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MedKoo Cat#: 526803 | Name: NKP-608
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

NKP-608 is a potent antagonist at the neurokinin-1 (NK-1) receptor both in vitro(IC50=2.6 nM). NKP608 has an anxiolytic action in the social interaction test in rats. NKP-608 inhibits substance P (SP)-induced airway plasma protein exudation in vivo.

Chemical Structure

NKP-608
CAS#177707-12-9

Theoretical Analysis

MedKoo Cat#: 526803

Name: NKP-608

CAS#: 177707-12-9

Chemical Formula: C31H24ClF6N3O2

Exact Mass: 619.1461

Molecular Weight: 619.99

Elemental Analysis: C, 60.06; H, 3.90; Cl, 5.72; F, 18.39; N, 6.78; O, 5.16

Price and Availability

Size Price Availability Quantity
10mg USD 475.00 2 Weeks
50mg USD 1,295.00 2 Weeks
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Related CAS #
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Synonym
NKP-608; NKP 608; NKP608; AV-608; nk 608
IUPAC/Chemical Name
N-[(2R,4S)-1-[3,5-bis(trifluoromethyl)benzoyl]-2-[(4-chlorophenyl)methyl]piperidin-4-yl]quinoline-4-carboxamide
InChi Key
NXLUTEDAEFXMQR-BJKOFHAPSA-N
InChi Code
InChI=1S/C31H24ClF6N3O2/c32-22-7-5-18(6-8-22)13-24-17-23(40-28(42)26-9-11-39-27-4-2-1-3-25(26)27)10-12-41(24)29(43)19-14-20(30(33,34)35)16-21(15-19)31(36,37)38/h1-9,11,14-16,23-24H,10,12-13,17H2,(H,40,42)/t23-,24+/m0/s1
SMILES Code
O=C(C1=CC=NC2=CC=CC=C12)N[C@@H]3C[C@@H](CC4=CC=C(Cl)C=C4)N(C(C5=CC(C(F)(F)F)=CC(C(F)(F)F)=C5)=O)CC3
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
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.
In vitro activity:
This study found that NKP608 inhibited the proliferation, migration/invasion of HCT116 cells. In addition, NKP608 reduced expressions of Wnt-3a, β-catenin, Cyclin D1, and (vascular endothelial growth factor) VEGF while induced expression of E-Cadherin. Furthermore, flow cytometry analyzed that NKP608 induced apoptosis of HCT116 cells, consistently, western blotting detecting of apoptosis-related proteins revealed that NKP608 downregulated Bcl-2 while upregulated Bax and Active-Caspase-3. Reference: Biol Res. 2018 May 30;51(1):14. https://pubmed.ncbi.nlm.nih.gov/29843798/
In vivo activity:
Guinea pigs pre-treated with 0.03, 0.3 and 1mgkg(-1) of NKP608 exhibited a significant reduction of 77, 74 and 79%, respectively, in the numbers of cough compared to vehicle pre-treated animals (P<0.05). SR48968, 10 mg kg(-1), alone did not significantly affect the citric acid-induced cough but when co-administered with 1 mg kg(-1) of NKP608, there was a significant 90% reduction in cough. Reference: Pulm Pharmacol Ther. 2004;17(1):11-8. https://pubmed.ncbi.nlm.nih.gov/14643166/
Solvent mg/mL mM comments
Solubility
DMSO 100.0 161.29
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 619.99 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Niu XL, Hou JF, Li JX. The NK1 receptor antagonist NKP608 inhibits proliferation of human colorectal cancer cells via Wnt signaling pathway. Biol Res. 2018 May 30;51(1):14. doi: 10.1186/s40659-018-0163-x. PMID: 29843798; PMCID: PMC5975706. 2. 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. PMID: 14643166. 3. 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):287-293. doi: 10.1007/s00213-003-1545-4. Epub 2003 Aug 12. PMID: 12915956.
In vitro protocol:
1. Niu XL, Hou JF, Li JX. The NK1 receptor antagonist NKP608 inhibits proliferation of human colorectal cancer cells via Wnt signaling pathway. Biol Res. 2018 May 30;51(1):14. doi: 10.1186/s40659-018-0163-x. PMID: 29843798; PMCID: PMC5975706.
In vivo protocol:
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. PMID: 14643166. 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):287-293. doi: 10.1007/s00213-003-1545-4. Epub 2003 Aug 12. PMID: 12915956.
1: Griffante C, Carletti R, Andreetta F, Corsi M. [3H]GR205171 displays similar NK1 receptor binding profile in gerbil and human brain. Br J Pharmacol. 2006 May;148(1):39-45. PubMed PMID: 16501582; PubMed Central PMCID: PMC1617048. 2: Rodgers RJ, Gentsch C, Hoyer D, Bryant E, Green AJ, Kolokotroni KZ, Martin JL. The NK1 receptor antagonist NKP608 lacks anxiolytic-like activity in Swiss-Webster mice exposed to the elevated plus-maze. Behav Brain Res. 2004 Sep 23;154(1):183-92. PubMed PMID: 15302124. 3: Schmassmann A, Waser B, Flogerzi B, Reubi JC. Expression of functional neurokinin-1 receptors in regenerative glands during gastric wound healing in rodents. Gastroenterology. 2004 Mar;126(3):784-95. PubMed PMID: 14988833. 4: 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. PubMed PMID: 14643166. 5: 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. Epub 2003 Aug 12. PubMed PMID: 12915956. 6: Rupniak NM, Carlson EJ, Shepheard S, Bentley G, Williams AR, Hill A, Swain C, Mills SG, Di Salvo J, Kilburn R, Cascieri MA, Kurtz MM, Tsao KL, Gould SL, Chicchi GG. 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. PubMed PMID: 12842129. 7: Coulson FR, Bigg CS, O'Donnell SR. Antagonism by NKP608 of substance P-induced plasma protein exudation in a novel preparation of perfused trachea in rats and guinea-pigs in vivo. Inflamm Res. 2002 Jul;51(7):317-23. PubMed PMID: 12146722. 8: Gentsch C, Cutler M, Vassout A, Veenstra S, Brugger F. 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. PubMed PMID: 12110470. 9: Spooren WP, Schoeffter P, Gasparini F, Kuhn R, Gentsch C. Pharmacological and endocrinological characterisation of stress-induced hyperthermia in singly housed mice using classical and candidate anxiolytics (LY314582, MPEP and NKP608). Eur J Pharmacol. 2002 Jan 25;435(2-3):161-70. PubMed PMID: 11821022. 10: Vassout A, Veenstra S, Hauser K, Ofner S, Brugger F, Schilling W, Gentsch C. 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. PubMed PMID: 11102646. 11: File SE. NKP608, an NK1 receptor antagonist, has an anxiolytic action in the social interaction test in rats. Psychopharmacology (Berl). 2000 Sep;152(1):105-9. PubMed PMID: 11041322. 12: Papp M, Vassout A, Gentsch C. The NK1-receptor antagonist NKP608 has an antidepressant-like effect in the chronic mild stress model of depression in rats. Behav Brain Res. 2000 Oct;115(1):19-23. PubMed PMID: 10996404. 1: Griffante C, Carletti R, Andreetta F, Corsi M. [3H]GR205171 displays similar NK1 receptor binding profile in gerbil and human brain. Br J Pharmacol. 2006 May;148(1):39-45. PubMed PMID: 16501582; PubMed Central PMCID: PMC1617048. 2: Rodgers RJ, Gentsch C, Hoyer D, Bryant E, Green AJ, Kolokotroni KZ, Martin JL. The NK1 receptor antagonist NKP608 lacks anxiolytic-like activity in Swiss-Webster mice exposed to the elevated plus-maze. Behav Brain Res. 2004 Sep 23;154(1):183-92. PubMed PMID: 15302124. 3: Schmassmann A, Waser B, Flogerzi B, Reubi JC. Expression of functional neurokinin-1 receptors in regenerative glands during gastric wound healing in rodents. Gastroenterology. 2004 Mar;126(3):784-95. PubMed PMID: 14988833. 4: 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. PubMed PMID: 14643166. 5: 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. Epub 2003 Aug 12. PubMed PMID: 12915956. 6: Rupniak NM, Carlson EJ, Shepheard S, Bentley G, Williams AR, Hill A, Swain C, Mills SG, Di Salvo J, Kilburn R, Cascieri MA, Kurtz MM, Tsao KL, Gould SL, Chicchi GG. 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. PubMed PMID: 12842129. 7: Coulson FR, Bigg CS, O'Donnell SR. Antagonism by NKP608 of substance P-induced plasma protein exudation in a novel preparation of perfused trachea in rats and guinea-pigs in vivo. Inflamm Res. 2002 Jul;51(7):317-23. PubMed PMID: 12146722. 8: Gentsch C, Cutler M, Vassout A, Veenstra S, Brugger F. 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. PubMed PMID: 12110470. 9: Spooren WP, Schoeffter P, Gasparini F, Kuhn R, Gentsch C. Pharmacological and endocrinological characterisation of stress-induced hyperthermia in singly housed mice using classical and candidate anxiolytics (LY314582, MPEP and NKP608). Eur J Pharmacol. 2002 Jan 25;435(2-3):161-70. PubMed PMID: 11821022. 10: Vassout A, Veenstra S, Hauser K, Ofner S, Brugger F, Schilling W, Gentsch C. 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. PubMed PMID: 11102646. 11: File SE. NKP608, an NK1 receptor antagonist, has an anxiolytic action in the social interaction test in rats. Psychopharmacology (Berl). 2000 Sep;152(1):105-9. PubMed PMID: 11041322. 12: Papp M, Vassout A, Gentsch C. The NK1-receptor antagonist NKP608 has an antidepressant-like effect in the chronic mild stress model of depression in rats. Behav Brain Res. 2000 Oct;115(1):19-23. PubMed PMID: 10996404.

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BN 50726

BN 50726