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SSR240612

CAT: 0804-HY-15039-01Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-15039-01Size:1 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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.
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.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, sealed storage, away from moisture)
Scientific Category
Reference compound1
Clinical Information
Phase 2
Isoform
Bradykinin B1 Receptor (B1R)