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Epaminurad (UR-1102) is a novel and potent urate transporter URAT1 inhibitor and a uricosuric agent with the potential to be used for gout and hyperuricemia. It is an orally bioactive urate transporter inhibitor with a Ki of 0.057 μM. Epaminurad inhibits OAT1 and OAT3 (organic anion transporter) modestly.
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| ln Vitro |
UR-1102 (0–12 μM) prevents HEK293 cells transiently expressing URAT1, OAT1, or OAT3 from absorbing urate and PAH (p-aminohippuric acid)[1].
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| ln Vivo |
Epaminurad (0–30 mg/kg, Orally, once daily for three days in a row) has urate-lowering and uricosuric properties[1]. Epaminurad (3–30 mg/kg, Orally, once) decreases plasma uric acid more efficiently, enhances the fractional excretion of urine uric acid, and exhibits an excellent pharmacokinetic profile[1]. Epaminurad (UR-1102) pharmacokinetic parameters in tufted capuchin monkeys[1]. Section 3 mg/kg; Group 10 mg/kg; Group 30 mg/kg; Cmax (μg/mL) 8.96 ± 1.74; 42.4 ± 12.8 92.9 ± 21.0; Tmax (h) 0.6 ± 0.2 0.5 ± 0.0 0.8 ± 0.3; T1/2 (h) 4.7 ± 0.9 4.2 ± 1.1 3.3 ± 0.8; AUC0-inf (mg*h/ mL) 26.2 ± 8.1 108 ± 51 257 ± 60
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| Animal Protocol |
Animal/Disease Models: Tufted capuchin monkeys[1]
Doses: 0, 3, 10, and 30 mg/kg Route of Administration: Orally, one time/day, for 3 days Experimental Results: demonstrated good uricosuric and urate-lowering effects at 3 mg/kg, the lowest dose, which were comparable to those of benzbromarone at 100 mg/kg, the highest dose, with maximum efficacy. Animal/Disease Models: Tufted capuchin monkeys[1] Doses: 0, 3 , 10, and 30 mg/kg Route of Administration: Orally, once Experimental Results: demonstrated a good pharmacokinetic/PK profile. demonstrated both good systemic exposure and Dramatically great plasma urate-lowering at 3 mg/kg. |
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| Additional Infomation |
Lowering uric acid levels is essential for treating gout, but existing medications are insufficient in controlling serum uric acid levels. While uricosuric drugs benzbromarone and probenecid can inhibit a uric acid reabsorption transporter called renal urate transporter 1 (URAT1), thereby lowering serum uric acid levels, they also inhibit other transporters responsible for excreting uric acid into the urine. This suggests that selective inhibition of URAT1 might be more effective in lowering serum uric acid levels. We discovered a novel, highly potent, and selective URAT1 inhibitor, UR-1102, and compared its efficacy with benzbromarone in vitro and in vivo. In human embryonic kidney (HEK) 293 cells overexpressing urea transporter 1 (URAT1), organic anion transporter 1 (OAT1), and organic anion transporter 3 (OAT3), benzbromarone showed similar inhibitory effects on all transporters; while UR-1102 showed comparable inhibitory effects on URAT1 to benzbromarone, but weaker inhibitory effects on OAT1 and OAT3. UR-1102 (3-30 mg/kg) or benzbromarone (3-100 mg/kg) was administered orally once daily for 3 consecutive days to capuchin monkeys with low uricase activity, resulting in high plasma uric acid levels. Compared with the same dose of benzbromarone, UR-1102 showed better pharmacokinetic characteristics, increased the fractional excretion of uric acid in urine, and more effectively reduced plasma uric acid levels. In addition, the maximum efficacy of UR-1102 was twice that of benzbromarone, indicating that selective inhibition of URAT1 is effective. Furthermore, UR-1102 showed a lower mechanism of hepatotoxicity caused by benzbromarone in vitro. These results suggest that UR-1102 exerts a potent uricosuric effect in monkeys by selectively inhibiting URAT1 rather than OAT1 and OAT3, and may become a novel treatment option for patients with gout or hyperuricemia. [1]
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| Molecular Formula |
C14H10BR2N2O3
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| Molecular Weight |
414.05
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| Exact Mass |
411.905
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| Elemental Analysis |
C, 40.61; H, 2.43; Br, 38.60; N, 6.77; O, 11.59
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| CAS # |
1198153-15-9
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| Related CAS # |
1198153-46-6 (HCl)
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| PubChem CID |
44608229
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| Appearance |
White to off-white solid powder
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| Density |
1.9±0.1 g/cm3
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| Boiling Point |
530.0±50.0 °C at 760 mmHg
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| Flash Point |
274.3±30.1 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.691
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| LogP |
3.05
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
21
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| Complexity |
386
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZMVGQIIOXCGAFV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H10Br2N2O3/c15-9-5-8(6-10(16)13(9)19)14(20)18-3-4-21-12-1-2-17-7-11(12)18/h1-2,5-7,19H,3-4H2
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| Chemical Name |
(3,5-dibromo-4-hydroxyphenyl)-(2,3-dihydropyrido[4,3-b][1,4]oxazin-4-yl)methanone
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| Synonyms |
Epaminurad; UR-1102; Epaminurad; URC-102; 1198153-15-9; UR 1102; Epaminurad [INN]; URC102; 0YP1ME85GH; UNII-0YP1ME85GH; CHEMBL4640580; UR1102
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4152 mL | 12.0758 mL | 24.1517 mL | |
| 5 mM | 0.4830 mL | 2.4152 mL | 4.8303 mL | |
| 10 mM | 0.2415 mL | 1.2076 mL | 2.4152 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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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