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NKP-608
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WARNING: This product is for research use only, not for human or veterinary use.

Hodoodo CAT#: H526803

CAS#: 177707-12-9

Description: 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

Instruction

Theoretical Analysis

Hodoodo Cat#: H526803
Name: NKP-608
CAS#: 177707-12-9
Chemical Formula: C31H24ClF6N3O2
Exact Mass: 619.15
Molecular Weight: 619.992
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
10mg	USD 475	2 Weeks
50mg	USD 1295	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. Hodoodo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: NKP-608; NKP 608; NKP608.

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:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

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.

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:
In vitro protocol:
In vivo protocol:

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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.