1. GPCR/G Protein
  2. Bradykinin Receptor
  3. SSR240612

SSR240612 

Cat. No.: HY-15039 Purity: 99.19%
Handling Instructions

SSR240612 is a potent, and orally active specific non-peptide bradykinin B1 receptor antagonist, with Kis of 0.48 nM and 0.73 nM for B1 kinin receptors of human fibroblast MRC5 and HEK cells expressing human B1 receptors, 481 nM and 358 nM for B2 receptors of guinea pig ileum membranes and CHO cells expressing human B1 receptor, respectively.

For research use only. We do not sell to patients.

SSR240612 Chemical Structure

SSR240612 Chemical Structure

CAS No. : 464930-42-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 288 In-stock
Estimated Time of Arrival: December 31
5 mg USD 230 In-stock
Estimated Time of Arrival: December 31
10 mg USD 330 In-stock
Estimated Time of Arrival: December 31
25 mg USD 660 In-stock
Estimated Time of Arrival: December 31
50 mg USD 950 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Technical Information

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  • References

Description

SSR240612 is a potent, and orally active specific non-peptide bradykinin B1 receptor antagonist, with Kis of 0.48 nM and 0.73 nM for B1 kinin receptors of human fibroblast MRC5 and HEK cells expressing human B1 receptors, 481 nM and 358 nM for B2 receptors of guinea pig ileum membranes and CHO cells expressing human B1 receptor, respectively.

IC50 & Target

Ki: 0.48 nM (bradykinin B1 receptor, Human MRC5), 0.73 nM (bradykinin B1 receptor, Human HEK-B1), 481 nM (bradykinin B2 receptor, guinea pig ileum membranes), 358 nM (bradykinin B2 receptor, Human CHO-B2)[1]

In Vitro

SSR240612 is a potent bradykinin B1 receptor antagonist, with Kis of 0.48 nM and 0.73 nM for B2 kinin receptors of human fibroblast MRC5 and HEK cells expressing human B1 receptors, 481 nM and 358 nM for B1 receptors of guinea pig ileum membranes and CHO cells expressing human B1 receptor, respectively. SSR240612 inhibits inositol phosphate 1 formation with an IC50 of 1.9 nM, but shows no obvious effect on inositol phosphate-1 formation induced by BK (3 nM) activation of B2 receptor in human fibroblast MRC5[1].

In Vivo

SSR240612 (10 mg/kg p.o. or 0.3, 1 mg/kg i.p.) obviously blocks the des-Arg9-BK-induced paw edema in the mice. SSR240612 (10 and 30 mg/kg) reduces the duration of the late phase of paw licking in a dose dependent manner in the formalin model of inflammation in mice. SSR240612 (0.3, 3, and 30 mg/kg, p.o.) treatment before capsaicin potently and non-concentration-dependently reduces the ear edema. SSR240612 (0.3 mg/kg, i.v.) also suppresses the tissue destruction and neutrophil accumulation in the rat intestine, after splanchnic artery occlusion/reperfusion. Moreover, SSR240612 (1 and 3 mg/kg p.o.) dramacally increases the withdrawal latencies in the thermal hyperalgesia induced by UV irradiation in rats[1]. SSR240612 inhibits tactile and cold allodynia at 3 h in glucose-fed rats but had no effect in control rats with ID50s of 5.5 and 7.1 mg/kg, respectively. SSR240612 shows no effect on plasma glucose and insulin, insulin resistance (HOMA index) and aortic superoxide anion production in glucose-fed rats at 10 mg/kg[2].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 106.6 mg/mL (134.36 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2604 mL 6.3019 mL 12.6038 mL
5 mM 0.2521 mL 1.2604 mL 2.5208 mL
10 mM 0.1260 mL 0.6302 mL 1.2604 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

[3H]Lys0-des-Arg9-BK binding to cell membranes is 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 are 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. Filters are washed three times with 5 mL of binding buffer, and radioactivity is determined by liquid scintillation spectrometry. Nonspecific binding is determined by the addition of 1 μM of unlabeled Lys0-des-Arg9BK[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]
Groups of eight male albino mice under isoflurane anesthesia receive 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 under anesthesia receive 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] is 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 is 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 is 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. Statistical analysis is performed after verification of normality and homogeneity of variances using repeated ANOVA, then Duncan's test, treated groups versus des-Arg9-BK control group[1].
Rats[1]
SSR240612 (suspended with 0.1% Tween 80 in saline) is administered by the oral route in a volume of 20 mL/kg, 2 h before the thermal hyperalgesia measurement. In the time course study, the compound is administered at 3 mg/kg p.o. 0.08, 0.25, 0.5, 1, 2, 4, 6, 8, and 24 h before measuring the withdrawal latencies in rats. Results are expressed in seconds as mean withdrawal latencies (s) ± S.E.M., and statistical analyses are performed using a two-way ANOVA followed by Dunnett's test[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

793.41

Formula

C₄₂H₅₃ClN₄O₇S

CAS No.

464930-42-5

SMILES

O=S(N[[email protected]@H](C1=CC=C2C(OCO2)=C1)CC(N[[email protected]@H](C(N(C)C(C)C)=O)CC3=CC=C(CN([[email protected]@H]4C)[[email protected]](CCC4)C)C=C3)=O)(C5=CC(C=CC(OC)=C6)=C6C=C5)=O.Cl[H]

Shipping

Room temperature in continental US; may vary elsewhere

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SSR240612
Cat. No.:
HY-15039
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SSR240612

Cat. No.: HY-15039