L 659,877 | CAS#125989-12-0 | neurokinin-2 receptor antagonist

MedKoo Cat#: 596610 | Name: L 659,877

Description:

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

L 659,877 is a Tachykinin and neurokinin-2 receptor antagonist.

Chemical Structure

L 659,877

CAS#125989-12-0

Theoretical Analysis

MedKoo Cat#: 596610

Name: L 659,877

CAS#: 125989-12-0

Chemical Formula: C38H50N8O7S

Exact Mass: 762.3523

Molecular Weight: 762.92

Elemental Analysis: C, 59.82; H, 6.61; N, 14.69; O, 14.68; S, 4.20

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

L 659,877; L-659,877; L659,877; L-659877; L 659877; L659877; Cyclo(Gln-Trp-Phe-Gly-Leu-Met);

IUPAC/Chemical Name

3-((2S,5S,8S,14S,17S)-5-((1H-indol-3-yl)methyl)-8-benzyl-14-isobutyl-17-(2-(methylthio)ethyl)-3,6,9,12,15,18-hexaoxo-1,4,7,10,13,16-hexaazacyclooctadecan-2-yl)propanamide

InChi Key

HOUZPIDCIQWWLS-FGHIVKBXSA-N

InChi Code

1S/C38H50N8O7S/c1-22(2)17-29-37(52)44-28(15-16-54-3)36(51)43-27(13-14-32(39)47)35(50)46-31(19-24-20-40-26-12-8-7-11-25(24)26)38(53)45-30(18-23-9-5-4-6-10-23)34(49)41-21-33(48)42-29/h4-12,20,22,27-31,40H,13-19,21H2,1-3H3,(H2,39,47)(H,41,49)(H,42,48)(H,43,51)(H,44,52)(H,45,53)(H,46,50)/t27-,28-,29-,30-,31?/m0/s1

SMILES Code

O=C([C@H](CCC(N)=O)NC([C@H](CCSC)NC([C@H](CC(C)C)NC(CNC1=O)=O)=O)=O)N[C@@H](Cc(c[nH]2)c3c2cccc3)C(N[C@H]1Cc4ccccc4)=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

>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

Preparing Stock Solutions

The following data is based on the product molecular weight 762.92 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: Chen X, Yu L, Steill JD, Oomens J, Polfer NC. Effect of peptide fragment size on the propensity of cyclization in collision-induced dissociation: oligoglycine b(2)-b(8). J Am Chem Soc. 2009 Dec 30;131(51):18272-82. doi: 10.1021/ja9030837. PubMed PMID: 19947633. 2: Li H, Bao Y, Zhao Z. Expression of tachykinin receptors inXenopus oocytes injected with poly (A)(+) RNA from cat dorsal root ganglion. Sci China C Life Sci. 1998 Apr;41(2):139-45. doi: 10.1007/BF02882718. PubMed PMID: 18726197. 3: Minowa S, Tsuchiya S, Someya A, Horie S, Murayama T. Role of neuropeptide receptor systems in vanilloid VR1 receptor-mediated gastric acid secretion in rat brain. Eur J Pharmacol. 2004 Feb 23;486(3):317-24. PubMed PMID: 14985054. 4: Gaspar MN, Ribeiro CA, Cunha-Vaz JG, Macedo TR. Effects of neuropeptides on the sumatriptan-disturbed circulation in the optic nerve head of rabbits. Pharmacology. 2004 Mar;70(3):152-9. PubMed PMID: 14752235. 5: Barrios VE, Jarosinski MA, Wright CD. Proteinase-activated receptor-2 mediates hyperresponsiveness in isolated guinea pig bronchi. Biochem Pharmacol. 2003 Aug 1;66(3):519-25. PubMed PMID: 12907252. 6: Andoh T, Kuraishi Y. Nitric oxide enhances substance P-induced itch-associated responses in mice. Br J Pharmacol. 2003 Jan;138(1):202-8. PubMed PMID: 12522091; PubMed Central PMCID: PMC1573631. 7: Wang DS, Xu TL, Li JS. Modulation of glycine-activated chloride currents by substance P in rat sacral dorsal commissural neurons. Sheng Li Xue Bao. 1999 Aug;51(4):361-70. PubMed PMID: 11498962. 8: Tao YX, Zhao ZQ. [Neurokinin-1 receptor mediated formalin-induced c-fos expression in the rat spinal cord]. Sheng Li Xue Bao. 1998 Aug;50(4):361-6. Chinese. PubMed PMID: 11324543. 9: Mustafa S, Oriowo MA. Inhibitory effect of capsaicin on cholinergic transmission in ovine airways: evidence for non-cholinergic contractions. Eur J Pharmacol. 1999 Dec 3;385(2-3):203-8. PubMed PMID: 10607877. 10: Pisera D, Theas S, De Laurentiis A, Lasaga M, Duvilanski B, Seilicovich A. The hormonal status modulates the effect of neurokinin A on prolactin secretion in female rats. J Endocrinol. 1998 Dec;159(3):389-95. PubMed PMID: 9834456. 11: Li HS, Zhao ZQ. Small sensory neurons in the rat dorsal root ganglia express functional NK-1 tachykinin receptor. Eur J Neurosci. 1998 Apr;10(4):1292-9. PubMed PMID: 9749783. 12: Andoh T, Nagasawa T, Satoh M, Kuraishi Y. Substance P induction of itch-associated response mediated by cutaneous NK1 tachykinin receptors in mice. J Pharmacol Exp Ther. 1998 Sep;286(3):1140-5. PubMed PMID: 9732370. 13: Meade CJ. The mechanism by which epinastine stops an adenosine analog from contracting BDE rat airways. Am J Respir Crit Care Med. 1998 Feb;157(2):522-30. PubMed PMID: 9476868. 14: Matsumoto S, Takeda M, Saiki C, Takahashi T, Ojima K. Effects of tachykinins on rapidly adapting pulmonary stretch receptors and total lung resistance in anesthetized, artificially ventilated rabbits. J Pharmacol Exp Ther. 1997 Dec;283(3):1026-31. PubMed PMID: 9399972. 15: Sarosi GA Jr, Kimball BC, Barnhart DC, Zhang W, Mulholland MW. Tachykinin neuropeptide-evoked intracellular calcium transients in cultured guinea pig myenteric neurons. Peptides. 1998;19(1):75-84. PubMed PMID: 9437739. 16: Ko FN, Huang SY, Teng CM. Activation by high potassium of a novel voltage-operated Ca2+ channel in rat spleen. Br J Pharmacol. 1997 Feb;120(4):565-70. PubMed PMID: 9051291; PubMed Central PMCID: PMC1564497. 17: Parlani M, Conte B, Cirillo R, Manzini S. Characterization of tachykinin NK2 receptor on dog proximal colon. Antagonism by MEN 10,627 and SR 48,968. Eur J Pharmacol. 1996 Dec 30;318(2-3):419-24. PubMed PMID: 9016933. 18: Meade CJ, Mierau J, Leon I, Ensinger HA. In vivo role of the adenosine A3 receptor: N6-2-(4-aminophenyl)ethyladenosine induces bronchospasm in BDE rats by a neurally mediated mechanism involving cells resembling mast cells. J Pharmacol Exp Ther. 1996 Dec;279(3):1148-56. PubMed PMID: 8968336. 19: Ukai M, Shinkai N, Kameyama T. Neurokinin A and senktide attenuate scopolamine-induced impairment of spontaneous alternation performance in mice. Nihon Shinkei Seishin Yakurigaku Zasshi. 1996 Jun;16(3):97-101. PubMed PMID: 8905797. 20: Mizuta A, Takano Y, Honda K, Saito R, Matsumoto T, Kamiya H. Nitric oxide is a mediator of tachykinin NK3 receptor-induced relaxation in rat mesenteric artery. Br J Pharmacol. 1995 Dec;116(7):2919-22. PubMed PMID: 8680725; PubMed Central PMCID: PMC1909215.