| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
BMS-248360 targets both the angiotensin II receptor type 1 (AT1) and the endothelin A (ETA) receptor. It has Ki values of 10 nM for human AT1 (hAT1), 1.9 nM for human ETA (hETA), 6.0 nM for rat AT1 (rAT1), and 1.9 nM for rat ETA (rETA). It shows no activity against AT2 or ETB receptor subtypes.
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|---|---|
| ln Vitro |
Rat AT1 and rat ETA receptors are active against BMS-248360, with Kis values of 6.0 nM and 1.9 nM, respectively[1]. When it comes to AT2 and ETB receptor subtypes, BMS-248360 is inert [1].
BMS-248360 shows activity against rat AT1 and rat ETA receptors with Ki values of 6.0 nM and 1.9 nM, respectively. It displays no activity against AT2 and ETB receptor subtypes, confirming its selectivity for AT1 and ETA over related receptors. The compound's dual antagonism has been confirmed in radioligand binding assays. |
| ln Vivo |
Rats were shown to have good oral exposure (Cmax = 3.1 µM) and a decent elimination profile (T1/2 = 5.5 hours) for BMS-248360, making it orally accessible (%F=38) [1]. Intravenous AII causes hypertension, although BMS-248360 (30 µmol/kg, 100 µmol/kg; oral) prevents this effect [1].
BMS-248360 is orally bioavailable in rats (%F = 38) with excellent oral exposure (Cmax = 3.1 µM) and a reasonable elimination profile (T1/2 = 5.5 hours). At 30 µmol/kg and 100 µmol/kg (p.o.), it blocks the hypertensive effects of intravenously administered angiotensin II (AII) in male rats. |
| Enzyme Assay |
BMS-248360 is evaluated in radioligand binding assays using membranes expressing human or rat AT1, ETA, AT2, and ETB receptors. Ki values are determined by competition binding experiments. Selectivity is confirmed by lack of activity at AT2 and ETB receptors.
|
| Cell Assay |
BMS-248360 is tested in cell lines expressing AT1 or ETA receptors to assess functional antagonism. Readouts include inhibition of angiotensin II- or endothelin-1-induced signaling (e.g., calcium mobilization, second messenger production). Selectivity is confirmed in cells expressing AT2 or ETB receptors.
|
| Animal Protocol |
Animal/Disease Models: Male rats [1]
Doses: 30 µM/kg, 100 µM/kg Route of Administration: Oral Experimental Results:Blocks the hypertensive effect of intravenous (iv) (iv)injection of AII. Animal/Disease Models: Male rat[1] Doses: 10 µM/kg Route of Administration: Oral Experimental Results:T1/2= 5.5 hrs (hrs (hours)) BMS-248360 is evaluated in male rats at oral doses of 30 µmol/kg and 100 µmol/kg. The compound blocks the hypertensive effects of intravenously administered angiotensin II. Pharmacokinetic parameters (F=38%, Cmax=3.1 µM, T1/2=5.5 h) are also determined in rats. |
| References |
| Molecular Formula |
C36H45N5O5S
|
|---|---|
| Molecular Weight |
659.84
|
| Exact Mass |
659.314
|
| CAS # |
254737-87-6
|
| PubChem CID |
9895957
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
7.226
|
| tPSA |
133.56
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
11
|
| Heavy Atom Count |
47
|
| Complexity |
1290
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1(C2=CC=C(CN3C(=O)C4(CCCC4)N=C3CCCC)C=C2CN2CCC(C)(C)C2=O)=CC=CC=C1S(NC1ON=C(C)C=1C)(=O)=O
|
| InChi Key |
NBDFXMDYBLSGLX-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C36H45N5O5S/c1-6-7-14-31-37-36(17-10-11-18-36)34(43)41(31)22-26-15-16-28(27(21-26)23-40-20-19-35(4,5)33(40)42)29-12-8-9-13-30(29)47(44,45)39-32-24(2)25(3)38-46-32/h8-9,12-13,15-16,21,39H,6-7,10-11,14,17-20,22-23H2,1-5H3
|
| Chemical Name |
2-[4-[(2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl]-2-[(3,3-dimethyl-2-oxopyrrolidin-1-yl)methyl]phenyl]-N-(3,4-dimethyl-1,2-oxazol-5-yl)benzenesulfonamide
|
| Synonyms |
BMS-248360 BMS248360 BMS 248360
|
| 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)
|
| 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 | 1.5155 mL | 7.5776 mL | 15.1552 mL | |
| 5 mM | 0.3031 mL | 1.5155 mL | 3.0310 mL | |
| 10 mM | 0.1516 mL | 0.7578 mL | 1.5155 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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