LY-78335 | CAS# 39959-66-5 | PNMT inhibitor

MedKoo Cat#: 574775 | Name: LY-78335

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Description:

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

LY-78335 is an inhibitor of phenylethanolamine-N-methyltransferase (PNMT) that suppresses the release of growth hormone in an in vivo rat model.

Chemical Structure

LY-78335

CAS# 39959-66-5

Theoretical Analysis

MedKoo Cat#: 574775

Name: LY-78335

CAS#: 39959-66-5

Chemical Formula: C8H10Cl3N

Exact Mass: 224.9879

Molecular Weight: 226.53

Elemental Analysis: C, 42.42; H, 4.45; Cl, 46.95; N, 6.18

Price and Availability

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

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Related CAS #

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Synonym

LY-78335; LY 78335; LY78335

IUPAC/Chemical Name

2,3-Dichloro-α-methylbenzylamine hydrochloride

InChi Key

FQTXPVLCCDQRHY-UHFFFAOYSA-N

InChi Code

InChI=1S/C8H9Cl2N.ClH/c1-5(11)6-3-2-4-7(9)8(6)10;/h2-5H,11H2,1H3;1H

SMILES Code

NC(C)C1=CC=CC(Cl)=C1Cl.[H]Cl

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

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

1-(2,3-Dichlorophenyl)ethanamine hydrochloride (DCMB) is a phenylethanolamine N-methyltransferase (PNMT) inhibitor.

In vitro activity:

Human hepatic microsomal TMT was inhibited by the arylalkylamine 2,3-dichloro-alpha-methylbenzylamine (DCMB), and by a series of arylalkylamines, as well as the arylamine, aniline. Kis and Kii values were, respectively, 1.1 and 0.29 microM for DCMB, 160 microM each for benzylamine, 680 and 370 microM for aniline, 1640 and 1380 microM for phenylethylamine, and 2300 and 1400 microM for phenylethanolamine. Reference: Xenobiotica. 1993 Jun;23(6):657-69. https://pubmed.ncbi.nlm.nih.gov/8212739/

In vivo activity:

In the present investigation, central nervous system (CNS) EPI biosynthesis was selectively interrupted with the specific norepinephrine N-methyltransferase inhibitors, SK & F 64139 (Smith, Kline & French Laboratories) and LY 78335, (Eli Lilly & Co. Research Laboratories) and the effects of central EPI depletion on episodic GH secretion in the chronically cannulated rat model were determined. Administration of LY 78335 produced similar effects on pulsatile GH. Morphine-induced, but not clonidine-induced, GH release also was blocked by SK & F 64139. Reference: J Clin Invest. 1982 Jan;69(1):104-12. https://pubmed.ncbi.nlm.nih.gov/7054231/

Preparing Stock Solutions

The following data is based on the product molecular weight 226.53 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. Glauser TA, Saks E, Vasova VM, Weinshilboum RM. Human liver microsomal thiol methyltransferase: inhibition by arylalkylamines. Xenobiotica. 1993 Jun;23(6):657-69. doi: 10.3109/00498259309059403. Erratum in: Xenobiotica 1993 Dec;23(12):1451. PMID: 8212739. 2. Matta S, Singh J, Newton R, Sharp BM. The adrenocorticotropin response to interleukin-1 beta instilled into the rat median eminence depends on the local release of catecholamines. Endocrinology. 1990 Nov;127(5):2175-82. doi: 10.1210/endo-127-5-2175. PMID: 2171909. 3. Mefford IN, Lister RG, Ota M, Linnoila M. Antagonism of ethanol intoxication in rats by inhibitors of phenylethanolamine N-methyltransferase. Alcohol Clin Exp Res. 1990 Feb;14(1):53-7. doi: 10.1111/j.1530-0277.1990.tb00446.x. PMID: 2178473. 4. Terry LC, Crowley WR, Johnson MD. Regulation of episodic growth hormone secretion by the central epinephrine system. Studies in the chronically cannulated rat. J Clin Invest. 1982 Jan;69(1):104-12. doi: 10.1172/jci110420. PMID: 7054231; PMCID: PMC371173.

In vitro protocol:

In vivo protocol:

1. Mefford IN, Lister RG, Ota M, Linnoila M. Antagonism of ethanol intoxication in rats by inhibitors of phenylethanolamine N-methyltransferase. Alcohol Clin Exp Res. 1990 Feb;14(1):53-7. doi: 10.1111/j.1530-0277.1990.tb00446.x. PMID: 2178473. 2. Terry LC, Crowley WR, Johnson MD. Regulation of episodic growth hormone secretion by the central epinephrine system. Studies in the chronically cannulated rat. J Clin Invest. 1982 Jan;69(1):104-12. doi: 10.1172/jci110420. PMID: 7054231; PMCID: PMC371173.

1. Fuller et al (1973) Inhibition of phenylethanolamine N-methyltransferase by benzylamines. 2. In vitro and in vivo studies with 2,3-dichloro-α-methylbenzylamine. J.Med.Chem. 16 106 PMID: 4683104 2. Terry et al (1982) Regulation of episodic GH secretion by the central epinephrine system. J.Clin.Invest. 69 104 PMID: 7054231 3. Grunewald et al (1988) Synthesis and evaluation of 3-substituted analogues of 1,2,3,4-tetrahydroisoquinoline as inhibitors of phenylethanolamine N-methyltransferase. J.Med.Chem. 31 824 PMID: 3351861