Gentisuric acid
Based on 1 Customer Validation
Gentisuric Acid is a metabolite of Aspirin (HY-14654). Gentisuric Acid activates GPR35. Gentisuric Acid inhibits HIF-1α and HIF-2α. Gentisuric Acid inhibits Mitomycin C (HY-13316)-induced genotoxicity and twin spots (mitotic recombination), reduces spot frequency without reducing survival, and modulates replication or repair of Mitomycin C-damaged DNA. Gentisuric Acid can be used in research on VHL-deficient renal cell carcinoma and Drosophila melanogaster infection.
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- Purity : 99.65%
- CAS No.: 25351-24-0
- 화학식: C9H9NO5
- 분자량:211.17
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보관:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Biological Activity
제품 설명
IC50 & Target
[3]|
HIF-1α |
HIF-2α |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HT-29 | EC50 |
182 μM
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DMR agonism in HT-29 human colorectal adenocarcinoma cells endogenously expressing GPR35 assessed by dynamic mass redistribution measured within 15 min poststimulation.
DMR agonism in HT-29 human colorectal adenocarcinoma cells endogenously expressing GPR35 assessed by dynamic mass redistribution measured within 15 min poststimulation.
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22526472 |
In Vitro
Gentisuric acid inhibits HIF-1α levels in RCC4 VHL-deficient renal cancer cells[3].
Gentisuric acid (approximately 1 h) activates GPR35 in HT-29 cells, with a DMR EC50 of 182 μM and an efficacy of 120 pm, and this DMR is dose-dependently blocked by SPB05142, with an IC50 of 6.46 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Gentisuric acid (5-40 mg/bottle; dietary administration via larval medium; after MMC exposure; until hatching) reduces MMC-induced wing spots in Drosophila SMART, with the strongest inhibition of 48.6% at 5 mg/bottle[4].
Gentisuric acid (5-320 mg/bottle; dietary administration via larval medium; 6 h; before MMC exposure) does not show a consistent dose-dependent reduction of MMC-induced wing spots in Drosophila SMART[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:mwh jv; spapol × flr3/TM3, Ser (60-h-old larvae; virgin female and male cross)[2]
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Dosage:5 mg/bottle, 10 mg/bottle, 20 mg/bottle, and 40 mg/bottle
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Administration:larval ingestion (dietary); continuous exposure until larval hatching
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Result:In marker-heterozygous wings, gentisuric acid + MMC at 5 mg/bottle yielded N=58, survival 81.3%, small single spots 1.09 (63), large single spots 0.90 (52), twin spots 0.21 (12), total spots 2.19 (127), spots with mwh clone 124, and recombination ratio 83.2%.
In marker-heterozygous wings, gentisuric acid + MMC at 10 mg/bottle yielded N=56, survival 92.5%, small single spots 0.80 (45), large single spots 0.57 (32), twin spots 0.27 (15), total spots 1.64 (92), spots with mwh clone 87, and recombination ratio 76.8%.
In marker-heterozygous wings, gentisuric acid + MMC at 20 mg/bottle yielded N=88, survival 100.0%, small single spots 0.73 (64), large single spots 0.41 (36), twin spots 0.08 (7), total spots 1.22 (107), spots with mwh clone 104, and recombination ratio 70.3%.
In marker-heterozygous wings, gentisuric acid + MMC at 40 mg/bottle yielded N=82, survival 98.8%, small single spots 0.29 (24), large single spots 0.16 (13), twin spots 0.07 (6), total spots 0.52 (43), spots with mwh clone 43, and recombination ratio 65.4%.
In balancer-heterozygous wings, gentisuric acid + MMC at 5 mg/bottle yielded N=72, small single spots 0.33 (24), large single spots 0.03 (2), total spots 0.36 (26), and spots with mwh clone 26.
In balancer-heterozygous wings, gentisuric acid + MMC at 10 mg/bottle yielded N=92, small single spots 0.33 (30), large single spots 0.03 (3), total spots 0.36 (33), and spots with mwh clone 33.
In balancer-heterozygous wings, gentisuric acid + MMC at 20 mg/bottle yielded N=72, small single spots 0.32 (23), large single spots 0.03 (2), total spots 0.35 (25), and spots with mwh clone 25.
In balancer-heterozygous wings, gentisuric acid + MMC at 40 mg/bottle yielded N=76, small single spots 0.15 (11), large single spots 0.04 (3), total spots 0.18 (14), and spots with mwh clone 14.
Inhibition percentages for gentisuric acid + MMC at 5 mg/bottle were −3.8% for small single spots, 10.0% for large single spots, 16.0% for twin spots, and 4.8% for total spots.
Inhibition percentages for gentisuric acid + MMC at 10 mg/bottle were 23.8% for small single spots, 43.0% for large single spots, −8.0% for twin spots, and 28.7% for total spots.
Inhibition percentages for gentisuric acid + MMC at 20 mg/bottle were 30.5% for small single spots, 59.0% for large single spots, 68.0% for twin spots, and 47.0% for total spots.
Inhibition percentages for gentisuric acid + MMC at 40 mg/bottle were 72.4% for small single spots, 84.0% for large single spots, 72.0% for twin spots, and 77.4% for total spots.
Small single spots and twin spots were reduced at 20 and 40 mg/bottle, and large single spots were reduced at 10, 20, and 40 mg/bottle.
In balancer-heterozygous wings, a slight reduction in MMC-induced small single spots and large single spots was observed.
At 40 mg/bottle, total genotoxicity frequency was reduced by more than 70% (77.4% for total spots).
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Animal Model:mwh jv; spa^pol × flr^3/TM3, Ser (virgin females crossed with males; larvae cultured at 24°C for 60 h before exposure)[4]
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Dosage:5 mg/bottle, 10 mg/bottle, 20 mg/bottle, 40 mg/bottle
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Administration:dietary administration via larval medium; after MMC exposure; until hatching
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Result:At 5 mg/bottle, survival was 72.5%, total spots were 1.27 spots/wing, and inhibition was 48.6%.
At 10 mg/bottle, survival was 75.0%, total spots were 1.52 spots/wing, and inhibition was 38.5%.
At 20 mg/bottle, survival was 77.5%, total spots were 1.44 spots/wing, and inhibition was 41.7%.
At 40 mg/bottle, survival was 73.8%, total spots were 1.93 spots/wing, and inhibition was 34.0%.
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Animal Model:mwh jv; spa^pol × flr^3/TM3, Ser (virgin females crossed with males; larvae cultured at 24°C for 54 h before exposure)[4]
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Dosage:5 mg/bottle, 20 mg/bottle, 80 mg/bottle, 320 mg/bottle
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Administration:dietary administration via larval medium; 6 h; before MMC exposure; until hatching
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Result:GUA alone pre-exposure:
At 5 mg/bottle, survival was 90.0% and total spots were 0.21 spots/wing.
At 20 mg/bottle, survival was 73.6% and total spots were 0.33 spots/wing.
At 80 mg/bottle, survival was 92.7% and total spots were 0.26 spots/wing.
At 320 mg/bottle, survival was 94.5% and total spots were 0.32 spots/wing.
GUA + MMC pre-exposure:
At 5 mg/bottle, survival was 78.8%, total spots were 1.14 spots/wing, and inhibition was 25.0%.
At 20 mg/bottle, survival was 75.3%, total spots were 0.92 spots/wing, and inhibition was 39.5%.
At 80 mg/bottle, survival was 80.0%, total spots were 1.42 spots/wing, and inhibition was 6.6%.
At 320 mg/bottle, survival was 70.7%, total spots were 1.58 spots/wing, and inhibition was -3.9%.
Chemical Information
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CAS No. 25351-24-0
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Appearance Solid
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분자량 211.17
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화학식 C9H9NO5
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Color White to off-white
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SMILES
OC1=CC(C(NCC(O)=O)=O)=C(O)C=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
용액&용해도
In Vitro:
DMSO : 83.33 mg/mL (394.61 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (288 KB)
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SDS (614 KB)
- English - EN (614 KB)
- Français - FR (614 KB)
- Deutsch - DE (614 KB)
- Norwegian - NO (614 KB)
- Español - ES (614 KB)
- Swedish - SV (614 KB)
- Italian - IT (614 KB)
- Korean - KR (614 KB)
- Portuguese - PT (614 KB)
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Handling Instructions (2659 KB)
References
[1]. Deng H, et al. Aspirin metabolites are GPR35 agonists. Naunyn-Schmiedeberg's archives of pharmacology. 2012 Jul;385(7):729-37. [Content Brief]
[2]. Niikawa M, et al. Effect of cotreatment of aspirin metabolites on mitomycin C-induced genotoxicity using the somatic mutation and recombination test in Drosophila melanogaster. Drug and chemical toxicology. 2006 Jan 1;29(4):379-96. [Content Brief]
[4]. Niikawa M, et al. Suppressive effect of post- or pre-treatment of aspirin metabolite on mitomycin C-induced genotoxicity using the somatic mutation and recombination test in Drosophila melanogaster. Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie. 2007;61(2-3):113-9. [Content Brief]
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 (protect from light). 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 |
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| DMSO | 1 mM | 4.7355 mL | 23.6776 mL | 47.3552 mL | 118.3880 mL |
| 5 mM | 0.9471 mL | 4.7355 mL | 9.4710 mL | 23.6776 mL | |
| 10 mM | 0.4736 mL | 2.3678 mL | 4.7355 mL | 11.8388 mL | |
| 15 mM | 0.3157 mL | 1.5785 mL | 3.1570 mL | 7.8925 mL | |
| 20 mM | 0.2368 mL | 1.1839 mL | 2.3678 mL | 5.9194 mL | |
| 25 mM | 0.1894 mL | 0.9471 mL | 1.8942 mL | 4.7355 mL | |
| 30 mM | 0.1579 mL | 0.7893 mL | 1.5785 mL | 3.9463 mL | |
| 40 mM | 0.1184 mL | 0.5919 mL | 1.1839 mL | 2.9597 mL | |
| 50 mM | 0.0947 mL | 0.4736 mL | 0.9471 mL | 2.3678 mL | |
| 60 mM | 0.0789 mL | 0.3946 mL | 0.7893 mL | 1.9731 mL | |
| 80 mM | 0.0592 mL | 0.2960 mL | 0.5919 mL | 1.4799 mL | |
| 100 mM | 0.0474 mL | 0.2368 mL | 0.4736 mL | 1.1839 mL |
Gentisuric acid Related Classifications
HY-W338852 Related Classifications
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