| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
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| Other Sizes |
| Targets |
Endothelin A receptor (ETA), Endothelin B receptor (ETB).
|
|---|---|
| ln Vitro |
SB-209670 is an extremely potent and highly specific non-peptide endothelin receptor antagonist. It selectively inhibits binding of ¹²⁵I-labeled ET-1 to cloned human ETA and ETB receptors with Ki values of 0.2 nM and 18 nM, respectively. It demonstrates subnanomolar affinity for ETA.
|
| ln Vivo |
SB-209670 produces a dose-dependent reduction in blood pressure in hypertensive rats. It prevents ischemia-induced neuronal degeneration in the gerbil stroke model. It attenuates neointima formation after rat carotid balloon angioplasty. These data demonstrate its in vivo efficacy in multiple cardiovascular disease models.
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| Enzyme Assay |
Radioligand binding assays are performed using membrane preparations from cells expressing human ETA or ETB receptors. Membranes are incubated with ¹²⁵I-labeled ET-1 (20-50 pM) and varying concentrations of SB-209670 (0.001 nM-10 μM) in 50 mM Tris-HCl buffer (pH 7.4) containing 0.1% BSA at 25°C for 2 hours. Non-specific binding is determined with 100 nM unlabeled ET-1. The Ki value is determined by measuring the displacement of specific binding, with termination via rapid filtration through GF/B filters.
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| Cell Assay |
Functional assays are performed using cultured cells expressing human ETA or ETB receptors. Cells are pre-incubated with SB-209670 (0.001 nM-10 μM) for 15-30 minutes and then stimulated with ET-1 (1-10 nM). Receptor-mediated signaling (e.g., intracellular Ca²⁺ mobilization, inhibition of cAMP accumulation) is measured, and the IC₅₀ is calculated from concentration-response curves.
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| Animal Protocol |
In a hypertensive rat model, SB-209670 is administered intravenously or intraperitoneally to spontaneously hypertensive rats at doses of 0.01-1 mg/kg. Mean arterial pressure is measured via an indwelling catheter. In a gerbil stroke model, it is administered prior to or after bilateral carotid artery occlusion, and neuronal degeneration is assessed by histological staining. In a rat carotid balloon angioplasty model, it is administered via osmotic pump or injection, and neointima formation is assessed by morphometric analysis of carotid arteries.
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| References |
| Molecular Formula |
C29H28O9
|
|---|---|
| Molecular Weight |
520.52722
|
| Exact Mass |
520.173
|
| CAS # |
157659-79-5
|
| PubChem CID |
108002
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
4.9
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| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
10
|
| Heavy Atom Count |
38
|
| Complexity |
820
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
CCCOC1=CC2=C(C=C1)[C@@H]([C@H]([C@@H]2C3=C(C=C(C=C3)OC)OCC(=O)O)C(=O)O)C4=CC5=C(C=C4)OCO5
|
| InChi Key |
UUAVCCWBNUITBB-UPRLRBBYSA-N
|
| InChi Code |
InChI=1S/C29H28O9/c1-3-10-35-18-6-7-19-21(12-18)27(20-8-5-17(34-2)13-23(20)36-14-25(30)31)28(29(32)33)26(19)16-4-9-22-24(11-16)38-15-37-22/h4-9,11-13,26-28H,3,10,14-15H2,1-2H3,(H,30,31)(H,32,33)/t26-,27+,28+/m0/s1
|
| Chemical Name |
(1S,2R,3S)-1-(1,3-benzodioxol-5-yl)-3-[2-(carboxymethoxy)-4-methoxyphenyl]-5-propoxy-2,3-dihydro-1H-indene-2-carboxylic acid
|
| Synonyms |
SB 209670 SB209670SB-209670
|
| HS Tariff Code |
2934.99.9001
|
| 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 | 1.9211 mL | 9.6056 mL | 19.2112 mL | |
| 5 mM | 0.3842 mL | 1.9211 mL | 3.8422 mL | |
| 10 mM | 0.1921 mL | 0.9606 mL | 1.9211 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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