L-732138 | CAS# 148451-96-1 | NK1 Antagonist

MedKoo Cat#: 564561 | Name: L-732138

Featured

Description:

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

L-732138 is an NK1 receptor antagonist.

Chemical Structure

L-732138

CAS#148451-96-1

Theoretical Analysis

MedKoo Cat#: 564561

Name: L-732138

CAS#: 148451-96-1

Chemical Formula: C22H18F6N2O3

Exact Mass: 472.1222

Molecular Weight: 472.39

Elemental Analysis: C, 55.94; H, 3.84; F, 24.13; N, 5.93; O, 10.16

Price and Availability

Size	Price	Availability
50mg	USD 350.00	2 Weeks
100mg	USD 650.00	2 Weeks
250mg	USD 1,250.00	2 Weeks

Bulk Inquiry

Buy Now

Add to Cart

Related CAS #

No Data

Synonym

3,5-bis(TFM)Bz NAcTrp; L732138; L 732138; L-732138; L-732, 138

IUPAC/Chemical Name

[3,5-Bis(trifluoromethyl)phenyl]methyl (2S)-2-acetamido-3-(1H-indol-3-yl)propanoate

InChi Key

BYYQYXVAWXAYQC-IBGZPJMESA-N

InChi Code

InChI=1S/C22H18F6N2O3/c1-12(31)30-19(8-14-10-29-18-5-3-2-4-17(14)18)20(32)33-11-13-6-15(21(23,24)25)9-16(7-13)22(26,27)28/h2-7,9-10,19,29H,8,11H2,1H3,(H,30,31)/t19-/m0/s1

SMILES Code

O=C(OCC1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)[C@@H](NC(C)=O)CC2=CNC3=C2C=CC=C3

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

Product Data

Product Data

Instruction

View handling instruction

Biological target:

L-732138 is a selective, potent and competitive neurokinin-1 (NK-1) receptor antagonist with an IC50 of 2.3 nM.

In vitro activity:

L-732,138 elicits cell growth inhibition in a concentration dependent manner in the melanoma cells studied. Moreover, L-732,138 blocks SP mitogen stimulation. The specific antitumor action of L-732,138 occurred through the NK-1 receptor and melanoma cell death was by apoptosis. Reference: Cancers (Basel). 2010 Apr 20;2(2):611-23. https://pubmed.ncbi.nlm.nih.gov/24281084/

In vivo activity:

L-732,138 (5-200 nmol) administered i.t. prior to and for 3 consecutive days post-surgery attenuated the mechanical allodynia and cold hyperalgesia on days 4 and 8 post-surgery. The effects of i.t. L-732,138 were also determined in rats with established nerve injury-induced neuropathy. Reference: Pain. 2002 Feb;95(3):277-285. https://pubmed.ncbi.nlm.nih.gov/11839427/

	Solvent	mg/mL	mM
Solubility
	DMF	30.0	63.51
	DMSO	105.3	222.93
	Ethanol	57.1	120.83

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 472.39 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. Muñoz M, Rosso M, González-Ortega A, Coveñas R. The NK-1 Receptor Antagonist L-732,138 Induces Apoptosis and Counteracts Substance P-Related Mitogenesis in Human Melanoma Cell Lines. Cancers (Basel). 2010 Apr 20;2(2):611-23. doi: 10.3390/cancers2020611. PMID: 24281084; PMCID: PMC3835094. 2. Cascieri MA, Macleod AM, Underwood D, Shiao LL, Ber E, Sadowski S, Yu H, Merchant KJ, Swain CJ, Strader CD, et al. Characterization of the interaction of N-acyl-L-tryptophan benzyl ester neurokinin antagonists with the human neurokinin-1 receptor. J Biol Chem. 1994 Mar 4;269(9):6587-91. PMID: 7509807. 3. Cahill CM, Coderre TJ. Attenuation of hyperalgesia in a rat model of neuropathic pain after intrathecal pre- or post-treatment with a neurokinin-1 antagonist. Pain. 2002 Feb;95(3):277-285. doi: 10.1016/S0304-3959(01)00410-9. PMID: 11839427. 4. Kuo HP, Hwang KH, Lin HC, Wang CH, Liu CY, Lu LC. Lipopolysaccharide enhances neurogenic plasma exudation in guinea-pig airways. Br J Pharmacol. 1998 Oct;125(4):711-6. doi: 10.1038/sj.bjp.0702138. PMID: 9831906; PMCID: PMC1571012.

In vitro protocol:

In vivo protocol:

1. Cahill CM, Coderre TJ. Attenuation of hyperalgesia in a rat model of neuropathic pain after intrathecal pre- or post-treatment with a neurokinin-1 antagonist. Pain. 2002 Feb;95(3):277-285. doi: 10.1016/S0304-3959(01)00410-9. PMID: 11839427. 2. Kuo HP, Hwang KH, Lin HC, Wang CH, Liu CY, Lu LC. Lipopolysaccharide enhances neurogenic plasma exudation in guinea-pig airways. Br J Pharmacol. 1998 Oct;125(4):711-6. doi: 10.1038/sj.bjp.0702138. PMID: 9831906; PMCID: PMC1571012.

1: Molinos-Quintana A, Trujillo-Hacha P, Piruat JI, Bejarano-García JA, García-Guerrero E, Pérez-Simón JA, Muñoz M. Human acute myeloid leukemia cells express Neurokinin-1 receptor, which is involved in the antileukemic effect of Neurokinin-1 receptor antagonists. Invest New Drugs. 2018 May 2. doi: 10.1007/s10637-018-0607-8. [Epub ahead of print] PubMed PMID: 29721755. 2: Muñoz M, Rosso M, Coveñas R. The NK-1 receptor antagonist L-732,138 induces apoptosis in human gastrointestinal cancer cell lines. Pharmacol Rep. 2017 Aug;69(4):696-701. doi: 10.1016/j.pharep.2017.02.002. Epub 2017 Feb 12. PubMed PMID: 28550801. 3: Onaga T, Oh-ishi T, Shimoda T, Nishimoto S, Hayashi H. Role of tachykinin and neurokinin receptors in the regulation of ovine omasal contractions. Regul Pept. 2012 Jan 10;173(1-3):64-73. doi: 10.1016/j.regpep.2011.09.007. Epub 2011 Oct 3. PubMed PMID: 21971117.