A bradykinin B1 receptor antagonist
Technical Support & Resources

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

SSR 240612

Item No. 25544

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(3R)-3-(1,3-benzodioxol-5-yl)-N-[(6-methoxy-2-naphthalenyl)sulfonyl]-β-alanyl-4-[[(2R,6S)-2,6-dimethyl-1-piperidinyl]methyl]-N-methyl-N-(1-methylethyl)-D-phenylalaninamide, monohydrochloride
CAS Number
464930-42-5
Molecular Formula
C42H52N4O7S • HCl
Formula Weight
793.4
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 25 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH 7.2) (1:4): 0.20 mg/ml
λmax
241, 286 nm
SMILES
C[C@@H]1N(CC2=CC=C(C[C@H](C(N(C)C(C)C)=O)NC(C[C@H](C3=CC=C(OCO4)C4=C3)NS(C5=CC(C=CC(OC)=C6)=C6C=C5)(=O)=O)=O)C=C2)[C@H](C)CCC1.Cl
InChi Code
InChI=1S/C42H52N4O7S.ClH/c1-27(2)45(5)42(48)38(20-30-10-12-31(13-11-30)25-46-28(3)8-7-9-29(46)4)43-41(47)24-37(34-16-19-39-40(23-34)53-26-52-39)44-54(49,50)36-18-15-32-21-35(51-6)17-14-33(32)22-36;/h10-19,21-23,27-29,37-38,44H,7-9,20,24-26H2,1-6H3,(H,43,47);1H/t28-,29+,37-,38-;/m1./s1
InChi Key
GLHHFOSVBQQNAW-GDYXXZBVSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    1 mg

    $117

    Add

    5 mg

    $465

    Add

    10 mg

    $695

    Add

    25 mg

    $1,446

    Add
    Cayman Chemical
    Neutrophil Biology Wall Poster

    Explore how neutrophils shape the immune response in health and disease. This poster highlights neutrophil pathogen defense mechanisms, including phagocytosis, degranulation, and NETosis, as well as neutrophil roles in inflammation and NET-associated pathologies.

    DOWNLOAD NOW
    Product Description

    SSR 240612 is a selective, non-peptide antagonist of the bradykinin B1 receptor (Kis = 0.48-0.73 and 358-481 nM for B1 and B2 receptors, respectively).1 It inhibits the contraction of rabbit aorta and rat ileum induced by the B1 receptor agonist des-Arg9-bradykinin (des-Arg9-BK) ex vivo in a concentration-dependent manner. SSR 240612 (0.3 mg/kg) reduces tissue damage and neutrophil accumulation in a rat model of splanchnic artery occlusion/reperfusion-induced intestinal injury and inhibits des-Arg9-BK-induced paw edema in mice when administered orally at doses of 3 and 10 mg/kg or intraperitoneally at doses of 0.3 and 1 mg/kg. SSR 240612 (10 mg/kg per day) reduces fibrosis in a unilateral ureteral obstruction mouse model of kidney fibrosis.2 It also reduces mean arterial blood pressure in two rat models of hypertension when administered at doses of 5 and 10 mg/kg and reduces plasma glucose and insulin levels in a glucose-fed rat model of insulin resistance when administered at a dose of 10 mg/kg per day.3,4 SSR 240612 also exhibits analgesic properties in several rodent models of hyperalgesia.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gougat, J., Ferrari, B., Sarran, L., et al. SSR240612 [(2R)-2-[((3R)-3-(1,3-benzodioxol-5-yl)-3-[[(6-methoxy-2-naphthyl)sulfonyl]amino]propanoyl)amino]-3-(4-[[2R,6S)-2,6-dimethylpiperidinyl]methyl]phenyl)-N-isopropyl-N-methylpropanamide hydrochloride], a new nonpeptide antagonist of the bradykinin B1 receptor: Biochemical and pharmacological characterization. J. Pharmacol. Exp. Ther. 309(2), 661-669 (2004).

    2. Huart, A., Klein, J., Gonzalez, J., et al. Kinin B1 receptor antagonism is equally efficient as angiotensin receptor 1 antagonism in reducing renal fibrosis in experimental obstructive nephropathy, but is not additive. Front. Pharmacol. 6:8, (2015).

    3. De Brito Gariepy, H., Carayon, P., Ferrari, B., et al. Contribution of the central dopaminergic system in the anti-hypertensive effect of kinin B1 receptor antagonists in two rat models of hypertension. Neuropeptides 44(2), 191-198 (2010).

    4. Dias, J.P., and Couture, R. Blockade of kinin B1 receptor reverses plasma fatty acids composition changes and body and tissue fat gain in a rat model of insulin resistance. Diabetes Obes. Metab. 14(3), 244-253 (2012).