SSR240612

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.

Product Specifications

CAS Number

[464930-42-5]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Bradykinin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

COVID-19-immunoregulation

Field of Research

Metabolic Disease; Inflammation/Immunology; Endocrinology

Assay Protocol

https://www.medchemexpress.com/SSR240612.html

Concentration

10mM

Purity

98.72

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C42H53ClN4O7S

Molecular Weight

793.41

Precautions

H302, H315, H319, H335

References & Citations

[1]Gougat J, 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. 2004 May;309 (2) :661-9.|[2]Dias JP, et al. The kinin B1 receptor antagonist SSR240612 reverses tactile and cold allodynia in an experimental rat model of insulin resistance. Br J Pharmacol. 2007 Sep;152 (2) :280-7. Epub 2007 Jul 9.