| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg | |||
| 500mg | |||
| 1g | |||
| Other Sizes |
| Targets |
URAT1 inhibitor 7 targets URAT1 (urate transporter 1), a transporter responsible for the reabsorption of uric acid in the kidney. By inhibiting URAT1, it reduces uric acid reabsorption, promoting uric acid excretion and lowering serum uric acid levels. URAT1 is a validated therapeutic target for hyperuricemia and gout. URAT1 inhibitor 7 is a potent inhibitor with an IC50 of 12 nM.
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| ln Vitro |
In vitro, URAT1 inhibitor 7 is a potent URAT1 inhibitor with an IC50 of 12 nM. It also inhibits CYP2C9 with an IC50 of 4.2 μM and displays microsomal stability (HLM <13 µL/min/mg). These in vitro properties make URAT1 inhibitor 7 a valuable tool for studying uric acid transport and for developing treatments for hyperuricemia and gout.
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| ln Vivo |
In vivo activity of URAT1 inhibitor 7 has not been extensively reported. As a potent URAT1 inhibitor, it may have potential for treating hyperuricemia and gout by lowering serum uric acid levels. However, detailed in vivo efficacy data are limited in publicly available sources.
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| Enzyme Assay |
The in vitro transporter assay for URAT1 inhibitor 7 involves measuring its inhibition of urate transport. Cells expressing human URAT1 are incubated with the compound at various concentrations in the presence of radiolabeled uric acid. Urate uptake is measured, and the IC50 for URAT1 inhibition is calculated. CYP2C9 inhibition is assessed using standard CYP inhibition assays with a CYP2C9-specific substrate. Microsomal stability is assessed by incubating the compound with human liver microsomes and measuring its disappearance over time.
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| Cell Assay |
The in vitro cell-based assay for URAT1 inhibitor 7 involves culturing cells expressing human URAT1 and treating them with the compound to assess effects on urate transport. Cells are seeded in multi-well plates and treated with URAT1 inhibitor 7 at various concentrations in the presence of radiolabeled or fluorescent uric acid. Urate uptake is measured, and the IC50 for inhibition is calculated. Cell viability is assessed using MTT or CellTiter-Glo assays.
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| Animal Protocol |
In vivo animal studies for URAT1 inhibitor 7 have not been extensively reported. If conducted, such studies might involve mouse or rat models of hyperuricemia, where URAT1 inhibitor 7 is administered orally and serum uric acid levels are measured. Standard protocols for hyperuricemia models would be employed. No specific data are available.
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| ADME/Pharmacokinetics |
URAT1 inhibitor 7 has a molecular weight of 428.82 and a molecular formula of C19H10ClFN4O3S. It displays microsomal stability (HLM <13 µL/min/mg). The compound's pharmacokinetic properties, including oral bioavailability and half-life, have been characterized in preclinical studies. It can be formulated for in vivo administration. Detailed PK parameters are available from preclinical studies.
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| Toxicity/Toxicokinetics |
The toxicity profile of URAT1 inhibitor 7 has been evaluated in preclinical studies. As a URAT1 inhibitor, its primary safety concerns would relate to effects on kidney function and uric acid excretion. It also inhibits CYP2C9, which may affect the metabolism of co-administered drugs. Standard toxicology assessments would include acute and sub-chronic toxicity studies in rodents, with endpoints including clinical signs, body weight, clinical pathology, and histopathology.
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| References | |
| Additional Infomation |
URAT1 inhibitor 7 is a research compound and has not been approved for clinical use. It is a potent URAT1 inhibitor with an IC50 of 12 nM that displays microsomal stability and inhibits CYP2C9. URAT1 inhibitor 7 can be used to study hyperuricemia and gout by reducing uric acid reabsorption and lowering serum uric acid levels.
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| Exact Mass |
428.01
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| Elemental Analysis |
C, 53.22; H, 2.35; Cl, 8.27; F, 4.43; N, 13.07; O, 11.19; S, 7.48
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| CAS # |
1632002-28-8
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| PubChem CID |
86294663
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
773
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=C(C=C1OC2=C(C=C(C=C2)S(=O)(=O)NC3=NC=C(C=C3)F)C#N)Cl)C#N
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| InChi Key |
ABKCBHGHCYFDNT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H10ClFN4O3S/c20-17-8-15(3-1-12(17)9-22)28-18-5-4-16(7-13(18)10-23)29(26,27)25-19-6-2-14(21)11-24-19/h1-8,11H,(H,24,25)
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| Chemical Name |
4-(3-chloro-4-cyanophenoxy)-3-cyano-N-(5-fluoropyridin-2-yl)benzenesulfonamide
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| Synonyms |
URAT1-inhibitor 7; URAT1 inhibitor7; URAT1 inhibitor-7; Compound 10f
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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