of mammalian species and is bioavailable, stimulating lipolysis (increased serum free fatty acids) in mice fed high fat chow for 10 weeks.3 3-chloro-5-hydroxy BA, like lactate, blocks basal ghrelin secretion by primary gastric mucosal cells.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ahmed, K., Tunaru, S., and Offermanns, S. GPR109A, GPR109B and GPR81, a family of hydroxy-carboxylic acid receptors. Trends Pharmacol. Sci. 30(11), 557-562 (2009).

    2. Davenport, A.P., Alexander, S.P.H., Sharman, J.L., et al. International Union of Basic and Clinical Pharmacology. LXXXVIII. G protein-coupled receptor list: Recommendations for new pairings with cognate ligands. Pharmacol. Rev. 65(3), 967-986 (2013).

    3. Dvorak, C.A., Liu, C., Shelton, J., et al. Identification of hydroxybenzoic acids as selective lactate receptor (GPR81) agonists with antilipolytic effects. ACS Med. Chem. Lett. 3(8), 637-639 (2012).

    4. Engelstoft, M.S., Park, W.m., Sakata, I., et al. Seven transmembrane G protein-coupled receptor repertoire of gastric ghrelin cells. Mol. Metab. 2(4), 376-392 (2013).