1. GPCR/G Protein
  2. Hydroxycarboxylic Acid Receptor (HCAR)
  3. 3-Chloro-5-hydroxybenzoic acid

3-Chloro-5-hydroxybenzoic acid is a potent, orally active and selective lactate receptor GPR81 agonist, with an EC50 of 16 μM for human GPR81. 3-Chloro-5-hydroxybenzoic acid exhibits favorable in vivo effects on lipolysis in a mouse model of obesity.

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3-Chloro-5-hydroxybenzoic acid Chemical Structure

3-Chloro-5-hydroxybenzoic acid Chemical Structure

CAS No. : 53984-36-4

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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

3-Chloro-5-hydroxybenzoic acid is a potent, orally active and selective lactate receptor GPR81 agonist, with an EC50 of 16 μM for human GPR81. 3-Chloro-5-hydroxybenzoic acid exhibits favorable in vivo effects on lipolysis in a mouse model of obesity[1].

Cellular Effect
Cell Line Type Value Description References
COS-7 EC50
> 1000 μM
Compound: 2
Agonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay
Agonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay
[PMID: 24900524]
COS-7 EC50
16 μM
Compound: 2
Agonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay
Agonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay
[PMID: 24900524]
In Vitro

3-Chloro-5-hydroxybenzoic acid shows potency against human (EC50=16 μM), monkey (EC50=17 μM), dog (EC50=67 μM), rat (EC50=7 μM), mouse (EC50=22 μM), and hamster GPR81 (EC50=27 μM)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

3-Chloro-5-hydroxybenzoic acid (30, 100, and 300 mg/kg; PO in overnight fasted C57Bl6/J mice fed high fat chow for 10 weeks) shows significant reductions in free fatty acids at all doses tested, resulting in a minimum efficacious dose of 30 mg/kg[1].
Pharmacokinetic Parameters of 3-Chloro-5-hydroxybenzoic acid in Mice[1].

dose (mg/kg) tmax (h) AUCinf (h ng/mL) Cmax (ng/mL) Cmax (μM) t1/2 (h)
30 0.5 9356 11689.50 67.2 1.47
100 0.5 51312 55252.80 341.9 1.10

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57Bl6/J mice (DIO mice)[1]
Dosage: 30, 100, and 300 mg/kg
Administration: PO in overnight fasted C57Bl6/J mice fed high fat chow for 10 weeks
Result: Significant reductions in nonesterified free fatty acid cholesterol (NEFAc) at all doses tested.
Molecular Weight

172.57

Formula

C7H5ClO3

CAS No.
Appearance

Solid

Color

White to light brown

SMILES

ClC1=CC(O)=CC(C(O)=O)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (579.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.7947 mL 28.9737 mL 57.9475 mL
5 mM 1.1589 mL 5.7947 mL 11.5895 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.54%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 5.7947 mL 28.9737 mL 57.9475 mL 144.8687 mL
5 mM 1.1589 mL 5.7947 mL 11.5895 mL 28.9737 mL
10 mM 0.5795 mL 2.8974 mL 5.7947 mL 14.4869 mL
15 mM 0.3863 mL 1.9316 mL 3.8632 mL 9.6579 mL
20 mM 0.2897 mL 1.4487 mL 2.8974 mL 7.2434 mL
25 mM 0.2318 mL 1.1589 mL 2.3179 mL 5.7947 mL
30 mM 0.1932 mL 0.9658 mL 1.9316 mL 4.8290 mL
40 mM 0.1449 mL 0.7243 mL 1.4487 mL 3.6217 mL
50 mM 0.1159 mL 0.5795 mL 1.1589 mL 2.8974 mL
60 mM 0.0966 mL 0.4829 mL 0.9658 mL 2.4145 mL
80 mM 0.0724 mL 0.3622 mL 0.7243 mL 1.8109 mL
100 mM 0.0579 mL 0.2897 mL 0.5795 mL 1.4487 mL
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3-Chloro-5-hydroxybenzoic acid Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
3-Chloro-5-hydroxybenzoic acid
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