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ChemicalBook--->CAS DataBase List--->464930-42-5

464930-42-5

464930-42-5 Structure

464930-42-5 Structure
IdentificationBack Directory
[Name]

SSR 240612
[CAS]

464930-42-5
[Synonyms]

CS-2687
SSR 240612
SSR-240612 HCl
SSR 240612; SSR-240612
SSR 240612 hydrochloride
SSR-240612; SSR240612; SSR 240612
(R)-2-((R)-3-(Benzo[d][1,3]dioxol-5-yl)-3-(6-methoxynaphthalene-2-sulfonamido)propanamido)-3-(4-(((2R,6S)-2,6-dimethylpiperidin-1-yl)methyl)phenyl)-N-isopropyl-N-methylpropanamide hydrochloride
(2R)-2-[[(3R)-3-(1,3-benzodioxol-5-yl)-3-[(6-methoxynaphthalen-2-yl)sulfonylamino]propanoyl]amino]-3-[4-[[(2S,6R)-2,6-dimethylpiperidin-1-yl]methyl]phenyl]-N-methyl-N-propan-2-ylpropanamide:hydrochloride
[Molecular Formula]

C42H53ClN4O7S
[MDL Number]

MFCD19443777
[MOL File]

464930-42-5.mol
[Molecular Weight]

793.42
Chemical PropertiesBack Directory
[storage temp. ]

Store at -20°C
[solubility ]

DMF: 30 mg/ml; DMSO: 25 mg/ml; Ethanol: 30 mg/ml; Ethanol:PBS (pH 7.2) (1:4): 0.20 mg/ml
[form ]

A crystalline solid
[color ]

White to off-white
Safety DataBack Directory
[Symbol(GHS) ]


GHS07
[Signal word ]

Warning
[Hazard statements ]

H302-H315-H319-H335
[Precautionary statements ]

P261-P305+P351+P338
[HS Code ]

2935909099
Hazard InformationBack Directory
[Uses]

SSR 240612, is a potent, and orally active specific non-peptide bradykinin B1 receptor antagonist.
[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].

[IC 50]

Bradykinin B1 Receptor (B1R)
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