ARI-3099
Based on 1 Customer Validation
ARI-3099 is an oral fibroblast activation protein (FAP) inhibitor. ARI-3099 specifically inhibits the proteolytic activity of FAP and blocks the cleavage of human FGF-21 between residues P171 and S172. ARI-3099 extends the half-life of circulating human FGF-21 in mice. ARI-3099 can be used in the research of type 2 diabetes and metabolic disorders.
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- Purity: 99.95%
- CAS No.: 1432499-49-4
- 화학식: C13H18BN3O4
- 분자량:291.11
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Covalent Screening Library
HY-L036
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Anti-diabetic Compound Library
HY-L040
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Orally Active Compound Library
HY-L061
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Highly Selective Inhibitors Library
HY-L158
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Covalent Screening Library Plus
HY-L036P
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
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Immunology/Inflammation Compound Library
HY-L007
Biological Activity
ki: 9 nM (FAP)
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.025 μM
Compound: 6, ARI-3099
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Inhibition of recombinant mouse FAP purified from HEK293 cell supernatant using Ala-Pro-p-nitroanilide as substrate by spectrophotometry
Inhibition of recombinant mouse FAP purified from HEK293 cell supernatant using Ala-Pro-p-nitroanilide as substrate by spectrophotometry
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[PMID: 24617858] |
ARI-3099 (16 μM; 30 minutes) completely inhibits recombinant human FAP-mediated cleavage of recombinant human FGF-21 in an in vitro biochemical assay[1].
ARI-3099 (16 μM; 24 h at 37°C) completely inhibits FAP-mediated cleavage of human FGF-21 in pooled mouse, cynomolgus monkey, and human plasma[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
ARI-3099 (80 mg/kg; p.o.; single dose) potently suppresses plasma FAP activity in healthy C57BL/6J mice, with near-complete inhibition for at least 2 hours[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J[1]
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Dosage:80 mg/kg
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Administration:s.c.; single dose
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Result:Increased the amount of intact human FGF-21 detected in mouse plasma. Extended the estimated half-life of intact human FGF-21 from 48 minutes to 79 minutes.
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Animal Model:C57BL/6J[1]
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Dosage:80 mg/kg
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Administration:p.o.; single dose
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Result:Reduced plasma FAP activity to near 0% of initial levels at 1 and 2 hours post-administration.
Chemical Information
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CAS No. 1432499-49-4
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Appearance Solid
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분자량 291.11
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화학식 C13H18BN3O4
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Color White to off-white
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SMILES
O=C(C1=CC=NC=C1)N[C@H](C)C(N2[C@@H](CCC2)B(O)O)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (343.51 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. 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. 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.59 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.59 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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 | 3.4351 mL | 17.1756 mL | 34.3513 mL | 85.8782 mL |
| 5 mM | 0.6870 mL | 3.4351 mL | 6.8703 mL | 17.1756 mL | |
| 10 mM | 0.3435 mL | 1.7176 mL | 3.4351 mL | 8.5878 mL | |
| 15 mM | 0.2290 mL | 1.1450 mL | 2.2901 mL | 5.7252 mL | |
| 20 mM | 0.1718 mL | 0.8588 mL | 1.7176 mL | 4.2939 mL | |
| 25 mM | 0.1374 mL | 0.6870 mL | 1.3741 mL | 3.4351 mL | |
| 30 mM | 0.1145 mL | 0.5725 mL | 1.1450 mL | 2.8626 mL | |
| 40 mM | 0.0859 mL | 0.4294 mL | 0.8588 mL | 2.1470 mL | |
| 50 mM | 0.0687 mL | 0.3435 mL | 0.6870 mL | 1.7176 mL | |
| 60 mM | 0.0573 mL | 0.2863 mL | 0.5725 mL | 1.4313 mL | |
| 80 mM | 0.0429 mL | 0.2147 mL | 0.4294 mL | 1.0735 mL | |
| 100 mM | 0.0344 mL | 0.1718 mL | 0.3435 mL | 0.8588 mL |
ARI-3099 Related Classifications
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