FK 224 | CAS#125787-94-2 | Tachykinin receptor antagonist

MedKoo Cat#: 597927 | Name: FK 224

Description:

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

FK 224 is a tachykinin receptor antagonist.

Chemical Structure

FK 224

CAS#125787-94-2

Theoretical Analysis

MedKoo Cat#: 597927

Name: FK 224

CAS#: 125787-94-2

Chemical Formula: C54H72N8O13

Exact Mass: 1040.5219

Molecular Weight: 1041.21

Elemental Analysis: C, 62.29; H, 6.97; N, 10.76; O, 19.98

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

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Related CAS #

No Data

Synonym

FK 224; FK-224; FK224;

IUPAC/Chemical Name

N-((3S,6R,9S,12R,15S,21S,22R)-6-(2-amino-2-oxoethyl)-12-benzyl-18-((Z)-4-hydroxybenzylidene)-9-((S)-1-hydroxyethyl)-3-(hydroxymethyl)-15-isobutyl-19,22-dimethyl-2,5,8,11,14,17,20-heptaoxo-1-oxa-4,7,10,13,16,19-hexaazacyclodocosan-21-yl)-3-(2-pentylphenyl)propanamide

InChi Key

BEWCDVTWUFJSSM-NFHSPJBXSA-N

InChi Code

InChI=1S/C54H72N8O13/c1-7-8-10-17-36-18-13-14-19-37(36)22-25-45(67)60-47-33(5)75-54(74)42(30-63)59-49(69)41(29-44(55)66)58-52(72)46(32(4)64)61-50(70)40(27-34-15-11-9-12-16-34)56-48(68)39(26-31(2)3)57-51(71)43(62(6)53(47)73)28-35-20-23-38(65)24-21-35/h9,11-16,18-21,23-24,28,31-33,39-42,46-47,63-65H,7-8,10,17,22,25-27,29-30H2,1-6H3,(H2,55,66)(H,56,68)(H,57,71)(H,58,72)(H,59,69)(H,60,67)(H,61,70)/b43-28-/t32-,33+,39-,40+,41+,42-,46-,47-/m0/s1

SMILES Code

O[C@@H](C)[C@@H](C(N[C@H](CC(N)=O)C(N[C@H](C(O[C@H](C)[C@H](NC(CCc1ccccc1CCCCC)=O)C(N(C)/C(C(N[C@H](C(N[C@@H]2Cc3ccccc3)=O)CC(C)C)=O)=C\c4ccc(O)cc4)=O)=O)CO)=O)=O)NC2=O

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

>3 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

2934.99.03.00

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 1,041.21 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

1: Morimoto H, Murai M, Maeda Y, Yamaoka M, Nishikawa M, Kiyotoh S, Fujii T. FK 224, a novel cyclopeptide substance P antagonist with NK1 and NK2 receptor selectivity. J Pharmacol Exp Ther. 1992 Jul;262(1):398-402. PubMed PMID: 1378096. 2: Aizawa H, Koto H, Nakano H, Inoue H, Matsumoto K, Takata S, Shigyo M, Hara N. The effects of a specific tachykinin receptor antagonist FK-224 on ozone-induced airway hyperresponsiveness and inflammation. Respirology. 1997 Dec;2(4):261-5. PubMed PMID: 9525295. 3: Schmidt D, Jörres RA, Rabe KF, Magnussen H. Reproducibility of airway response to inhaled bradykinin and effect of the neurokinin receptor antagonist FK-224 in asthmatic subjects. Eur J Clin Pharmacol. 1996;50(4):269-73. PubMed PMID: 8803517. 4: Morimoto H, Yamashita M, Matsuda A, Miyake H, Fujii T. Effects of FR 113680 and FK 224, novel tachykinin receptor antagonists, on cigarette smoke-induced rat tracheal plasma extravasation. Eur J Pharmacol. 1992 Nov 24;224(1):1-5. PubMed PMID: 1280594. 5: Ogawa H, Fujimura M, Saito M, Matsuda T, Akao N, Kondo K. The effect of the neurokinin antagonist FK-224 on the cough response to inhaled capsaicin in a new model of guinea-pig eosinophilic bronchitis induced by intranasal polymyxin B. Clin Auton Res. 1994 Apr;4(1-2):19-28. PubMed PMID: 8054833. 6: Ichinose M, Nakajima N, Takahashi T, Yamauchi H, Inoue H, Takishima T. Protection against bradykinin-induced bronchoconstriction in asthmatic patients by neurokinin receptor antagonist. Lancet. 1992 Nov 21;340(8830):1248-51. PubMed PMID: 1359319. 7: Fujii K, Kohrogi H, Iwagoe H, Hamamoto J, Hirata N, Yamaguchi T, Kawano O, Ando M. Evidence that PGF2 alpha-induced contraction of isolated guinea pig bronchi is mediated in part by release of tachykinins. J Appl Physiol (1985). 1995 Nov;79(5):1411-8. PubMed PMID: 8593995. 8: Morimoto H, Yamashita M, Matsuda A, Ohori M, Miyake H, Fujii T. Characterization of dextran sulfate-induced guinea pig tracheal plasma extravasation. Jpn J Pharmacol. 1996 Nov;72(3):217-21. PubMed PMID: 8957682. 9: Kodjo MK, Leboulenger F, Morra M, Conlon JM, Vaudry H. Pharmacological profile of the tachykinin receptor involved in the stimulation of corticosteroid secretion in the frog Rana ridibunda. J Steroid Biochem Mol Biol. 1996 Mar;57(5-6):329-35. PubMed PMID: 8639469. 10: Hayashi K, Hashimoto M, Shigematsu N, Nishikawa M, Ezaki M, Yamashita M, Kiyoto S, Okuhara M, Kohsaka M, Imanaka H. WS9326A, a novel tachykinin antagonist isolated from Streptomyces violaceusniger no. 9326. I. Taxonomy, fermentation, isolation, physico-chemical properties and biological activities. J Antibiot (Tokyo). 1992 Jul;45(7):1055-63. PubMed PMID: 1381343. 11: Takahashi Y, Nakajima Y, Sakamoto T. Dermatome mapping in the rat hindlimb by electrical stimulation of the spinal nerves. Neurosci Lett. 1994 Feb 28;168(1-2):85-8. Erratum in: Neurosci Lett 1994 Jul 4;175(1-2):175. PubMed PMID: 7518069. 12: Katahashi T, Konno A. Effects of tachykinin receptor antagonists, FK224 and FK888, in a guinea-pig model of nasal allergy. Rhinology. 1997 Jun;35(2):63-6. PubMed PMID: 9299653. 13: Nakate T, Yoshida H, Ohike A, Tokunaga Y, Ibuki R, Kawashima Y. Improvement of pulmonary absorption of cyclopeptide FK224 in rats by co-formulating with beta-cyclodextrin. Eur J Pharm Biopharm. 2003 Mar;55(2):147-54. PubMed PMID: 12637090. 14: Arakawa M, Majima M, Nagai K, Goto F, Katori M. Role of tachykinins in enhancement of bradykinin-induced bronchoconstriction by captopril. Inflamm Res. 1996 Feb;45(2):75-82. PubMed PMID: 8907588. 15: Kiyoto S. [Substance P receptor antagonist]. Tanpakushitsu Kakusan Koso. 1993 Aug;38(11):1841-52. Review. Japanese. PubMed PMID: 7692470. 16: Shioya T, Kagaya M, Sano M, Itaba M, Shindo T, Fujii T, Miura M. Effect of a new dual neurokinin antagonist on airway smooth muscle in situ. Arzneimittelforschung. 1995 Nov;45(11):1194-7. PubMed PMID: 8929238. 17: Xiang A, Uchida Y, Nomura A, Iijima H, Dong F, Zhang MJ, Hasegawa S. Effects of airway inflammation on cough response in the guinea pig. J Appl Physiol (1985). 1998 Nov;85(5):1847-54. PubMed PMID: 9804590. 18: Nishitsuji M, Fujimura M, Oribe Y, Nakao S. A guinea pig model for cough variant asthma and role of tachykinins. Exp Lung Res. 2004 Dec;30(8):723-37. PubMed PMID: 15700549. 19: Bae SJ, Matsunaga Y, Takenaka M, Tanaka Y, Hamazaki Y, Shimizu K, Katayama I. Substance P induced preprotachykinin-a mRNA, neutral endopeptidase mRNA and substance P in cultured normal fibroblasts. Int Arch Allergy Immunol. 2002 Apr;127(4):316-21. PubMed PMID: 12021551. 20: Shirasaki H, Asakura K, Narita S, Watanabe M, Kataura A. The effects of NK1 receptor antagonists (FK224 and FK888) on agonist- and antigen-induced nasal microvascular leakage in guinea pigs. Inflamm Res. 1997 Jan;46(1):28-31. PubMed PMID: 9117514.