L-703606 Oxalate | CAS#144425-84-3 |NK1 receptor Antagonist

MedKoo Cat#: 532069 | Name: L-703606 Oxalate

Description:

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

L-703,606 is a potent, selective antagonist to the human NK1 receptor.

Chemical Structure

L-703606 Oxalate

CAS#144425-84-3 (Oxalate)

Theoretical Analysis

MedKoo Cat#: 532069

Name: L-703606 Oxalate

CAS#: 144425-84-3 (Oxalate)

Chemical Formula: C29H31IN2O4

Exact Mass: 508.1375

Molecular Weight: 598.48

Elemental Analysis: C, 58.20; H, 5.22; I, 21.20; N, 4.68; O, 10.69

Price and Availability

Size	Price	Availability	Quantity

Bulk Inquiry

Buy Now

Add to Cart

Related CAS #

144425-84-3 (Oxalate) 351351-06-9 (Oxalate hydrate) 144425-84-3

Synonym

L-703,606; L 703,606; L703,606; L-703606; L 703606; L703606; L-703606 Oxalate

IUPAC/Chemical Name

(7R,8R)-7-[di(phenyl)methyl]-N-[(2-iodophenyl)methyl]-1-azabicyclo[2.2.2]octan-8-amine oxalate

InChi Key

VHLWXEPQCNQPNC-CNZCJKERSA-N

InChi Code

InChI=1S/C27H29IN2.C2H2O4/c28-24-14-8-7-13-23(24)19-29-26-22-15-17-30(18-16-22)27(26)25(20-9-3-1-4-10-20)21-11-5-2-6-12-21;3-1(4)2(5)6/h1-14,22,25-27,29H,15-19H2;(H,3,4)(H,5,6)/t26-,27-;/m1./s1

SMILES Code

IC1=CC=CC=C1CN[C@H]2[C@@H](C(C3=CC=CC=C3)C4=CC=CC=C4)N5CCC2CC5.O=C(O)C(O)=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

Product Data

Product Data

Instruction

View handling instruction

Biological target:

L-703,606 is a potent, selective antagonist to the human NK1 receptor.

In vitro activity:

Moreover, NK-1 receptor antagonist L-703,606 blocked the SP-induced stimulation of proliferation. The results of Western blot analysis showed that L-703,606 attenuated the effects of substance P on NK1R, GSK-3β, and β-catenin expression. Reference: Front Neurosci. 2018 Nov 5;12:806. https://pubmed.ncbi.nlm.nih.gov/30455626/

In vivo activity:

Topical treatment of guinea pigs with L-703,606, either before histamine application or at the time of peak ORI (ocular redness index), effectively reduced ORI and suppressed conjunctival blood vessel dilation, along with decreased eosinophil and neutrophil infiltration, and inflammatory cytokine expression in the conjunctiva, as well as reduced SP levels in the tears. Reference: Ocul Surf. 2022 Oct;26:184-190. https://pubmed.ncbi.nlm.nih.gov/36067981/

Preparing Stock Solutions

The following data is based on the product molecular weight 598.48 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:

1. Zhang N, Gao D, Liu Y, Ji S, Sha L. Effects of Neuropeptide Substance P on Proliferation and β-Cell Differentiation of Adult Pancreatic Ductal Cells. Front Neurosci. 2018 Nov 5;12:806. doi: 10.3389/fnins.2018.00806. PMID: 30455626; PMCID: PMC6230717. 2. Masterson SP, Li J, Bickford ME. Frequency-dependent release of substance P mediates heterosynaptic potentiation of glutamatergic synaptic responses in the rat visual thalamus. J Neurophysiol. 2010 Sep;104(3):1758-67. doi: 10.1152/jn.00010.2010. Epub 2010 Jul 21. PMID: 20660425; PMCID: PMC2944677. 3. Wang S, Liu L, Blanco T, Ge H, Xia Y, Pang K, Chen Y, Dana R. Therapeutic efficacy of topical blockade of substance P in experimental allergic red eye. Ocul Surf. 2022 Oct;26:184-190. doi: 10.1016/j.jtos.2022.08.008. Epub 2022 Sep 5. PMID: 36067981. 4. Huang H, Zhang X, Fu X, Zhang X, Lang B, Xiang X, Hao W. Alcohol-induced conditioned place preference negatively correlates with anxiety-like behavior in adolescent mice: inhibition by a neurokinin-1 receptor antagonist. Psychopharmacology (Berl). 2018 Oct;235(10):2847-2857. doi: 10.1007/s00213-018-4976-7. Epub 2018 Jul 27. PMID: 30054674.

In vitro protocol:

In vivo protocol:

1. Wang S, Liu L, Blanco T, Ge H, Xia Y, Pang K, Chen Y, Dana R. Therapeutic efficacy of topical blockade of substance P in experimental allergic red eye. Ocul Surf. 2022 Oct;26:184-190. doi: 10.1016/j.jtos.2022.08.008. Epub 2022 Sep 5. PMID: 36067981. 2. Huang H, Zhang X, Fu X, Zhang X, Lang B, Xiang X, Hao W. Alcohol-induced conditioned place preference negatively correlates with anxiety-like behavior in adolescent mice: inhibition by a neurokinin-1 receptor antagonist. Psychopharmacology (Berl). 2018 Oct;235(10):2847-2857. doi: 10.1007/s00213-018-4976-7. Epub 2018 Jul 27. PMID: 30054674.

1: Tao K, Wang HT, Chen B, Wang BT, Li ZY, Zhu XX, Tang CW, Hu DH. Effect of nonpeptide NK1 receptor antagonist L-703,606 on the edema formation in rats at early stage after deep partial-thickness skin scalding. Asian Pac J Trop Med. 2013 May 13;6(5):387-94. doi: 10.1016/S1995-7645(13)60044-9. PubMed PMID: 23608379. 2: Tao K, Chen B, Hu DH, Wang BT. [The influence of non-peptide NK1 receptor antagonist L-703, 606 on the early tissue edema formation in rats with deep partial-thickness scald]. Zhonghua Shao Shang Za Zhi. 2005 Dec;21(6):455-8. Chinese. PubMed PMID: 16480633. 3: Francis BE, Swain C, Sabin V, Burns HD. Radioiodinated L-703,606: a potent, selective antagonist to the human NK1 receptor. Appl Radiat Isot. 1994 Jan;45(1):97-103. PubMed PMID: 8287060.

View History

VU0463841

MedKoo CAT#: 532948

CAS#: 1439095-16-5