Chemical Structure : NVP-SAA164
CAS No.:
312722-60-4
NVP-SAA164
Catalog No.: PC-26636Not For Human Use, Lab Use Only.
NVP-SAA164 is a potent, selective orally active nonpeptide bradykinin B1 receptor (B1R) antagonist with Ki of 8 nM, inhibits increases in intracellular calcium induced by desArg10kallidin (desArg10KD) with IC50 of 33 nM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
NVP-SAA164 is a potent, selective orally active nonpeptide bradykinin B1 receptor (B1R) antagonist with Ki of 8 nM, inhibits increases in intracellular calcium induced by desArg10kallidin (desArg10KD) with IC50 of 33 nM.
NVP-SAA164 shows high affinity in monkey fibroblasts with Ki of 7.7 nM, shows no affinity for the rat B1 receptor expressed in Cos-7 cells.
NVP-SAA164 exhibits marked selectivity for the human receptor, with no affinity for the rat B1 receptor.
Oral administration of NVP-SAA164 produced a dose-related reversal of FCA-induced mechanical hyperalgesia and desArg10KD-induced hyperalgesia in hB1-KI mice.
Physicochemical Properties
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M.Wt
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659.85
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Formula
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C36H45N5O5S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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Methanone, [2-[(2,2-diphenylethyl)amino]-5-[[4-[(4-methyl-1-piperazinyl)carbonyl]-1-piperidinyl]sulfonyl]phenyl]-4-morpholinyl-
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References
1. Alyson Fox, et al. Br J Pharmacol. 2005 Apr;144(7):889-99.
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