(2R,4S)-N-[1-[3,5-Bis(trifluoromethyl)benzoyl]-2-(4-chlorobenzyl)piperidin-4-yl]quinoline-4-carboxamide
- Product Name
- (2R,4S)-N-[1-[3,5-Bis(trifluoromethyl)benzoyl]-2-(4-chlorobenzyl)piperidin-4-yl]quinoline-4-carboxamide
- CAS No.
- 177707-12-9
- Chemical Name
- (2R,4S)-N-[1-[3,5-Bis(trifluoromethyl)benzoyl]-2-(4-chlorobenzyl)piperidin-4-yl]quinoline-4-carboxamide
- Synonyms
- NK-608;NK 608;NKP-608;NK 608;NK-608;NKP-608,NKP608;(2R,4S)-N-[1-[3,5-Bis(trifluoromethyl)benzoyl]-2-(4-chlorobenzyl)piperidin-4-yl]quinoline-4-carboxamide;N-((2R,4S)-1-(3,5-bis(trifluoromethyl)benzoyl)-2-(4-chlorobenzyl)piperidin-4-yl)quinoline-4-carboxamide;N-[(2R,4S)-1-[3,5-Bis(trifluoromethyl)benzoyl]-2-[(4-chlorophenyl)methyl]-4-piperidinyl]-4-quinolinecarboxamide;NKP-608((2R,4S)-N-[1-[3,5-Bis(trifluoromethyl)benzoyl]-2-(4-chlorobenzyl)piperidin-4-yl]quinoline-4-carboxamide);4-Quinolinecarboxamide, N-[(2R,4S)-1-[3,5-bis(trifluoromethyl)benzoyl]-2-[(4-chlorophenyl)methyl]-4-piperidinyl]-
- CBNumber
- CB72462173
- Molecular Formula
- C31H24ClF6N3O2
- Formula Weight
- 619.98
- MOL File
- 177707-12-9.mol
(2R,4S)-N-[1-[3,5-Bis(trifluoromethyl)benzoyl]-2-(4-chlorobenzyl)piperidin-4-yl]quinoline-4-carboxamide Property
- Boiling point:
- 719.2±60.0 °C(Predicted)
- Density
- 1.44±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 100 mg/mL (161.30 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble)
- form
- Powder
- pka
- 12.92±0.40(Predicted)
- color
- Light yellow to yellow
N-Bromosuccinimide Price
- Product number
- FN103039
- Product name
- N-[(2R,4S)-1-[3,5-Bis(trifluoromethyl)benzoyl]-2-[(4-chlorophenyl)methyl]-4-piperidinyl]-4-quinolinecarboxamide
- Packaging
- 1mg
- Price
- $95
- Updated
- 2021/12/16
- Product number
- FN103039
- Product name
- N-[(2R,4S)-1-[3,5-Bis(trifluoromethyl)benzoyl]-2-[(4-chlorophenyl)methyl]-4-piperidinyl]-4-quinolinecarboxamide
- Packaging
- 2mg
- Price
- $150
- Updated
- 2021/12/16
- Product number
- FN103039
- Product name
- N-[(2R,4S)-1-[3,5-Bis(trifluoromethyl)benzoyl]-2-[(4-chlorophenyl)methyl]-4-piperidinyl]-4-quinolinecarboxamide
- Packaging
- 5mg
- Price
- $250
- Updated
- 2021/12/16
- Product number
- CS-1077
- Product name
- NKP608
- Purity
- 99.89%
- Packaging
- 5mg
- Price
- $317
- Updated
- 2021/12/16
- Product number
- FN103039
- Product name
- N-[(2R,4S)-1-[3,5-Bis(trifluoromethyl)benzoyl]-2-[(4-chlorophenyl)methyl]-4-piperidinyl]-4-quinolinecarboxamide
- Packaging
- 10mg
- Price
- $370
- Updated
- 2021/12/16
(2R,4S)-N-[1-[3,5-Bis(trifluoromethyl)benzoyl]-2-(4-chlorobenzyl)piperidin-4-yl]quinoline-4-carboxamide Chemical Properties,Usage,Production
Uses
NKP608 is a non-peptidic derivative of 4-aminopiperidine which acts as a selective, specific and potent antagonist at the neurokinin-1 (NK-1) receptor both in vitro(IC50=2.6 nM) and in vivo. IC50 value: 2.6 nM Target: NK-1 receptor In vitro, the binding of NKP608 to bovine retina was characterized by an IC50 of 2.6+/-0.4 nM, whereas the compound's affinity to other receptor binding sites, including NK-2 and NK-3, was much lower. Species differences in IC(50) values with NKP608 were less pronounced than with previously described NK-1 receptor antagonists, being 13+/-2 and 27+/-2 nM in gerbil midbrain and rat striatum, respectively. In vivo, using the hind foot thumping model in gerbils, NKP608 exhibited a potent NK-1 antagonistic activity following oral administration (ID(50)=0.23 mg/kg; 2 h pretreatment), supporting a central activity of NKP608. NKP608 may prove a useful anxiolytic compound.
References
[1] El-Hashim AZ, Wyss D, Lewis C. Effect of a novel NK1 receptor selective antagonist (NKP608) on citric acid induced cough and airway obstruction. Pulm Pharmacol Ther. 2004;17(1):11-8. DOI:10.1016/j.pupt.2003.08.002
[2] Vendruscolo LF, Takahashi RN, Brüske GR, Ramos A. Evaluation of the anxiolytic-like effect of NKP608, a NK1-receptor antagonist, in two rat strains that differ in anxiety-related behaviors. Psychopharmacology (Berl). 2003 Nov;170(3):287-93. DOI:10.1007/s00213-003-1545-4
[3] Rupniak NM, Carlson EJ, Shepheard S, et al. Comparison of the functional blockade of rat substance P (NK1) receptors by GR205171, RP67580, SR140333 and NKP-608. Neuropharmacology. 2003 Aug;45(2):231-41. DOI:10.1016/s0028-3908(03)00157-6
[4] Gentsch C, Cutler M, Vassout A, et al. Anxiolytic effect of NKP608, a NK1-receptor antagonist, in the social investigation test in gerbils. Behav Brain Res. 2002 Jul 18;133(2):363-8. DOI:10.1016/s0166-4328(02)00024-4
[5] Vassout A, Veenstra S, Hauser K, et al. NKP608: a selective NK-1 receptor antagonist with anxiolytic-like effects in the social interaction and social exploration test in rats. Regul Pept. 2000 Dec 22;96(1-2):7-16. DOI:10.1016/s0167-0115(00)00194-4
(2R,4S)-N-[1-[3,5-Bis(trifluoromethyl)benzoyl]-2-(4-chlorobenzyl)piperidin-4-yl]quinoline-4-carboxamide Preparation Products And Raw materials
Raw materials
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