SSR 240612
SSR 240612 Basic information
- Product Name:
- SSR 240612
- Synonyms:
-
- SSR 240612
- (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
- SSR-240612 HCl
- SSR 240612; SSR-240612
- SSR-240612; SSR240612; SSR 240612
- CS-2687
- SSR 240612 hydrochloride
- (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
- CAS:
- 464930-42-5
- MF:
- C42H53ClN4O7S
- MW:
- 793.42
- Mol File:
- 464930-42-5.mol
SSR 240612 Chemical Properties
- 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
SSR 240612 Usage And Synthesis
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)
SSR 240612Supplier
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