Shopping Cart
  • Remove All
  • TargetMol
    Your shopping cart is currently empty

SSR240612

🥰Excellent
Catalog No. T5048Cas No. 464930-42-5

SSR240612 is a potent, orally active, specific non-peptide bradykinin B1 receptor antagonist (Kis = 0.48-0.73 nM for B1 receptors and 358-481 nM for B2 receptors, respectively).

SSR240612

SSR240612

🥰Excellent
Purity: 99.16%
Catalog No. T5048Cas No. 464930-42-5
SSR240612 is a potent, orally active, specific non-peptide bradykinin B1 receptor antagonist (Kis = 0.48-0.73 nM for B1 receptors and 358-481 nM for B2 receptors, respectively).
Pack SizePriceAvailabilityQuantity
1 mg$247In Stock
2 mg$357In Stock
5 mg$569In Stock
10 mg$778In Stock
25 mg$1,090In Stock
50 mg$1,480In Stock
100 mg$1,980In Stock
1 mL x 10 mM (in DMSO)$749In Stock
Bulk & Custom
Add to Cart
Questions
View More

Related Compound Libraries of "SSR240612"

Select Batch
Purity:99.16%
Contact us for more batch information
Resource Download
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Product Introduction

Bioactivity
Description
SSR240612 is a potent, orally active, specific non-peptide bradykinin B1 receptor antagonist (Kis = 0.48-0.73 nM for B1 receptors and 358-481 nM for B2 receptors, respectively).
Targets&IC50
Bradykinin B1 (human MRC5):0.48 nM (Ki), Bradykinin B2 (human CHO-B2):358 nM (Ki), Bradykinin B1 (human HEK-B1):0.73 nM (Ki)
In vitro
SSR240612 inhibited the binding of [(3)H]Lys(0)-des-Arg(9)-BK to the B(1) receptor in human fibroblast MRC5 and to recombinant human B(1) receptor expressed in human embryonic kidney cells with inhibition constants (K(i)) of 0.48 and 0.73 nM, respectively. SSR240612 inhibited Lys(0)-desAr(9)-BK (10 nM)-induced inositol monophosphate formation in human fibroblast MRC5, with an IC(50) of 1.9 nM [1]. M. tuberculosis was not susceptible to the concentrations of antagonists tested, which suggests that the minimum inhibitory concentration values are larger than 250 μM for SSR240612 [2].
In vivo
SSR240612 inhibited des-Arg(9)-BK-induced paw edema in mice (3 and 10 mg/kg p.o. and 0.3 and 1 mg/kg i.p.). Moreover, SSR240612 reduced capsaicin-induced ear edema in mice (0.3, 3 and 30 mg/kg p.o.) and tissue destruction and neutrophil accumulation in the rat intestine following splanchnic artery occlusion/reperfusion (0.3 mg/kg i.v.). The compound also inhibited thermal hyperalgesia induced by UV irradiation (1 and 3 mg/kg p.o.) and the late phase of nociceptive response to formalin in rats (10 and 30 mg/kg p.o.). SSR240612 (20 and 30 mg/kg p.o.) prevented neuropathic thermal pain induced by sciatic nerve constriction in the rat [1]. SSR240612 blocked tactile and cold allodynia at 3 h (ID(50)=5.5 and 7.1 mg/kg, respectively) in glucose-fed rats but had no effect in control rats. The antagonist (10 mg/kg) had no effect on plasma glucose and insulin, insulin resistance (HOMA index) and aortic superoxide anion production in glucose-fed rats [3].
Kinase Assay
MRC5 human fibroblasts and transfected HEK-293 cells expressing human B1 receptors were routinely grown in Dulbecco's modified Eagle's medium (DMEM) with Glutamax-I supplemented with 10% fetal calf serum and antibiotics. MRC5 were incubated for 4 h in DMEM containing 0.5 μg/ml interleukin-1β (IL-1β) to induce B1 receptor synthesis. Cells were scraped and homogenized for 1 min using a Polytron (setting 8) in 25 mM TES-HCl containing 1 mM 1-10 phenantrolin. Homogenates were centrifuged at 40,000g for 15 min at 4°C, and pellets were resuspended in the same buffer using the Polytron (setting 8) for 1 min. Membranes were pelleted at 40,000g for 10 min at 4°C, resuspended in the same buffer, and conserved at 80°C. [3H]Lys0-des-Arg9-BK binding to cell membranes was performed in binding buffer of the following composition: 137 mM NaCl, 5.4 mM KCl, 1.05 mM MgCl2, 1.8 mM CaCl2, 1.2 mM NaH2PO4, 15.5 mM NaHCO3, 10 mM HEPES, 1 g/l bovine serum albumin (BSA), 140 mg/l bacitracin, and 1 μM captopril, pH 7.4. Membranes were incubated for 30 min at 25°C in 500 μl of binding buffer containing 1 nM [3H]Lys0-des-Arg9-BK for competition curves or 0.1 to 10 nM for saturation isotherms. The reaction was terminated by filtration using a Brandel Harvester onto GF/B Whatman filters previously soaked for 2 h in 0.1% polyethyleneimine. Filters were washed three times with 5 ml of binding buffer, and radioactivity was determined by liquid scintillation spectrometry. Nonspecific binding was determined by the addition of 1 μM of unlabeled Lys0 -des-Arg9 BK [1].
Cell Research
[3H]Inositol phosphate1 accumulation was measured in MRC5 fibroblasts labeled with [3H]myoinositol according to the method described by Oury-Donat et al. Cells cultured in 6-well plates were labeled for 48 h with 5 μCi/ml [3H]myoinositol added to the culture medium (DMEM). Cells were then incubated for 4 h in DMEM containing 0.5 μg/ml IL-1β to induce B1 receptor synthesis. Agonist stimulation of inositol phosphate 1 accumulation was performed in DMEM containing 50 mM LiCl and test compounds. Antagonists were added 15 min before 10 nM Lys0-desArg10BK. After 30 min of incubation at 37°C, the medium was discarded, and the reaction was stopped by rapid addition of 1 ml of cold methanol and 1 N HCl (v/v). The cells were scraped, and the suspension was transferred to a glass tube with 1 ml of chloroform and 20 μl of 12 N HCl. The aqueous phase was neutralized by 350 μl of 1 M NaHCO3 and applied to 1 ml of Dowex AG1 × eight columns. [3H]inositol phosphate 1 was eluted with 0.2 M ammonium formate and 0.1 M formic acid. Radioactivity was measured by liquid scintillation spectrometry [1].
Animal Research
Groups of eight male albino mice under isoflurane anesthesia received a 20-μl intraplantar injection into the right hind paw of 5 μg of IL-1β in phosphate-buffered saline/0.1% BSA. Forty minutes later (T = 0), mice received, under anesthesia, a 20-μl intraplantar injection in the same paw of des-Arg9-BK (10 μg/paw) in water. SSR240612 or vehicle [5% (v/v) ethanol and 5% (v/v) Tween 80 in water] was administered by oral route at the doses of 1, 3, and 10 mg/kg 1 h before des-Arg9-BK injection and by intraperitoneal route at the doses of 0.1, 0.3, and 1 mg/kg 40 min before des-Arg9-BK injection. Paw volume was measured with a plethysmometer at T =-2 h (initial measurement) and at several times after edema induction (T = 20, 40, 60, and 120 min). Paw edema volume was expressed in milliliters as the difference between the paw volume at each time after edema induction and the initial paw volume. Results for each group are expressed as mean ± S.E.M. of individual paw edema volumes [1].
Chemical Properties
Molecular Weight793.41
FormulaC42H53ClN4O7S
Cas No.464930-42-5
SmilesCl.COc1ccc2cc(ccc2c1)S(=O)(=O)N[C@H](CC(=O)N[C@H](Cc1ccc(CN2[C@@H](C)CCC[C@H]2C)cc1)C(=O)N(C)C(C)C)c1ccc2OCOc2c1
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
H2O: Insoluble
DMSO: 100 mg/mL (126 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.2604 mL6.3019 mL12.6038 mL63.0191 mL
5 mM0.2521 mL1.2604 mL2.5208 mL12.6038 mL
10 mM0.1260 mL0.6302 mL1.2604 mL6.3019 mL
20 mM0.0630 mL0.3151 mL0.6302 mL3.1510 mL
50 mM0.0252 mL0.1260 mL0.2521 mL1.2604 mL
100 mM0.0126 mL0.0630 mL0.1260 mL0.6302 mL

Calculator

  • Molarity Calculator
  • Dilution Calculator
  • Reconstitution Calculator
  • Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
%Tween 80
%ddH2O

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

Related Tags: buy SSR240612 | purchase SSR240612 | SSR240612 cost | order SSR240612 | SSR240612 chemical structure | SSR240612 in vivo | SSR240612 in vitro | SSR240612 formula | SSR240612 molecular weight