| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
UT (urotensin II receptor, GPR14) – Ki = 121 nM at rat recombinant UT receptor. SB-611812 acts as a competitive antagonist with pA₂ values of 6.60 (inhibition of U-II-induced [Ca²⁺]i mobilization in rat UT-HEK293 cells) and 6.59 (inhibition of U-II-induced contraction in rat isolated aorta). It is selective for UT over other receptors (no effect on KCl, phenylephrine, endothelin-1, or angiotensin-II-induced contractions at 10 µM). [1][2]
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| ln Vitro |
SB-611812 is a potent ligand at the rat recombinant UT receptor with a Ki of 121 nM and acts as a competitive antagonist, inhibiting U-II-induced calcium mobilization in rat UT-HEK293 cells (pA₂ = 6.60) and U-II-induced contraction of rat isolated aorta (pA₂ = 6.59). Pretreatment of rat aorta with 10 µM SB-611812 (40-fold higher than its pA₂) did not alter contractions induced by KCl, phenylephrine, endothelin-1, or angiotensin-II, confirming its selectivity for the UT receptor. [1]
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| ln Vivo |
In a rat carotid artery balloon angioplasty model, daily oral administration of SB-611812 (30 mg/kg for 28 days) significantly reduced intima-to-media area ratio (from 1.777±0.708 in vehicle to 0.703±0.354, P<0.005) and intima-to-media length ratio (from 3.210±1.658 to 0.732±0.511, P<0.002), indicating reduced neointimal formation. [1]
As reviewed in [2], additional studies (Bousette et al.) demonstrated that SB-611812 treatment in a rat heart failure model (coronary ligation) significantly reduced mortality (P=0.024) and improved cardiac function (left ventricle end diastolic pressure reduced by 70%, central venous pressure by 58%, lung weight to dry weight ratio by 71%); delayed treatment starting on day 10 was also protective. In a further study, SB-611812 (30 mg/kg/day for 8 weeks) significantly decreased myocardial interstitial fibrosis in the non-infarct left ventricle zone (P=0.004) and reduced collagen I:III ratio by 83% (P<0.05). [2] |
| Enzyme Assay |
Receptor binding assay: Competition binding using rat recombinant UT receptor expressed in HEK293 cells with radiolabeled U-II to determine Ki (121 nM). [1]
Functional calcium mobilization assay: Rat UT-HEK293 cells were loaded with calcium-sensitive dye, and the inhibition of U-II-induced intracellular calcium increase by SB-611812 was measured; pA₂ = 6.60. [1] Vascular contraction assay: Rat isolated aortic rings were pre-contracted with U-II, and the antagonistic effect of SB-611812 was evaluated, yielding pA₂ = 6.59. Selectivity was confirmed by testing against other vasoconstrictors (KCl, phenylephrine, endothelin-1, angiotensin-II) at 10 µM. [1] |
| Cell Assay |
Calcium mobilization assay in rat UT-HEK293 cells: Cells expressing rat recombinant UT receptor were loaded with a calcium-sensitive fluorescent indicator, and the ability of SB-611812 to inhibit U-II-induced calcium flux was measured. The compound acted as a competitive antagonist with a pA₂ of 6.60. [1]
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| Animal Protocol |
Balloon angioplasty model in rats: Male Lewis rats (350-420 g) underwent right common carotid artery balloon injury using a 2F Fogarty catheter. From the day after surgery, rats received either vehicle (1% methylcellulose in water) or SB-611812 at 30 mg/kg via oral gavage (1 ml/200 g body weight, once daily) for 28 days. Sham-operated rats served as controls. At study end, carotid arteries were collected, and intima-to-media area and length ratios were measured. [1]
Heart failure model (as reviewed in [2]): Lewis rats underwent coronary artery ligation. Treatment with SB-611812 (30 mg/kg/day, oral gavage) was initiated on the day of ligation or delayed (day 10) and continued for up to 8 weeks. Cardiac function, survival, and fibrosis were assessed. [2] |
| ADME/Pharmacokinetics |
Oral bioavailability: ~100% in rats. Elimination half-life: 4-5 hours after oral gavage in rats. [1][2]
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| References |
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| Additional Infomation |
SB-611812 is a selective UT receptor antagonist with no activity against contractions induced by KCl, phenylephrine, endothelin-1, or angiotensin-II at concentrations up to 10 µM. [1]
It shows high oral bioavailability (~100%) and a moderate half-life (4-5 h), making it suitable for once-daily oral administration in rodent models. [1][2] The compound's ability to reduce neointimal formation after balloon angioplasty suggests a therapeutic potential for restenosis. [1] As reviewed in [2], additional studies indicate that SB-611812 may also reduce mortality and improve cardiac function in heart failure models, and decrease myocardial fibrosis, further supporting its cardioprotective potential. [2] |
| Molecular Formula |
C17H16N2O3F3SCL3
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|---|---|
| Molecular Weight |
491.73974
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| Exact Mass |
489.99
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| CAS # |
345892-71-9
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| PubChem CID |
10278166
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
6.56
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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 |
7
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| Heavy Atom Count |
29
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| Complexity |
622
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
UIZHOFJFIOCYLH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H16Cl3F3N2O3S/c1-25(2)5-6-28-15-9-11(3-4-12(15)18)24-29(26,27)16-13(19)7-10(8-14(16)20)17(21,22)23/h3-4,7-9,24H,5-6H2,1-2H3
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| Chemical Name |
2,6-dichloro-N-[4-chloro-3-[2-(dimethylamino)ethoxy]phenyl]-4-(trifluoromethyl)benzenesulfonamide
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
DMSO : ~16.67 mg/mL (~33.90 mM)
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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 | 2.0336 mL | 10.1680 mL | 20.3359 mL | |
| 5 mM | 0.4067 mL | 2.0336 mL | 4.0672 mL | |
| 10 mM | 0.2034 mL | 1.0168 mL | 2.0336 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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