JNJ-1661010 | CAS#681136-29-8 | FAAH Inhibitor

MedKoo Cat#: 525305 | Name: JNJ-1661010

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Description:

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

JNJ-1661010 is a selective, reversible inhibitor of fatty acid amide hydrolase (FAAH) (IC50 = 12 nM). JNJ-1661010 is a brain penetrant and active in vivo.

Chemical Structure

JNJ-1661010

CAS#681136-29-8

Theoretical Analysis

MedKoo Cat#: 525305

Name: JNJ-1661010

CAS#: 681136-29-8

Chemical Formula: C19H19N5OS

Exact Mass: 365.1310

Molecular Weight: 365.46

Elemental Analysis: C, 62.44; H, 5.24; N, 19.16; O, 4.38; S, 8.77

Price and Availability

Size	Price	Availability
10mg	USD 285.00	2 Weeks
25mg	USD 550.00	2 Weeks
50mg	USD 850.00	2 Weeks

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Synonym

JNJ-1661010; JNJ 1661010; JNJ1661010.

IUPAC/Chemical Name

1-Piperazinecarboxamide, N-phenyl-4-(3-phenyl-1,2,4-thiadiazol-5-yl)-

InChi Key

BHBOSTKQCZEAJM-UHFFFAOYSA-N

InChi Code

InChI=1S/C19H19N5OS/c25-18(20-16-9-5-2-6-10-16)23-11-13-24(14-12-23)19-21-17(22-26-19)15-7-3-1-4-8-15/h1-10H,11-14H2,(H,20,25)

SMILES Code

O=C(N1CCN(C2=NC(C3=CC=CC=C3)=NS2)CC1)NC4=CC=CC=C4

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

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Product Data

Product Data

Instruction

View handling instruction

Biological target:

JNJ-1661010 (Takeda-25) a potent and selective fatty acid amide hydrolase (FAAH) inhibitor with IC50s of 34 and 33 nM for rat FAAH and human FAAH, respectively.

In vitro activity:

Under these conditions, AEA (at 10−6 M and 10−8 M) and concomitant FAAH inhibition with JNJ1661010 (1 μM) reduced the production of IL-6 and IL-8 by RA but not OA mixed synoviocytes (Fig. 1b, d). Reference: Arthritis Res Ther. 2015 Nov 14;17:321. https://pubmed.ncbi.nlm.nih.gov/26567045/

In vivo activity:

JNJ-1661010 dose-dependently increases arachidonoyl ethanolamide, oleoyl ethanolamide, and palmitoyl ethanolamide in the rat brain. The compound attenuates tactile allodynia in the rat mild thermal injury model of acute tissue damage and in the rat spinal nerve ligation (Chung) model of neuropathic pain. JNJ-1661010 also diminishes thermal hyperalgesia in the inflammatory rat carrageenan paw model. These data suggest that FAAH inhibitors with modes of action similar to JNJ-1661010 may be useful clinically as broad-spectrum analgesics. Reference: Anesth Analg. 2009 Jan;108(1):316-29. https://pubmed.ncbi.nlm.nih.gov/19095868/

	Solvent	mg/mL	mM
Solubility
	DMF	25.0	68.41
	DMF:PBS (pH 7.2) (1:5)	0.2	0.44
	DMSO	48.1	131.72
	Ethanol	2.6	7.05

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 365.46 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. Lowin T, Apitz M, Anders S, Straub RH. Anti-inflammatory effects of N-acylethanolamines in rheumatoid arthritis synovial cells are mediated by TRPV1 and TRPA1 in a COX-2 dependent manner. Arthritis Res Ther. 2015 Nov 14;17:321. doi: 10.1186/s13075-015-0845-5. PMID: 26567045; PMCID: PMC4644337. 2. Karbarz MJ, Luo L, Chang L, Tham CS, Palmer JA, Wilson SJ, Wennerholm ML, Brown SM, Scott BP, Apodaca RL, Keith JM, Wu J, Breitenbucher JG, Chaplan SR, Webb M. Biochemical and biological properties of 4-(3-phenyl-[1,2,4] thiadiazol-5-yl)-piperazine-1-carboxylic acid phenylamide, a mechanism-based inhibitor of fatty acid amide hydrolase. Anesth Analg. 2009 Jan;108(1):316-29. doi: 10.1213/ane.0b013e31818c7cbd. PMID: 19095868.

In vitro protocol:

In vivo protocol:

1: Karbarz MJ, Luo L, Chang L, Tham CS, Palmer JA, Wilson SJ, Wennerholm ML, Brown SM, Scott BP, Apodaca RL, Keith JM, Wu J, Breitenbucher JG, Chaplan SR, Webb M. Biochemical and biological properties of 4-(3-phenyl-[1,2,4] thiadiazol-5-yl)-piperazine-1-carboxylic acid phenylamide, a mechanism-based inhibitor of fatty acid amide hydrolase. Anesth Analg. 2009 Jan;108(1):316-29. doi: 10.1213/ane.0b013e31818c7cbd. PubMed PMID: 19095868.